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M3 receptor

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Target not currently curated in GtoImmuPdb

Target id: 15

Nomenclature: M3 receptor

Family: Acetylcholine receptors (muscarinic)

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 590 1q43 CHRM3 cholinergic receptor muscarinic 3 33
Mouse 7 589 13 3.72 cM Chrm3 cholinergic receptor, muscarinic 3, cardiac 71
Rat 7 589 17q12.1 Chrm3 cholinergic receptor, muscarinic 3 50,110
Previous and Unofficial Names Click here for help
HM4 [84-85] | Chrm-3 | M3R | cholinergic receptor, muscarinic 3 | cholinergic receptor | cholinergic receptor, muscarinic 3, cardiac
Database Links Click here for help
Specialist databases
GPCRdb acm3_human (Hs), acm3_mouse (Mm), acm3_rat (Rn)
Other databases
Alphafold P20309 (Hs), Q9ERZ3 (Mm), P08483 (Rn)
ChEMBL Target CHEMBL245 (Hs), CHEMBL5105 (Mm), CHEMBL320 (Rn)
DrugBank Target P20309 (Hs)
Ensembl Gene ENSG00000133019 (Hs), ENSMUSG00000046159 (Mm), ENSRNOG00000049410 (Rn)
Entrez Gene 1131 (Hs), 12671 (Mm), 24260 (Rn)
Human Protein Atlas ENSG00000133019 (Hs)
KEGG Gene hsa:1131 (Hs), mmu:12671 (Mm), rno:24260 (Rn)
OMIM 118494 (Hs)
Orphanet ORPHA299148 (Hs)
Pharos P20309 (Hs)
RefSeq Nucleotide NM_000740 (Hs), NM_033269 (Mm), NM_012527 (Rn)
RefSeq Protein NP_000731 (Hs), NP_150372 (Mm), NP_036659 (Rn)
UniProtKB P20309 (Hs), Q9ERZ3 (Mm), P08483 (Rn)
Wikipedia CHRM3 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the M3 Muscarinic Acetylcholine Receptor
PDB Id:  4DAJ
Ligand:  tiotropium
Resolution:  3.4Å
Species:  Rat
References:  56
Natural/Endogenous Ligands Click here for help
acetylcholine

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]iperoxo Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Agonist 8.4 pKd 97
⤷ pKd 8.4 (Kd 3.98x10-9 M) [97]
NNC 11-1585 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.3 pKi 20
⤷ pKi 8.3 [20]
NNC 11-1607 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 pKi 20
⤷ pKi 8.1 [20]
pentylthio-TZTP Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.1 pKi 47
⤷ pKi 8.1 [47]
NNC 11-1314 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.1 – 7.7 pKi 20
⤷ pKi 7.1 – 7.7 [20]
xanomeline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 7.2 – 7.4 pKi 88,117,126
⤷ pKi 7.2 – 7.4 [88,117,126]
sabcomeline Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.0 pKi 126
⤷ pKi 7.0 [126]
arecaidine propargyl ester Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.7 pKi 47
⤷ pKi 5.7 [47]
acetylcholine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Full agonist 5.6 pKi 19
⤷ pKi 5.6 [19]
cevimeline Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist 5.6 pKi 69
⤷ pKi 5.6 (Ki 2.575x10-6 M) [69]
Description: Displacement of [3H]QNB from cloned receptor.
