CB1 receptor

Target id: 56

Nomenclature: CB1 receptor

Family: Cannabinoid receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     CB1 receptor has curated GtoImmuPdb data

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 472 6q14-q15 CNR1 cannabinoid receptor 1 20,28
Mouse 7 473 4 A5 Cnr1 cannabinoid receptor 1 (brain) 7
Rat 7 473 5q21 Cnr1 cannabinoid receptor 1 50
Previous and Unofficial Names
Names References
Central cannabinoid receptor
Neuronal cannabinoid receptor
THC receptor
CB-R
Cann6 68
SKR6R
CB1R
Cann7
Database Links
Specialist databases
GPCRDB cnr1_human (Hs), cnr1_mouse (Mm), cnr1_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of the Human Cannabinoid Receptor CB1
PDB Id:  5TGZ
Ligand:  AM6538
Resolution:  2.8Å
Species:  Human
References:  31
Image of receptor 3D structure from RCSB PDB
Description:  High-resolution crystal structure of the human CB1 cannabinoid receptor
PDB Id:  5TJV
Ligand:  taranabant
Resolution:  2.6Å
Species:  Human
References:  64
Natural/Endogenous Ligands
anandamide
2-arachidonoylglycerol
Comments: Endogenous ligands include other endocannabinoids

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]HU-243 Rn Full agonist 10.4 pKd 10
pKd 10.4 [10]
[3H]CP55940 Hs Full agonist 8.5 – 9.4 pKd 4-5,15,21,66,69
pKd 8.5 – 9.4 [4-5,15,21,66,69]
[3H]WIN55212-2 Hs Full agonist 7.8 – 7.9 pKd 9,71
pKd 7.8 – 7.9 [9,71]
HU-210 Hs Full agonist 9.1 – 10.2 pKi 14,69
pKi 9.1 – 10.2 [14,69]
arachidonyl-2-chloroethylamide Rn Full agonist 8.9 pKi 26
pKi 8.9 [26]
CP55940 Hs Full agonist 8.3 – 9.2 pKi 14,62,69
pKi 8.3 – 9.2 [14,62,69]
arachidonylcyclopropylamide Rn Full agonist 8.7 pKi 26
pKi 8.7 [26]
AM7499 Rn Agonist 8.6 pKi 39
pKi 8.6 (Ki 2.4x10-9 M) [39]
O-1812 Rn Full agonist 8.5 pKi 11
pKi 8.5 (Ki 3.16x10-9 M) [11]
nabilone Hs Agonist 8.4 pKi 3
pKi 8.4 (Ki 3.98x10-9 M) [3]
WIN55212-2 Hs Full agonist 6.9 – 8.7 pKi 14,67,69
pKi 6.9 – 8.7 [14,67,69]
R-(+)-methanandamide Rn Agonist 7.7 pKi 37
pKi 7.7 (Ki 2x10-8 M) [37]
Δ9-tetrahydrocannabinol Hs Partial agonist 7.3 – 7.4 pKi 14,69
pKi 7.3 – 7.4 [14,69]
2-arachidonoylglycerol Rn Full agonist 6.3 – 7.2 pKi 2,51
pKi 6.3 – 7.2 [2,51]
anandamide Hs Partial agonist 6.3 – 7.0 pKi 14,69
pKi 6.3 – 7.0 [14,69]
cannabinol Hs Partial agonist 6.0 – 6.5 pKi 14,69
pKi 6.0 – 6.5 [14,69]
View species-specific agonist tables
Agonist Comments
The higher pKi value of anandamide (7.05) was determined in the presence of phenylmethylsulfonyl fluoride to prevent enzymic hydrolysis. For reviews see references [29,53-54].
