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M5 receptor

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Target not currently curated in GtoImmuPdb

Target id: 17

Nomenclature: M5 receptor

Family: Acetylcholine receptors (muscarinic)

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 7 532 15q14 CHRM5 cholinergic receptor muscarinic 5 6
Mouse 7 532 2 57.02 cM Chrm5 cholinergic receptor, muscarinic 5 46
Rat 7 531 3q35 Chrm5 cholinergic receptor, muscarinic 5 6,38,44,65
Previous and Unofficial Names Click here for help
M5R | cholinergic receptor, muscarinic 5 | cholinergic receptor
Database Links Click here for help
Specialist databases
GPCRDB acm5_human (Hs), acm5_mouse (Mm), acm5_rat (Rn)
Other databases
Alphafold
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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
NNC 11-1585 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.3 pKi 16
pKi 8.3 [16]
NNC 11-1607 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 8.2 pKi 16
pKi 8.2 [16]
NNC 11-1314 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.8 pKi 16
pKi 7.8 [16]
sabcomeline Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 7.1 pKi 80
pKi 7.1 [80]
xanomeline Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 6.7 – 7.4 pKi 31,73,80
pKi 6.7 – 7.4 [31,73,80]
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 6.1 pKi 14
pKi 6.1 [14]
milameline Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.4 pKi 80
pKi 5.4 [80]
pilocarpine Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Partial agonist 5.0 pKi 4,19,31
pKi 5.0 [4,19,31]
McN-A-343 Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 4.9 pKi 54
pKi 4.9 [54]
carbachol Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Full agonist 4.9 pKi 4,31,80
pKi 4.9 [4,31,80]
(+)-aceclidine Small molecule or natural product Click here for species-specific activity table Hs Full agonist 5.5 pEC50 21
pEC50 5.5 [21]
(-)-aceclidine Small molecule or natural product Click here for species-specific activity table Hs Partial agonist 5.1 pEC50 21
pEC50 5.1 [21]
arecoline Small molecule or natural product Click here for species-specific activity table Hs Agonist - - 52,54
[52,54]
bethanechol Small molecule or natural product Approved drug Click here for species-specific activity table Hs Agonist - - 54
[54]
iperoxo Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Agonist - - 56
[56]
methacholine Small molecule or natural product Approved drug Immunopharmacology Ligand Hs Agonist - - 54
[54]
Agonist Comments
Please consult references [9,41,54,71] for further details of the activity of some of the ligands in this list.
Oxotremorine has also been found to be a partial agonist at the M5 receptor [54,71] (no binding data available).
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]QNB Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 10.2 – 10.7 pKd 36
pKd 10.2 – 10.7 (Kd 6x10-11 – 2x10-11 M) [36]
[3H]N-methyl scopolamine Small molecule or natural product Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.3 – 9.7 pKd 13-14,34,36,39,68,71
pKd 9.3 – 9.7 (Kd 4.8x10-10 – 2x10-10 M) [13-14,34,36,39,68,71]
biperiden Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.2 pKd 5
pKd 8.2 (Kd 6.3x10-9 M) [5]
guanylpirenzepine Small molecule or natural product ? Antagonist 6.8 pKd 24
pKd 6.8 (Kd 1.75x10-7 M) [24]
tiotropium Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 9.8 – 10.2 pKi 62-63
pKi 9.8 – 10.2 [62-63]
umeclidinium Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 9.9 pKi 55
pKi 9.9 [55]
aclidinium Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 9.9 pKi 63
pKi 9.9 [63]
AE9C90CB Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.5 pKi 58
pKi 9.5 [58]
atropine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 9.4 pKi 38
pKi 9.4 [38]
glycopyrrolate Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 8.9 – 9.9 pKi 61-62
pKi 8.9 – 9.9 [61-62]
4-DAMP Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 20
pKi 9.0 [20]
4-DAMP Small molecule or natural product Click here for species-specific activity table Rn Antagonist 8.9 pKi 38
pKi 8.9 [38]
atropine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.3 – 9.3 pKi 17,34,50
pKi 8.3 – 9.3 [17,34,50]
ipratropium Small molecule or natural product Approved drug Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 8.8 pKi 34
pKi 8.8 [34]
scopolamine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.7 pKi 5
pKi 8.7 [5]
silahexocyclium Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.7 pKi 10
pKi 8.7 [10]
tolterodine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.5 – 8.8 pKi 30,58
pKi 8.5 – 8.8 [30,58]
hexocyclium Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 pKi 10
pKi 8.4 [10]
UH-AH 37 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.3 pKi 30,79
pKi 8.3 [30,79]
darifenacin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.9 – 8.6 pKi 30,34,58
pKi 7.9 – 8.6 [30,34,58]
revefenacin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 8.2 pKi 33
pKi 8.2 (Ki 6.31x10-9 M) [33]