arecoline Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.4 pKi 47,82,94
⤷ pKi 5.4 [47,82,94]
oxotremorine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.3 pKi 47,94
⤷ pKi 5.3 [47,94]
McN-A-343 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.0 – 5.3 pKi 94
⤷ pKi 5.0 – 5.3 [94]
milameline Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.1 pKi 126
⤷ pKi 5.1 [126]
oxotremorine-M Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.1 pKi 47
⤷ pKi 5.1 [47]
pilocarpine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 5.1 pKi 47,94
⤷ pKi 5.1 [47,94]
acetylcholine Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 4.5 – 5.4 pKi 19,47,51
⤷ pKi 4.5 – 5.4 [19,47,51]
methylfurmethide Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.6 pKi 47
⤷ pKi 4.6 [47]
bethanechol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Full agonist 4.2 pKi 47,94
⤷ pKi 4.2 [47,94]
carbachol Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 4.0 – 4.4 pKi 19,47,126
⤷ pKi 4.0 – 4.4 [19,47,126]
carbachol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Full agonist 4.2 pKi 19
⤷ pKi 4.2 [19]
furtrethonium Small molecule or natural product Click here for species-specific activity table Hs Full agonist 4.1 pKi 47
⤷ pKi 4.1 [47]
methacholine Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Rn Agonist 6.9 pEC50 83,94
⤷ pEC50 6.9 (EC50 1.2x10-7 M) [83,94]
(+)-aceclidine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.7 pEC50 29
⤷ pEC50 5.7 [29]
(-)-aceclidine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.1 pEC50 29
⤷ pEC50 5.1 [29]
iperoxo Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist - - 97
⤷ [97]
[3H]acetylcholine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Agonist - -
⤷
View species-specific agonist tables
Agonist Comments
Please consult references [10,30,62,94,115,124] for further details of the activity of some of the ligands in this list.
McN-A-343 has been found to be a partial agonist at the M3 receptor [94,115]. However, in reference [62] it was found to be inactive in a study of GTPase activation.
Oxotremorine has been found to be a full agonist [30,94,115] and a partial agonist [62,94] at the M3 receptor.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]tiotropium Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 10.7 pKd 96
⤷ pKd 10.7 [96]
[3H]QNB Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 10.4 pKd 46,85
⤷ pKd 10.4 (Kd 3.98x10-11 M) [46,85]
CHF-6366 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 10.2 pKd 16
⤷ pKd 10.2 (Kd 6.3x10-11 M) [16]
Description: Binding to human cloned M3 receptor using [3H]-N-methylscopolamine as tracer
[3H]N-methyl scopolamine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Rn Antagonist 10.0 pKd 19,115
⤷ pKd 10.0 [19,115]
[3H]N-methyl scopolamine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.7 – 10.2 pKd 17,43,46-47,52,60
⤷ pKd 9.7 – 10.2 (Kd 2.2x10-10 – 6x10-11 M) [17,43,46-47,52,60]
[3H]darifenacin Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.5 pKd 101
⤷ pKd 9.5 (Kd 3.16x10-10 M) [101]
biperiden Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.4 pKd 6
⤷ pKd 8.4 (Kd 3.9x10-9 M) [6]
N-methyl scopolamine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 10.4 pKi 25
⤷ pKi 10.4 [25]
tiotropium Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 9.5 – 11.1 pKi 24-25,90,107-108
⤷ pKi 9.5 – 11.1 [24-25,90,107-108]
umeclidinium Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 10.2 pKi 57,96
⤷ pKi 10.2 (Ki 6x10-11 M) [57,96]
aclidinium Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 10.1 – 10.2 pKi 90,108
⤷ pKi 10.1 – 10.2 [90,108]
propantheline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 10.0 pKi 44
⤷ pKi 10.0 [44]
AE9C90CB Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.9 pKi 100
⤷ pKi 9.9 [100]
revefenacin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 9.8 pKi 42
⤷ pKi 9.8 (Ki 1.78x10-10 M) [42]
Description: Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM3 receptor, and displacement of [3H]NMS tracer.