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[123I]AM251 Mm Antagonist 9.6 pKd 18
pKd 9.6 [18]
[3H]rimonabant Rn Antagonist 8.9 – 10.0 pKd 6,27,36,55,61,70,74
pKd 8.9 – 10.0 (Kd 1.2x10-9 – 1x10-10 M) [6,27,36,55,61,70,74]
taranabant Hs Inverse agonist 9.5 pKi 16
pKi 9.5 (Ki 3x10-10 M) [16]
Description: Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting.
otenabant Hs Inverse agonist 9.1 pKi 23
pKi 9.1 (Ki 7x10-10 M) [23]
Description: Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells
otenabant Rn Inverse agonist 8.6 pKi 23
pKi 8.6 (Ki 2.8x10-9 M) [23]
Description: Displacement of [3H]SR141716A from CB1 receptor in rat brain
surinabant Hs Antagonist 8.5 pKi 59
pKi 8.5 (Ki 3.5x10-9 M) [59]
Description: Inhibition of [3H]CP-55940 binding to human cannabinoid receptor 1 expressed in CHO cells
AM6538 Hs Antagonist 8.3 pKi 31
pKi 8.3 (Ki 4.6x10-9 M) [31]
Description: Competition binding assay using [3H]-CP55,940
rimonabant Hs Antagonist 7.9 – 8.7 pKi 13-14,60,63,69
pKi 7.9 – 8.7 (Ki 1.26x10-8 – 1.99x10-9 M) [13-14,60,63,69]
compound 70 [PMID: 26161824] Hs Antagonist 8.1 pKi 65
pKi 8.1 (Ki 7x10-9 M) [65]
ibipinabant Hs Antagonist 8.1 pKi 42
pKi 8.1 (Ki 7.8x10-9 M) [42]
Description: Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells
AM251 Rn Antagonist 8.1 pKi 41
pKi 8.1 (Ki 7.94x10-9 M) [41]
AM281 Rn Antagonist 7.9 pKi 40
pKi 7.9 (Ki 1.26x10-8 M) [40]
LY320135 Hs Antagonist 6.9 pKi 13
pKi 6.9 (Ki 1.26x10-7 M) [13]
TM-38837 Hs Antagonist 8.1 pIC50 32
pIC50 8.1 (IC50 8.5x10-9 M) [32]
View species-specific antagonist tables
Antagonist Comments
AM6538 behaves as a competitive antagonist in functional assays in vitro. It inhibits CP55940- and Δ9-tetrahydrocannabinol (THC)-mediated inhibition of adenylyl cyclase activity and β-arrestin2 recruitment at the human CB1 receptor and [35S]-GTPγS binding in mouse cerebellum [31].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
pepcan-12 Hs Negative 8.1 – 8.3 pKB 1
pKB 8.1 – 8.3 [1]
GAT100 Hs Negative 6.4 – 7.7 pEC50 38,44
pEC50 7.7 (EC50 1.92x10-8 M) [38]
Description: Although GAT100 antagonized CP55940-induced stimulation of [35S]GTPγS binding to human CB1 CHO cell membranes, it enhanced the binding of [3H]CP55940 to these membranes. The EC50 and Emax values of GAT100 for this enhancement, with the 95% confidence limits shown in brackets, were 19.6 nM (10.4 & 36.9 nM) and 116.5% (108.3 & 124.6%), respectively. GAT100 (500 nM) was also found to enhance saturation binding of [3H]CP55940 to human CB1 HEK293 cell membranes.
pEC50 6.4 (EC50 4.098x10-7 M) [44]
Description: Measuring GAT100's inhibition of [3H]SR141716A binding, in radioligand binding assays
Org27569 Hs Positive 6.8 pEC50 57
pEC50 6.8 (EC50 1.4x10-7 M) [57]
Description: Measured as increased binding of radiolabelled orthosteric agonist CP55940
ZCZ011 Mm Positive 6.3 – 6.9 pEC50 33
pEC50 6.9 [33]
Description: Equilibrium binding experiment versus [3H]CP55940, to mouse brain membranes.
pEC50 6.3 [33]
Description: Equilibrium binding experiment versus [3HWIN55212, to mouse brain membranes.
cannabidiol Hs Negative - - 43
[43]
View species-specific allosteric modulator tables
Allosteric Modulator Comments
It is likely that ZCZ011 can also behave as a positive allosteric modulator of CB1 receptor activation when it is administered in vivo. Thus, evidence was obtained that it can act in vivo to enhance pharmacological effects both of exogenously administered anandamide and CP55940, and of endogenously released anandamide, that are most probably CB1-receptor mediated.