Description: Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM5 receptor, and displacement of [3H]NMS tracer.
oxybutynin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.9 pKi 18,58
pKi 7.9 [18,58]
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 7.8 pKi 60
pKi 7.8 (Ki 1.57x10-8 M) [60]
tripitramine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.5 pKi 45
pKi 7.5 [45]
hexahydrosiladifenidol Small molecule or natural product Click here for species-specific activity table Rn Antagonist 7.4 pKi 38
pKi 7.4 [38]
solifenacin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.2 pKi 58
pKi 7.2 [58]
hexahydrodifenidol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.1 pKi 10
pKi 7.1 [10]
pirenzepine Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 7.1 pKi 38
pKi 7.1 [38]
dosulepin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.0 pKi 60
pKi 7.0 (Ki 9.2x10-8 M) [60]
hexahydrosiladifenidol Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 – 7.2 pKi 10,23
pKi 6.8 – 7.2 [10,23]
pirenzepine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.8 – 7.1 pKi 32,37,79
pKi 6.8 – 7.1 [32,37,79]
AQ-RA 741 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.1 – 7.8 pKi 20,30
pKi 6.1 – 7.8 [20,30]
methoctramine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 – 7.2 pKi 10,20,23,32
pKi 6.3 – 7.2 [10,20,23,32]
tropicamide Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 6.4 pKi 17
pKi 6.4 [17]
p-F-HHSiD Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 23
pKi 6.3 [23]
AFDX384 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 20
pKi 6.3 [20]
ML381 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.3 pKi 27
pKi 6.3 [27]
(S)-dimetindene Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 6.1 pKi 12
pKi 6.1 (Ki 7.586x10-7 M) [12]
Description: Binding to hM5 receptors expressed in CHO cells.
muscarinic toxin 3 Peptide Click here for species-specific activity table Hs Antagonist <6.0 pKi 37
pKi <6.0 [37]
himbacine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.4 – 6.5 pKi 20,37,49
pKi 5.4 – 6.5 [20,37,49]
otenzepad Small molecule or natural product Click here for species-specific activity table Rn Antagonist 5.7 pKi 38
pKi 5.7 [38]
otenzepad Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 10
pKi 5.6 [10]
VU0255035 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.6 pKi 57
pKi 5.6 [57]
lithocholylcholine Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.2 pKi 14
pKi 5.2 [14]
muscarinic toxin 7 Peptide Click here for species-specific activity table Hs Antagonist <5.0 pKi 51
pKi <5.0 [51]
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 [5].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
amiodarone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Positive 7.3 pKB 59
pKB 7.3 [59]
ML375 Small molecule or natural product Hs Negative 6.2 – 6.6 pKB 28,68
pKB 6.2 – 6.6 [28,68]
ML380 Small molecule or natural product Hs Positive 4.8 pKB 4,29
pKB 4.8 [4,29]
N-chloromethyl-brucine Small molecule or natural product Click here for species-specific activity table Hs Negative 4.4 pKd 42
pKd 4.4 [42]
N-benzyl brucine Small molecule or natural product Click here for species-specific activity table Hs Negative 3.7 pKd 42
pKd 3.7 [42]
N-benzyl brucine Small molecule or natural product Click here for species-specific activity table Hs Neutral 3.7 pKd 42
pKd 3.7 [42]
strychnine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Negative 3.6 pKd 40
pKd 3.6 [40]
brucine Small molecule or natural product Click here for species-specific activity table Hs Negative 2.9 pKd 42
pKd 2.9 [42]
brucine N-oxide Small molecule or natural product Click here for species-specific activity table Hs Negative 2.3 pKd 42
pKd 2.3 [42]
brucine N-oxide Small molecule or natural product Click here for species-specific activity table Hs Positive 2.3 pKd 42
pKd 2.3 [42]
VU0238429 Small molecule or natural product Hs Positive 5.9 pEC50 7
pEC50 5.9 (EC50 1.16x10-6 M) [7]
VU0119498 Small molecule or natural product Click here for species-specific activity table Hs Positive 5.4 pEC50 7
pEC50 5.4 (EC50 4.08x10-6 M) [7]
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  8
Tissue Distribution Click here for help
Ciliary muscle.
Species:  Human
Technique:  In situ hybridisation and Northern blotting.
References:  87
Esophageal smooth muscle.
Species:  Human
Technique:  Radioligand binding.
References:  53
Vestibular system.
Species:  Human
Technique:  RT-PCR.
References:  69
Bladder.
Species:  Human
Technique:  RT-PCR.
References:  66
Vestibular system.
Species:  Rat
Technique:  RT-PCR.
References:  69
CNS: basal forebrain, parabigeminal nucleus.
Species:  Rat
Technique:  in situ hybridisation.
References:  67
CNS: cerebral cortex, hippocampus, corpus striatum, olfactory tubercle, midbrain, pons-medulla, cerebellum.
Species:  Rat
Technique:  Immunoprecipitation.
References:  84
CNS: substantia nigra, pars compacta and vental tegmental area.
Species:  Rat
Technique:  in situ hybridisation.
References:  75