clidinium Small molecule or natural product Approved drug Primary target of this compound Hs Antagonist 9.6 pKi 25
⤷ pKi 9.6 [25]
ipratropium Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 9.3 – 9.8 pKi 25,43,90
⤷ pKi 9.3 – 9.8 [25,43,90]
scopolamine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 9.4 pKi 6,44
⤷ pKi 9.4 [6,44]
4-DAMP Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.3 pKi 27
⤷ pKi 9.3 [27]
4-DAMP Small molecule or natural product Click here for species-specific activity table Rn Antagonist 9.2 pKi 50
⤷ pKi 9.2 [50]
atropine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.5 – 9.8 pKi 21,43-44,85
⤷ pKi 8.5 – 9.8 [21,43-44,85]
[3H]4-DAMP Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.8 – 9.4 pKi 18,48
⤷ pKi 8.8 – 9.4 [18,48]
dicyclomine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.0 pKi 3
⤷ pKi 9.0 (Ki 9.3x10-10 M) [3]
atropine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.7 – 9.3 pKi 19,50
⤷ pKi 8.7 – 9.3 [19,50]
darifenacin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.9 – 9.1 pKi 37,43,100
⤷ pKi 8.9 – 9.1 [37,43,100]
hexocyclium Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.9 pKi 11
⤷ pKi 8.9 [11]
silahexocyclium Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.9 pKi 11
⤷ pKi 8.9 [11]
oxybutynin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.8 pKi 23,100
⤷ pKi 8.8 [23,100]
mepenzolic acid Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.6 pKi 129
⤷ pKi 8.6 (Ki 2.6x10-9 M) [129]
tolterodine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.4 – 8.5 pKi 37,100
⤷ pKi 8.4 – 8.5 [37,100]
UH-AH 37 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.1 – 8.2 pKi 37,123
⤷ pKi 8.1 – 8.2 [37,123]
p-F-HHSiD Small molecule or natural product Rn Antagonist 8.0 pKi 50
⤷ pKi 8.0 [50]
amitriptyline Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 7.9 pKi 102
⤷ pKi 7.9 (Ki 1.28x10-8 M) [102]
hexahydrosiladifenidol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.7 – 8.0 pKi 11,31
⤷ pKi 7.7 – 8.0 [11,31]
solifenacin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.7 – 8.0 pKi 45,100
⤷ pKi 7.7 – 8.0 [45,100]
hexahydrodifenidol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 pKi 11
⤷ pKi 7.8 [11]
p-F-HHSiD Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.3 – 7.9 pKi 31,44
⤷ pKi 7.3 – 7.9 [31,44]
dosulepin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.4 pKi 102
⤷ pKi 7.4 (Ki 3.8x10-8 M) [102]
AQ-RA 741 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 – 7.3 pKi 27,37
⤷ pKi 7.2 – 7.3 [27,37]
AFDX384 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.2 pKi 27
⤷ pKi 7.2 [27]
himbacine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.9 – 7.2 pKi 27,49,75
⤷ pKi 6.9 – 7.2 [27,49,75]
tropicamide Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 7.0 pKi 21
⤷ pKi 7.0 [21]
(S)-dimetindene Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.9 pKi 14
⤷ pKi 6.9 (Ki 1.38x10-7 M) [14]
Description: Binding to hM3 receptors expressed in CHO cells.
tripitramine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 76
⤷ pKi 6.8 [76]
pirenzepine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.7 pKi 50
⤷ pKi 6.7 [50]
pirenzepine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.5 – 6.8 pKi 11,27,41,44,49,123
⤷ pKi 6.5 – 6.8 [11,27,41,44,49,123]
methoctramine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 – 6.9 pKi 11,27,31,41,101
⤷ pKi 6.1 – 6.9 [11,27,31,41,101]
guanylpirenzepine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.2 pKi 114
⤷ pKi 6.2 [114]
otenzepad Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 11
⤷ pKi 6.1 [11]
VU0255035 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 pKi 98
⤷ pKi 6.1 [98]
otenzepad Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.0 pKi 50
⤷ pKi 6.0 [50]
muscarinic toxin 3 Peptide Click here for species-specific activity table Hs Antagonist <6.0 pKi 49
⤷ pKi <6.0 [49]
lithocholylcholine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.0 pKi 19
⤷ pKi 6.0 [19]