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
Potassium channel
Calcium channel
Other - See Comments
Comments:  Activation of MAP kinase leading to immediate early gene expression[29]
References:  4,8,17,19,24,30,46-47,52,73,77
Secondary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  22,58
Tissue Distribution
Primarily CNS and some peripheral neurones; particularly prevalent in basal ganglia, hippocampus, cerebellum, cerebral cortex. Also present in some non-neuronal cells and tissues, for example leukocytes and testis.
Species:  Human
Technique:  Radioligand binding
References:  25,29,48,53
Primarily CNS and innervation to tissues by peripheral nervous system; particularly prevalent in basal ganglia, hippocampus, cerebellum, cerebral cortex.
Species:  Rat
Technique:  Radioligand binding
References:  25,35,75
Expression Datasets

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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
Drug discrimination (also primates and pigeons)
Species:  Rat
Tissue:  In vivo
Response measured:  Drug discrimination
References:  29
Tetrad of hypothermia, antinociception, hypoactivity and catalepsy
Species:  Rat
Tissue:  In vivo
Response measured:  Rectal temperature, tail flick or hot plate response, spontaneous locomotor activity and ring immobility, all measured in the same animal.
References:  29,49,78
Nerve-smooth muscle tissue preparation
Species:  Mouse
Tissue:  Vas deferens
Response measured:  Inhibition of electrically-evoked contractions
References:  29,53
Tetrad of hypothermia, antinociception, hypoactivity and catalepsy
Species:  Mouse
Tissue:  In vivo
Response measured:  Rectal temperature, tail flick or hot plate response, spontaneous locomotor activity and ring immobility, all measured in the same animal.
References:  29,49,78
Reduction by GAT100 of β-arrestin recruitment induced by the established CB1 receptor orthosteric agonist, CP55940 (EC50 31.1 nM). The antagonistic EC50 of GAT100 was 2.09 nM.
Species:  Human
Tissue:  CB1 receptor expressing CHO cells
Response measured:  β-arrestin recruitment
References:  38
Reduction by GAT100 of inhibition of forskolin-induced stimulation the established CB1 receptor orthosteric agonist, CP55940 (EC50 7.5 nM). The antagonistic EC50 of GAT100 was 174 nM.
Species:  Human
Tissue:  CB1 receptor expressing CHO cells
Response measured:  Forskolin-induced stimulation
References:  38
Reduction by GAT100 of the Emax of the established CB1 receptor orthosteric agonist, CP55940, for its stimulation of [35S]GTPγS binding.
Species:  Human
Tissue:  CB1 receptor expressing CHO cell membranes
Response measured:  [35S]GTPγS binding
References:  38
Significant enhancement, by 100 nM ZCZ011, of the Emax value but not the potency of the endocannabinoid, anandamide, for its stimulation of [35S]GTPγS binding.
Species:  Mouse
Tissue:  Mouse brain membranes
Response measured:  [35S]GTPγS binding
References:  33
Significant enhancement of the potencies but not the Emax values of (i) the endocannabinoid, anandamide, by 10 and 100 nM ZCZ011, and (ii) the synthetic CB1 receptor agonist, CP55940 by 1 µM ZCZ011, for their activation of ERK 1/2 MAP-kinase phosphorylation.