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 IP1 levels in CHO cells transfected with the human M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IP1 accumulation.
References:  54
Measurement of IP1 levels in murine fibroblast cells (B82) transfected with the rat M5 receptor.
Species:  Rat
Tissue:  B82 cells.
Response measured:  Stimulation of IP1 accumulation.
References:  38
Measurement of PLC activity and Ca2+ levels in murine L cells transfected with the rat M5 receptor.
Species:  Rat
Tissue:  Murine L cells.
Response measured:  Stimulation of PLC activity and Ca2+ mobilisation.
References:  43
Measurement of the levels of IPs in CHO cells transfected with the human M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IPs accumulation.
References:  74
Measurement of Ca2+ levels in Sf9 cells transfected with the rat M5 receptor.
Species:  Rat
Tissue:  Sf9 cells.
Response measured:  Ca2+ mobilisation.
References:  35
Measurement of PI hydrolysis in CHO cells transfected with the human M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of PI hydrolysis.
References:  16
Measurement of NO synthetase activity in CHO cells transfected with the M5 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Activation of nitric oxide synthetase.
References:  72
Measurement of ERK1/2 activity.
Species:  Human
Tissue: 
Response measured:  Increase in ERK1/2 activity.
References:  81
Physiological Functions Click here for help
Modulation of dopaminergic neurotransmission.
Species:  Rat
Tissue:  In vivo (nucleus accumbens/striatum).
References:  48
Stimulation of gastric acid secretion.
Species:  Mouse
Tissue:  In vivo (stomach).
References:  1
Vasodilation.
Species:  Human
Tissue:  Intracortical arterioles.
References:  22
Physiological Consequences of Altering Gene Expression Click here for help
M5 receptor knockout mice exhibit impaired gastric acid secretion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  1
M5 receptor knockout mice exhibit a reduction in the reinforcing effects and withdrawal symptoms of morphine.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  3
M5 receptor knockout mice exhibit a lack of agonist-induced cerebral blood vessel dilation, as seen in wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  83
Striatal slices from M5 receptor knockout mice exhibit a decrease in agonist-induced potentiation of dopamine release.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  83,86
M5 receptor knockout mice exhibit a reduction in the reinforcing effects and withdrawal symptoms of cocaine.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  25,64
M5 receptor knockout mice exhibit an increase in antagonist-induced locomotion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  15
M5 receptor knockout mice exhibit an abolished late phase activation of dopaminergic neurons.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  26,85
M5 receptor knockout mice exhibit an increase in D2 receptor expression in some brain areas, a decrease in amphetamine-induced locomotion and an increase in latent inhibition.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  70
M5 muscarinic receptor knockout mice show significantly reduced cerebral blood flow and exhibit impairments in hippocampus-dependent learning and hippocampal neuronal plasticity.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  2
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
Chrm5tm1Jwe Chrm5tm1Jwe/Chrm5tm1Jwe
involves: 129S6/SvEvTac * CF-1
MGI:109248  MP:0001905 abnormal dopamine level PMID: 11707605 
Chrm5tm1Minm Chrm5tm1Minm/Chrm5tm1Minm
B6.129X1-Chrm5
MGI:109248  MP:0002503 abnormal histamine physiology PMID: 15691866 
Chrm5tm1Jabe Chrm5tm1Jabe/Chrm5tm1Jabe
involves: C57BL/6
MGI:109248  MP:0010149 abnormal synaptic dopamine release PMID: 20664521 
Chrm5tm1Jwe Chrm5tm1Jwe/Chrm5tm1Jwe
B6.129S6-Chrm5
MGI:109248  MP:0010149 abnormal synaptic dopamine release PMID: 20664521 
Chrm5tm1Jwe Chrm5tm1Jwe/Chrm5tm1Jwe
involves: 129S6/SvEvTac * CF-1
MGI:109248  MP:0001613 abnormal vasodilation PMID: 11707605 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
involves: 129X1/SvJ * CD-1
MGI:109248  MP:0001529 abnormal vocalization PMID: 18382674 
Chrm5tm1Minm Chrm5tm1Minm/Chrm5tm1Minm
B6.129X1-Chrm5
MGI:109248  MP:0000505 decreased digestive secretion PMID: 15691866 
Chrm1tm1Kano|Chrm5tm1Minm Chrm1tm1Kano/Chrm1tm1Kano,Chrm5tm1Minm/Chrm5tm1Minm
involves: 129X1/SvJ * C57BL/6
MGI:109248  MGI:88396  MP:0000505 decreased digestive secretion PMID: 15691866 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
Not Specified
MGI:109248  MP:0000623 decreased salivation PMID: 11900778 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
Not Specified
MGI:109248  MP:0005111 hyperdipsia PMID: 11900778 
Chrm5tm1Yeo Chrm5tm1Yeo/Chrm5tm1Yeo
involves: 129X1/SvJ * CD-1
MGI:109248  MP:0009750 impaired behavioral response to addictive substance PMID: 18382674 
General Comments
For reviews on muscarinic receptor knockout mice see [11,47,76-78].
For a review specifically on M5 receptor knockout mice see [82].