lithocholylcholine Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.0 pKi 19
⤷ pKi 6.0 [19]
muscarinic toxin 7 Peptide Click here for species-specific activity table Hs Antagonist <5.0 pKi 78
⤷ pKi <5.0 [78]
ML381 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <4.5 pKi 36
⤷ pKi <4.5 (Ki >3x10-5 M) [36]
glycopyrrolate Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 9.6 – 9.8 pIC50 105,107
⤷ pIC50 9.6 – 9.8 [105,107]
Description: Assay uses glycopyrronium bromide
solifenacin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 6.9 pIC50 89
⤷ pIC50 6.9 (IC50 1.308x10-7 M) [89]
View species-specific antagonist tables
Antagonist Comments
Biperiden is an approved drug antagonist of muscarinic acetylcholine receptors. We have tagged the M1 subtype as the drug's primary target as affinity is 10-fold higher at this receptor subtype [6].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
alcuronium Small molecule or natural product Click here for species-specific activity table Hs Negative 5.8 pKd 47
⤷ pKd 5.8 [47]
vincamine Small molecule or natural product Click here for species-specific activity table Hs Neutral 5.7 pKd 47
⤷ pKd 5.7 [47]
WIN 51,708 Small molecule or natural product Click here for species-specific activity table Hs Negative 5.5 pKd 65
⤷ pKd 5.5 [65]
vinburnine Small molecule or natural product Click here for species-specific activity table Hs Neutral 5.2 pKd 47
⤷ pKd 5.2 [47]
Gö 7874 Small molecule or natural product Click here for species-specific activity table Hs Negative 5.1 pKd 64
⤷ pKd 5.1 [64]
WIN 62,577 Small molecule or natural product Click here for species-specific activity table Hs Positive 5.1 pKd 65
⤷ pKd 5.1 (Kd 7.94x10-6 M) [65]
strychnine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Negative 4.2 – 5.7 pKd 47,60
⤷ pKd 4.2 – 5.7 [47,60]
thiochrome Small molecule or natural product Click here for species-specific activity table Hs Neutral 4.4 pKd 61
⤷ pKd 4.4 [61]
N-benzyl brucine Small molecule or natural product Click here for species-specific activity table Hs Negative 3.8 pKd 63
⤷ pKd 3.8 [63]
N-benzyl brucine Small molecule or natural product Click here for species-specific activity table Hs Positive 3.8 pKd 63
⤷ pKd 3.8 [63]
brucine Small molecule or natural product Click here for species-specific activity table Hs Negative 3.6 – 4.0 pKd 47,63
⤷ pKd 3.6 – 4.0 [47,63]
N-chloromethyl-brucine Small molecule or natural product Click here for species-specific activity table Hs Positive 3.3 pKd 63
⤷ pKd 3.3 (Kd 5.012x10-4 M) [63]
brucine N-oxide Small molecule or natural product Click here for species-specific activity table Hs Neutral 2.5 pKd 63
⤷ pKd 2.5 [63]
brucine N-oxide Small molecule or natural product Click here for species-specific activity table Hs Positive 2.5 pKd 63
⤷ pKd 2.5 [63]
VU0119498 Small molecule or natural product Click here for species-specific activity table Hs Positive 5.2 pEC50 9
⤷ pEC50 5.2 (EC50 6.38x10-6 M) [9]
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  8,84
Tissue Distribution Click here for help
Lung.
Species:  Human
Technique:  Radioligand binding.
References:  70
Ciliary muscle.
Species:  Human
Technique:  In situ hybridisation and Northern blotting.
References:  133
Esophageal smooth muscle.
Species:  Human
Technique:  Radioligand binding.
References:  91
Bladder.
Species:  Human
Technique:  RT-PCR.
References:  111
CNS: cerebral cortex, corpus striatum, hippocampus, thalamus, hypothalamus, midbrain, pons-medulla.
Species:  Mouse
Technique:  Radioligand binding.
References:  79
Intestinal smooth muscle.
Species:  Rat
Technique:  Radioligand binding.
References:  15
Heart: intrinsic neurons.
Species:  Rat
Technique:  in situ hybridisation.
References:  40
Gastric smooth muscle.
Species:  Rat
Technique:  RT-PCR.
References:  68
CNS: pons.
Species:  Rat
Technique:  Radioligand binding.
References:  4
CNS: basal forebrain, parabigeminal nucleus, pedunculopontine and laterodorsal tegmental nuclei, cranial nerve nuclei.