Species:  Human
Tissue:  CHO cells stably transfected with cDNA encoding human cannabinoid CB1 receptors
Response measured:  ERK 1/2 MAP-kinase phosphorylation
References:  33
Inhibition of forskolin-induced stimulation of cyclic AMP production in human CB1 cells by ZCZ011 when administered alone, hence behaving as an apparent CB1 agonist (pEC50 5.68).
Species:  Human
Tissue:  CHO cells stably transfected with cDNA encoding human cannabinoid CB1 receptors
Response measured:  Forskolin-induced stimulation of cyclic AMP production
References:  33
Concentration-dependent enhancement by 100 nM and 1 µM ZCZ011 of the Emax value but not the potency of anandamide for its stimulation of β-arrestin recruitment.
Species:  Human
Tissue:  PathHunter® cells expressing the human CB1 receptor
Response measured:  β-arrestin recruitment
References:  33
Physiological Functions
Modulation of neurotransmitter release
Species:  Rat
Tissue:  Brain, spinal cord and some peripheral tissues
References:  29
Modulation of neurotransmitter release
Species:  Mouse
Tissue:  Brain and some peripheral tissues
References:  29
Physiological Consequences of Altering Gene Expression
CB1 knockout mice bred on a C57BL/6J background show hypoactivity, reduced locomotion and rearing, hypoalgesia, hypophagia, changed male hormone balance and increased mortality. CB1 knockout mice bred on a CD1 background show increased locomotor and exploratory activity when newly exposed to an arena but no change in nociception or mortality. Neither of these mouse lines respond to CB1 receptor agonists in CB1 assays, one notable exception being the antinociceptive response to Δ9-THC that is exhibited in the tail flick test by CB1 knockout mice with the C57/BL/6J background. CB1 knockout mice respond less than wild-type mice to the reinforcing properties of opioids.
Species:  Mouse
Tissue: 
Technique:  Induced mutation.
References:  45,79
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Cnr1tm1.2Ltz|Tg(dlx6a-cre)1Mekk Cnr1tm1.2Ltz/Cnr1tm1.2Ltz,Tg(dlx6a-cre)1Mekk/?
involves: 129P2/OlaHsd
MGI:104615  MGI:3758078  MP:0000788 abnormal cerebral cortex morphology PMID: 17525344 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0002912 abnormal excitatory postsynaptic potential PMID: 12060781 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0005449 abnormal food intake PMID: 14770190 
Cnr1tm1.2Ltz|Tg(dlx6a-cre)1Mekk Cnr1tm1.2Ltz/Cnr1tm1.2Ltz,Tg(dlx6a-cre)1Mekk/?
involves: 129P2/OlaHsd * C57BL/6NCrl
MGI:104615  MGI:3758078  MP:0002945 abnormal inhibitory postsynaptic currents PMID: 16908411 
Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1tm1.1Ltz
B6.129P2-Cnr1
MGI:104615  MP:0002063 abnormal learning/memory/conditioning PMID: 12152079 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0004948 abnormal neuronal precursor proliferation PMID: 15266010 
Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1tm1.1Ltz
B6.129P2-Cnr1
MGI:104615  MP:0002918 abnormal paired-pulse facilitation PMID: 12152079 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0002907 abnormal parturition PMID: 18833324 
Cnr1tm1Zim|Ptgs1tm1Unc Cnr1tm1Zim/Cnr1tm1Zim,Ptgs1tm1Unc/Ptgs1tm1Unc
involves: 129/Sv * 129P2/OlaHsd * C57BL/6J
MGI:104615  MGI:97797  MP:0002907 abnormal parturition PMID: 18833324 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0003461 abnormal response to novel object PMID: 9888857 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0001899 absent long term depression PMID: 12060781 
Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1tm1.1Ltz
B6.129P2-Cnr1
MGI:104615  MP:0001899 absent long term depression PMID: 12152079 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0002822 catalepsy PMID: 10318961 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0001262 decreased body weight PMID: 14770190 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0001982 decreased chemically-elicited antinociception PMID: 9888857 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0002727 decreased circulating insulin level PMID: 14770190 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0005668 decreased circulating leptin level PMID: 14770190 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0005185 decreased circulating progesterone level PMID: 18833324 
Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1tm1.1Ltz
B6.129P2-Cnr1
MGI:104615  MP:0001417 decreased exploration in new environment PMID: 12152079 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0008770 decreased survivor rate PMID: 10318961 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0010025 decreased total body fat amount PMID: 14770190 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0002757 decreased vertical activity PMID: 10318962 
Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1tm1.1Ltz
B6.129P2-Cnr1
MGI:104615  MP:0003008 enhanced long term potentiation PMID: 12152079 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0001399 hyperactivity PMID: 9888857 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0001402 hypoactivity PMID: 10318961  10318962 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0003043 hypoalgesia PMID: 10318961 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0009750 impaired behavioral response to addictive substance PMID: 9888857 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0009750 impaired behavioral response to addictive substance PMID: 10318961 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0009757 impaired behavioral response to morphine PMID: 9888857 
Cnr1tm1Dgen Cnr1tm1Dgen/Cnr1tm1Dgen
involves: 129S1/Sv * 129X1/SvJ
MGI:104615  MP:0009747 impaired behavioral response to xenobiotic PMID: 12917492 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0009712 impaired conditioned place preference behavior PMID: 9888857 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0008531 increased chemical nociceptive threshold PMID: 10318961 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0001745 increased circulating corticosterone level PMID: 18833324 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0005182 increased circulating estradiol level PMID: 18833324 
Cnr1tm1Map Cnr1tm1Map/Cnr1tm1Map
involves: 129S1/Sv * 129X1/SvJ * CD-1
MGI:104615  MP:0001415 increased exploration in new environment PMID: 9888857 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0005131 increased follicle stimulating hormone level PMID: 18833324 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0002891 increased insulin sensitivity PMID: 14770190 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0005659 increased resistance to diet-induced obesity PMID: 14770190 
Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1tm1.1Ltz
involves: 129P2/OlaHsd * C57BL/6N
MGI:104615  MP:0009766 increased sensitivity to xenobiotic induced morbidity/mortality PMID: 14526074 
Cnr1tm1.2Ltz|Tg(Camk2a-cre)2Gsc Cnr1tm1.2Ltz/Cnr1tm1.2Ltz,Tg(Camk2a-cre)2Gsc/0
involves: 129P2/OlaHsd * C57BL/6N
MGI:104615  MGI:2181425  MP:0009766 increased sensitivity to xenobiotic induced morbidity/mortality PMID: 14526074 
Cnr1tm1.2Ltz|Tg(Camk2a-cre)2Gsc Cnr1tm1.2Ltz/Cnr1tm1.2Ltz,Tg(Camk2a-cre)2Gsc/0
involves: 129P2/OlaHsd * C57BL/6N
MGI:104615  MGI:2181425  MP:0008235 increased susceptibility to neuronal excitotoxicity PMID: 14526074 
Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1tm1.1Ltz
involves: 129P2/OlaHsd * C57BL/6N
MGI:104615  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 14526074 
Cnr1+|Cnr1tm1.1Ltz Cnr1tm1.1Ltz/Cnr1+
involves: 129P2/OlaHsd * C57BL/6N
MGI:104615  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 14526074 
Cnr1tm1.2Ltz|Tg(Camk2a-cre)2Gsc Cnr1tm1.2Ltz/Cnr1tm1.2Ltz,Tg(Camk2a-cre)2Gsc/0
involves: 129P2/OlaHsd * C57BL/6N
MGI:104615  MGI:2181425  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 14526074 
Cnr1tm1.2Ltz|Tg(Camk2a-cre)2Gsc Cnr1tm1.2Ltz/Cnr1tm1.2Ltz,Tg(Camk2a-cre)2Gsc/?