References

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1. 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]

2. Araya R, Noguchi T, Yuhki M, Kitamura N, Higuchi M, Saido TC, Seki K, Itohara S, Kawano M, Tanemura K et al.. (2006) Loss of M5 muscarinic acetylcholine receptors leads to cerebrovascular and neuronal abnormalities and cognitive deficits in mice. Neurobiol Dis, 24 (2): 334-44. [PMID:16956767]

3. Basile AS, Fedorova I, Zapata A, Liu X, Shippenberg T, Duttaroy A, Yamada M, Wess J. (2002) Deletion of the M5 muscarinic acetylcholine receptor attenuates morphine reinforcement and withdrawal but not morphine analgesia. Proc Natl Acad Sci USA, 99 (17): 11452-7. [PMID:12154229]

4. Berizzi AE, Gentry PR, Rueda P, Den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A. (2016) Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators. Mol Pharmacol, 90 (4): 427-36. [PMID:27461343]

5. Bolden C, Cusack B, Richelson E. (1992) Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells. J Pharmacol Exp Ther, 260 (2): 576-80. [PMID:1346637]

6. Bonner TI, Young AC, Brann MR, Buckley NJ. (1988) Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes. Neuron, 1 (5): 403-10. [PMID:3272174]

7. Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. (2009) Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem, 52 (11): 3445-8. [PMID:19438238]

8. Bräuner-Osborne H, Brann MR. (1996) Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): high throughput assays in mammalian cells. Eur J Pharmacol, 295 (1): 93-102. [PMID:8925880]

9. Bräuner-Osborne H, Ebert B, Brann MR, Falch E, Krogsgaard-Larsen P. (1996) Functional partial agonism at cloned human muscarinic acetylcholine receptors. Eur J Pharmacol, 313 (1-2): 145-50. [PMID:8905341]

10. Buckley NJ, Bonner TI, Buckley CM, Brann MR. (1989) Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells. Mol Pharmacol, 35 (4): 469-76. [PMID:2704370]

11. 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]

12. Böhme TM, Keim C, Kreutzmann K, Linder M, Dingermann T, Dannhardt G, Mutschler E, Lambrecht G. (2003) Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists. J Med Chem, 46 (5): 856-67. [PMID:12593665]

13. Cembala TM, Sherwin JD, Tidmarsh MD, Appadu BL, Lambert DG. (1998) Interaction of neuromuscular blocking drugs with recombinant human m1-m5 muscarinic receptors expressed in Chinese hamster ovary cells. Br J Pharmacol, 125 (5): 1088-94. [PMID:9846649]

14. Cheng K, Khurana S, Chen Y, Kennedy RH, Zimniak P, Raufman JP. (2002) Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist. J Pharmacol Exp Ther, 303 (1): 29-35. [PMID:12235229]

15. Chintoh A, Fulton J, Koziel N, Aziz M, Sud M, Yeomans JS. (2003) Role of cholinergic receptors in locomotion induced by scopolamine and oxotremorine-M. Pharmacol Biochem Behav, 76 (1): 53-61. [PMID:13679217]

16. Christopoulos A, Grant MK, Ayoubzadeh N, Kim ON, Sauerberg P, Jeppesen L, El-Fakahany EE. (2001) Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists. J Pharmacol Exp Ther, 298 (3): 1260-8. [PMID:11504829]

17. Croy CH, Chan WY, Castetter AM, Watt ML, Quets AT, Felder CC. (2016) Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol, 782: 70-6. [PMID:27085897]

18. Del Bello F, Barocelli E, Bertoni S, Bonifazi A, Camalli M, Campi G, Giannella M, Matucci R, Nesi M, Pigini M et al.. (2012) 1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists. J Med Chem, 55 (4): 1783-7. [PMID:22243489]

19. Dong GZ, Kameyama K, Rinken A, Haga T. (1995) Ligand binding properties of muscarinic acetylcholine receptor subtypes (m1-m5) expressed in baculovirus-infected insect cells. J Pharmacol Exp Ther, 274 (1): 378-84. [PMID:7616422]

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