Species:  Rat
Technique:  in situ hybridisation.
References:  112
CNS: cerebral cortex, hippocampu, corpus striatum, olfactory tubercle, midbrain, pons-medulla, cerebellum.
Species:  Rat
Technique:  Immunoprecipitation.
References:  130
CNS: hippocampus.
Species:  Rat
Technique:  immunocytochemistry.
References:  67
CNS: limbic cortical regions, striatum, hippocampus, anterior thalamic nuclei, superior colliculus, pontine nuclei.
Species:  Rat
Technique:  immunocytochemistry.
References:  66
Vestibular system.
Species:  Rat
Technique:  RT-PCR.
References:  113
Salivary gland: striated and interlobular duct cells.
Species:  Rat
Technique:  Immunohistochemistry.
References:  99
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of IP levels in isolated rat ventricular cardiomyocytes.
Species:  Rat
Tissue:  Isolated ventricular cardiomyocytes.
Response measured:  Stimulation of IP formation.
References:  92
Measurement of PI hydrolysis in CHO cells transfected with the human M3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of PI hydrolysis.
References:  20
Measurement of IP3 levels in CHO cells transfected with the rat M3 receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation of IP3 accumulation.
References:  19
Measurement of IP1 levels in murine fibroblast cells (B82) transfected with the rat M3 receptor.
Species:  Rat
Tissue:  B82 cells.
Response measured:  Stimulation of IP1 accumulation.
References:  50
Measurement of cAMP and Ca2+ levels in rat parotid cells endogenously expressing the M3 receptor.
Species:  Rat
Tissue:  Parotid cells.
Response measured:  Inhibition of cAMP accumulation and stimulation of Ca2+ mobilisation.
References:  80
Measurement of IP levels in CHO cells transfected with the human M3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IP accumulation.
References:  94,118
Measurement of IP levels in human right atrial slices.
Species:  Human
Tissue:  Atrial slices.
Response measured:  Stimulation of IP formation.
References:  125
Measurement of neuronal nitric oxide synthetase activity in CHO cells transfected with the M3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Increase in NO synthetase activity.
References:  116
Measurement of ERK1/2 activity in COS-7 cells transfected with the human M3 receptor.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  Increase in ERK1/2 activity.
References:  95
Measurement of ERK1/2 activity in CHO cells transfected with the human M3 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Increase in ERK1/2 activity.
References:  12
Measurement of ERK1/2 activity in human SK-N-BE2(C) cells endogenously expressing the M3 receptor.
Species:  Human
Tissue:  SK-N-BE2(C) cells.
Response measured:  Increase in ERK1/2 activity.
References:  54
Measurement of the effects of a ligand on the level, or rate, of binding of GTPγ35S to membranes.
Species:  Human
Tissue:  CHO cells.
Response measured:  The binding of GTPγ35S to G proteins coupled to the receptor.
References:  5,59-62,64-65
Measurement of the effects of a ligand on the rate of hydrolysis of GTP by G proteins in membranes.
Species:  Human
Tissue:  CHO cell membranes.
Response measured:  Generation of 32Pi from [γ-32P]GTP.
References:  62
Physiological Functions Click here for help
Vasodilation.
Species:  Rat
Tissue:  Thoracic aortic rings.
References:  53
Vasodilation
Species:  Mouse
Tissue:  Thoracic aortic rings.
References:  53
Stimulation of pancreatic insulin and glucagon release.
Species:  Mouse
Tissue:  In vivo.
References:  26
Bronchoconstriction.
Species:  Rat
Tissue:  Isolated lung.
References:  87
Modulation of salivary gland function.
Species:  Rat
Tissue:  In vivo.
References:  109
Modulation of excitatory transmission.
Species:  Rat
Tissue:  Mesencephalic slices.
References:  39
Gastric acid secretion.
Species:  Rat
Tissue:  Gastric parietal cells.
References:  86
Modulation of insulin secretion.
Species:  Rat
Tissue:  Isolated pancreatic islets.