involves: 129P2/OlaHsd * C57BL/6NCrl * FVB/N
MGI:104615  MGI:2181425  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 16908411 
Cnr1tm1.2Ltz Cnr1tm1.2Ltz/Cnr1tm1.2Ltz
involves: 129P2/OlaHsd * C57BL/6NCrl
MGI:104615  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 16908411 
Cnr1tm1.2Ltz|Neurod6+|Neurod6tm1(cre)Kan Cnr1tm1.2Ltz/Cnr1tm1.2Ltz,Neurod6tm1(cre)Kan/Neurod6+
involves: 129P2/OlaHsd * 129S1/Sv * 129X1/SvJ * C57BL/6NCrl
MGI:104615  MGI:106593  MP:0002906 increased susceptibility to pharmacologically induced seizures PMID: 16908411 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0001973 increased thermal nociceptive threshold PMID: 10318961 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0003718 maternal effect PMID: 18833324 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0002082 postnatal lethality PMID: 10318961 
Cnr1tm1Zim Cnr1tm1Zim/Cnr1tm1Zim
involves: 129/Sv * C57BL/6J
MGI:104615  MP:0002083 premature death PMID: 10318961 
Cnr1tm1Dgen Cnr1tm1Dgen/Cnr1tm1Dgen
involves: 129S1/Sv * 129X1/SvJ * ICR
MGI:104615  MP:0001475 reduced long term depression PMID: 18256258 
Cnr1tm1Ojm Cnr1tm1Ojm/Cnr1tm1Ojm
involves: 129P2/OlaHsd * C57BL/6
MGI:104615  MP:0001263 weight loss PMID: 14770190 
Biologically Significant Variants
Type:  Splice variant
Species:  Human
Description:  A shorter human splice variant (411aa) has been identified in the brain and other tissues by reverse-transcriptase PCR but mRNA levels were less than 10-fold the levels of the longer isoform. It is unlikely to exist in mouse or rat due to an altered splice donor site. The pharmacological characteristics of the isoforms are similar. CB1 receptor knock-out mice are now available to clarify receptor-mediated responses.
References:  29,68
General Comments
Techniques used include in situ hybridization and immunohistochemistry [12,76].
Immunopharmacology Comments
CB1 receptor is involved in controlling mast cell degranulation and maturation [72], and mediates production of MCP-1 by mast cells which results in recruitment of monocytic myeloid-derived suppressor cells with immunosuppressive outcome [34]. High levels of CB1 expression in the CNS suggest a possible role in neuroinflammation and potential as a drug target [56].
Immuno Cell Type Associations
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  Mast cells express both cannabinoid receptors, although the CB1 receptor is most abundantly expressed in the central nervous system.
References: 
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process ID:  2
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  positive regulation of acute inflammatory response to antigenic stimulus (GO:0002866) IEA
positive regulation of fever generation (GO:0031622) IEA
negative regulation of mast cell activation (GO:0033004) IEA
References: 
Immuno Process:  Immune regulaton
Immuno Process ID:  6
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  positive regulation of acute inflammatory response to antigenic stimulus (GO:0002866) IEA
positive regulation of fever generation (GO:0031622) IEA
negative regulation of mast cell activation (GO:0033004) IEA
References: 
Immuno Process:  Cellular signalling
Immuno Process ID:  11
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  negative regulation of mast cell activation (GO:0033004) IEA
References: 

References

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Mary Abood, Francis Barth, Tom I. Bonner, Guy Cabral, Pierre Casellas, Ben F. Cravatt, William A. Devane, Maurice R. Elphick, Christian C. Felder, Miles Herkenham, Allyn C. Howlett, George Kunos, Ken Mackie, Raphael Mechoulam, Roger G. Pertwee.
Cannabinoid receptors: CB1 receptor. Last modified on 16/05/2017. Accessed on 24/07/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=56.