References:  93
Vasodilation.
Species:  Rat
Tissue:  Pulmonary artery.
References:  74
Stimulation of urination.
Species:  Rat
Tissue:  In vivo.
References:  55
Contraction.
Species:  Human
Tissue:  Urinary bladder detrusor muscle.
References:  22
Contraction.
Species:  Rat
Tissue:  Urinary bladder detrusor muscle.
References:  81
Contraction.
Species:  Human
Tissue:  Esophageal smooth muscle.
References:  91
Contraction.
Species:  Rat
Tissue:  Ileum.
References:  15
Physiological Consequences of Altering Gene Expression Click here for help
M3 receptor knockout mice exhibit impaired gastric acid secretion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  1-2
M3 receptor knockout mice show reduced adiposity and serum insulin and leptin levels, and exhibit reduced food intake.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  128
Lung slices from M3 receptor knockout mice exhibit reduced agonist-induced bronchoconstriction compared to wild-type mice.
This bronchoconstriction is completely abolished in M2/M3 double knockout mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  106
M3 receptor knockout mice exhibit abolished agonist-induced or vagally-stimulated bronchoconstriction in vivo.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  32
Isolated coronary arteries and aortic rings from M3 receptor knockout mice exhibit a reduction in agonist-induced dilation compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  58
M3 receptor knockout mice exhibit alterations in paradoxical sleep.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  38
M3 receptor knockout mice exhibit growth retardation, increased pupil size and reduced salivary secretion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  72
Striatal slices from M3 receptor knockout mice exhibit an increase in muscarinic agonist-induced potentiation of dopamine release.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  132
M3 receptor knockout mice exhibit abolished agonist-induced PLC activation and insulin secretion from pancreatic islets.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  131
M3 receptor knockout mice exhibit altered ventilatory pattern and chemosensitivity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  7
M3 receptor knockout mice exhibit impaired salivation.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  77
M3 receptor knockout mice exhibit abolished agonist-induced pancreatic insulin and glucagon release as seen in wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  26
M3 receptor knockout mice exhibit reduced gastric pepsinogen secretion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  127
Thoracic aortic rings from M3 receptor knockout mice exhibit reduced agonist-induced relaxation compared to those from wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  53
Transgenic mice overexpressing the M3 receptor in pancreatic β-cells exhibit increased glucose tolerance and insulin release. They are resistant to diet-induced glucose intolerance and hyperglycemia.
Species:  Mouse
Tissue: 
Technique:  Transgenesis.
References:  35
Mice that selectively lack the M3 receptor in pancreatic β-cells exhibit decreased glucose tolerance and impaired insulin release.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  35
M3 receptor knockout mice express an increase in basal and total energy expenditure.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  34
Smooth muscle preparations (gallbladder, urinary bladder, stomach fundus, trachea, ileum) from M3 receptor knockout mice exhibit reduced agonist-induced contractions compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  28,72,103-104
Smooth muscle preparations (gallbladder, urinary bladder, stomach fundus, trachea) from M3 receptor knockout mice exhibit reduced agonist-induced contractions compared to wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  72,103-104
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0004994 abnormal brain wave pattern PMID: 16110248 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac		 MGI:88398  MP:0001663 abnormal digestive system physiology PMID: 11959688 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0003194 abnormal frequency of paradoxical sleep PMID: 16110248 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0005085 abnormal gallbladder physiology PMID: 11961069 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0002078 abnormal glucose homeostasis PMID: 11242080 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
B6.129X1-Chrm3		 MGI:88398  MP:0002503 abnormal histamine physiology PMID: 15691866 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ		 MGI:88398  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 12859343 
Chrm1tm1Kano|Chrm3tm1Mmt Chrm1tm1Kano/Chrm1tm1Kano,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88396  MGI:88398  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 12859343 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac		 MGI:88398  MP:0002133 abnormal respiratory system physiology PMID: 11959688 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ		 MGI:88398  MP:0005310 abnormal salivary gland physiology PMID: 15146045 
Chrm1tm1Kano|Chrm3tm1Mmt Chrm1tm1Kano/Chrm1tm1Kano,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88396  MGI:88398  MP:0005310 abnormal salivary gland physiology PMID: 15146045 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0000538 abnormal urinary bladder morphology PMID: 10944224 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac		 MGI:88398  MP:0010386 abnormal urinary bladder physiology PMID: 11959688 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0001945 bronchoconstriction PMID: 14645675 
Chrm2tm1Jwe|Chrm3tm1Jwe Chrm2tm1Jwe/Chrm2tm1Jwe,Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S4/SvJae * 129S6/SvEvTac * CF-1		 MGI:88397  MGI:88398  MP:0001945 bronchoconstriction PMID: 14645675 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0001265 decreased body size PMID: 10944224 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0005534 decreased body temperature PMID: 11242080 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0001262 decreased body weight PMID: 10944224 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0001262 decreased body weight PMID: 11242080  15220195 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
129S6/SvEvTac-Chrm3		 MGI:88398  MP:0001262 decreased body weight PMID: 11242080 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac		 MGI:88398  MP:0001262 decreased body weight PMID: 11959688 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0002696 decreased circulating glucagon level PMID: 15220195 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0005560 decreased circulating glucose level PMID: 15220195 
Chrm3tm2.1Jwe|Tg(Alb-cre)21Mgn Chrm3tm2.1Jwe/Chrm3tm2.1Jwe,Tg(Alb-cre)21Mgn/0
involves: 129S6/SvEvTac * C57BL/6 * DBA * FVB/N		 MGI:2176226  MGI:88398  MP:0005560 decreased circulating glucose level PMID: 19752163 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0002727 decreased circulating insulin level PMID: 11242080  15220195 
Chrm3+|Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3+
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0002727 decreased circulating insulin level PMID: 15220195 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0005668 decreased circulating leptin level PMID: 11242080 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0002644 decreased circulating triglyceride level PMID: 11242080 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
B6.129X1-Chrm3		 MGI:88398  MP:0000505 decreased digestive secretion PMID: 15691866 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0003910 decreased eating behavior PMID: 11242080 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0002711 decreased glucagon secretion PMID: 15220195 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0009283 decreased gonadal fat pad weight PMID: 11242080 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
129S6/SvEvTac-Chrm3		 MGI:88398  MP:0009283 decreased gonadal fat pad weight PMID: 11242080 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0003059 decreased insulin secretion PMID: 15220195 
Chrm3tm2Jwe|Tg(Ins2-cre)25Mgn Chrm3tm2Jwe/Chrm3tm2Jwe,Tg(Ins2-cre)25Mgn/0
involves: 129S6/SvEvTac * C57BL/6 * DBA		 MGI:2176225  MGI:88398  MP:0003059 decreased insulin secretion PMID: 16753580 
Chrm3+|Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3+
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0003059 decreased insulin secretion PMID: 15220195 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ		 MGI:88398  MP:0000623 decreased salivation PMID: 15146045 
Chrm1tm1Kano|Chrm3tm1Mmt Chrm1tm1Kano/Chrm1tm1Kano,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88396  MGI:88398  MP:0000623 decreased salivation PMID: 15146045 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0000623 decreased salivation PMID: 10944224 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0005591 decreased vasodilation PMID: 15130910 
Chrm2tm1Minm|Chrm3tm1Mmt Chrm2tm1Minm/Chrm2tm1Minm,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88397  MGI:88398  MP:0000539 distended urinary bladder PMID: 12486155 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0000539 distended urinary bladder PMID: 10944224 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0000519 hydronephrosis PMID: 10944224 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0009454 impaired contextual conditioning behavior PMID: 20439723 
Chrm3tm1Abt Chrm3tm1Abt/Chrm3tm1Abt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0009454 impaired contextual conditioning behavior PMID: 20439723 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0000741 impaired contractility of detrusor smooth muscle PMID: 10944224 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ		 MGI:88398  MP:0000742 impaired contractility of ileal smooth muscle PMID: 12486155 
Chrm2tm1Minm|Chrm3tm1Mmt Chrm2tm1Minm/Chrm2tm1Minm,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88397  MGI:88398  MP:0000742 impaired contractility of ileal smooth muscle PMID: 12486155 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0000742 impaired contractility of ileal smooth muscle PMID: 10944224 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0009456 impaired cued conditioning behavior PMID: 20439723 
Chrm3tm1Abt Chrm3tm1Abt/Chrm3tm1Abt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0009456 impaired cued conditioning behavior PMID: 20439723 
Chrm3tm2Jwe|Tg(Ins2-cre)25Mgn Chrm3tm2Jwe/Chrm3tm2Jwe,Tg(Ins2-cre)25Mgn/0
involves: 129S6/SvEvTac * C57BL/6 * DBA		 MGI:2176225  MGI:88398  MP:0005293 impaired glucose tolerance PMID: 16753580 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ		 MGI:88398  MP:0000740 impaired smooth muscle contractility PMID: 12486155 
Chrm2tm1Minm|Chrm3tm1Mmt Chrm2tm1Minm/Chrm2tm1Minm,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88397  MGI:88398  MP:0000740 impaired smooth muscle contractility PMID: 12486155 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * CF-1		 MGI:88398  MP:0000740 impaired smooth muscle contractility PMID: 11961069 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac		 MGI:88398  MP:0000740 impaired smooth muscle contractility PMID: 11959688 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0005292 improved glucose tolerance PMID: 15220195 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ		 MGI:88398  MP:0003911 increased drinking behavior PMID: 15146045 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0002891 increased insulin sensitivity PMID: 11242080 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ		 MGI:88398  MP:0002546 mydriasis PMID: 12486155 
Chrm2tm1Minm|Chrm3tm1Mmt Chrm2tm1Minm/Chrm2tm1Minm,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88397  MGI:88398  MP:0002546 mydriasis PMID: 12486155 
Chrm3tm1Mmt Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88398  MP:0002546 mydriasis PMID: 10944224 
Chrm2tm1Minm|Chrm3tm1Mmt Chrm2tm1Minm/Chrm2tm1Minm,Chrm3tm1Mmt/Chrm3tm1Mmt
involves: 129X1/SvJ * C57BL/6		 MGI:88397  MGI:88398  MP:0001732 postnatal growth retardation PMID: 12486155 
Chrm3tm1Jwe Chrm3tm1Jwe/Chrm3tm1Jwe
involves: 129S6/SvEvTac * C57BL/6J		 MGI:88398  MP:0001263 weight loss PMID: 11242080 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Prune belly syndrome
Synonyms: Abdominal muscles, absence of, with urinary tract abnormality and cryptorchidism
Eagle-Barrett syndrome
OMIM: 100100
Orphanet: ORPHA2970
References:  119
General Comments
For reviews on muscarinic receptor knockout mice see [13,73,120-122].

References

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2. Aihara T, Nakamura Y, Taketo MM, Matsui M, Okabe S. (2005) Cholinergically stimulated gastric acid secretion is mediated by M(3) and M(5) but not M(1) muscarinic acetylcholine receptors in mice. Am J Physiol Gastrointest Liver Physiol, 288 (6): G1199-207. [PMID:15691866]

3. Auerbach SS, DrugMatrix® and ToxFX® Coordinator National Toxicology Program. National Toxicology Program: Dept of Health and Human Services. Accessed on 02/05/2014. Modified on 02/05/2014. DrugMatrix, https://ntp.niehs.nih.gov/drugmatrix/index.html

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13. Bymaster FP, McKinzie DL, Felder CC, Wess J. (2003) Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res, 28 (3-4): 437-42. [PMID:12675128]

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16. Carzaniga L, Linney ID, Rizzi A, Delcanale M, Schmidt W, Knight CK, Pastore F, Miglietta D, Carnini C, Cesari N et al.. (2022) Discovery of Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β2 Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases. J Med Chem, 65 (15): 10233-10250. [PMID:35901125]

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