Page last updated: 2024-08-07 16:10:26

Cannabinoid receptor 1

A cannabinoid receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P21554]

Synonyms

CB-R;
CB1;
CANN6

Research

Bioassay Publications (287)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (1.39)18.2507
2000's95 (33.10)29.6817
2010's158 (55.05)24.3611
2020's30 (10.45)2.80

Compounds (98)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
tacrineHomo sapiens (human)Ki1.000011
am 251Homo sapiens (human)IC500.089277
am 251Homo sapiens (human)Ki0.016778
cannabinolHomo sapiens (human)Ki0.372844
econazoleHomo sapiens (human)IC5036.270010
econazoleHomo sapiens (human)Ki28.627010
miconazoleHomo sapiens (human)IC5021.050010
miconazoleHomo sapiens (human)Ki16.614010
nimodipineHomo sapiens (human)IC501.736010
nimodipineHomo sapiens (human)Ki1.371010
palmidrolHomo sapiens (human)Ki5.000023
mestranolHomo sapiens (human)IC5028.540010
mestranolHomo sapiens (human)Ki22.532010
phenothiazineHomo sapiens (human)IC5024.857010
phenothiazineHomo sapiens (human)Ki19.624010
indopanHomo sapiens (human)Ki10.000011
dronabinolHomo sapiens (human)IC500.002811
dronabinolHomo sapiens (human)Ki0.02951818
cannabichromeneHomo sapiens (human)Ki0.714011
pravadolineHomo sapiens (human)IC500.453011
epigallocatechin gallateHomo sapiens (human)Ki33.600022
gallocatecholHomo sapiens (human)Ki35.700011
magnololHomo sapiens (human)Ki2.575022
honokiolHomo sapiens (human)Ki2.743233
(6ar-trans)-isomer of tetrahydrocannabivarin 9Homo sapiens (human)IC500.013111
(6ar-trans)-isomer of tetrahydrocannabivarin 9Homo sapiens (human)Ki0.359033
delta(9)-tetrahydrocannabinolic acidHomo sapiens (human)Ki0.024011
rimonabantHomo sapiens (human)IC500.013011
rimonabantHomo sapiens (human)Ki0.015222
sr141716Homo sapiens (human)IC500.02193131
sr141716Homo sapiens (human)Ki0.04477983
cp-55,940Homo sapiens (human)IC500.00421313
cp-55,940Homo sapiens (human)Ki0.00262527
1,1-dimethylheptyl-11-hydroxytetrahydrocannabinolHomo sapiens (human)Ki0.018822
epicatechin gallateHomo sapiens (human)Ki47.300011
4-methoxyhonokiolHomo sapiens (human)Ki0.843014
8-hydroxy-delta(9)-tetrahydrocannabinolHomo sapiens (human)Ki0.065011
delta-8-tetrahydrocannabinolHomo sapiens (human)Ki0.043867
cannabidiolHomo sapiens (human)Ki3.139844
flunarizineHomo sapiens (human)IC503.028010
flunarizineHomo sapiens (human)Ki2.391010
capsaicinHomo sapiens (human)Ki8.900034
N-(4-chlorophenethyl)-N'-(4-chlorophenyl)ureaHomo sapiens (human)IC500.162211
orlistatHomo sapiens (human)IC500.100011
orlistatHomo sapiens (human)Ki2.500011
sr 144528Homo sapiens (human)IC50271.347222
sr 144528Homo sapiens (human)Ki9.87121213
lenabasumHomo sapiens (human)Ki0.019022
jhw 015Homo sapiens (human)Ki0.800169
am 281Homo sapiens (human)Ki0.422011
am 630Homo sapiens (human)Ki3.415189
anandamideHomo sapiens (human)Ki0.18342223
homo-gamma-linolenylethanolamideHomo sapiens (human)Ki0.325722
7,10,13,16-docosatetraenylethanolamideHomo sapiens (human)Ki0.034411
glyceryl 2-arachidonateHomo sapiens (human)Ki0.605544
arachidonoyl amineHomo sapiens (human)Ki9.600011
linoleoyl ethanolamideHomo sapiens (human)Ki41.400011
n-oleoylethanolamineHomo sapiens (human)Ki3.325034
nabiloneHomo sapiens (human)Ki0.003622
arachidonyl-2-chloroethylamideHomo sapiens (human)Ki0.005311
l 759633Homo sapiens (human)Ki8.446522
ly 320135Homo sapiens (human)Ki0.141011
(3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanoneHomo sapiens (human)IC500.071077
(3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanoneHomo sapiens (human)Ki0.19076771
cannabigerolHomo sapiens (human)IC503.310011
cannabigerolHomo sapiens (human)Ki1.419033
virodhamineHomo sapiens (human)Ki0.912011
guineensineHomo sapiens (human)Ki20.000011
(2E,4E)-N-isobutyl-2,4-dodecadienamideHomo sapiens (human)Ki1.940011
noladin etherHomo sapiens (human)Ki0.022522
am 404Homo sapiens (human)Ki1.630022
jwh-133Homo sapiens (human)Ki0.55571313
CB-13Homo sapiens (human)IC500.797522
CB-13Homo sapiens (human)Ki0.035022
am-411Homo sapiens (human)Ki0.006822
hu 210Homo sapiens (human)Ki0.005166
slv 319Homo sapiens (human)IC500.018522
slv 319Homo sapiens (human)Ki0.006199
sr 147778Homo sapiens (human)Ki0.003511
jte 907Homo sapiens (human)Ki3.147022
emindole SBHomo sapiens (human)Ki7.050011
1-(2,3-dichlorobenzoyl)-5-methoxy-2-methyl-(2-(mopholin-4-yl)ethyl)-1h-indoleHomo sapiens (human)Ki2.658544
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chlorideHomo sapiens (human)Ki1.000011
amg 3Homo sapiens (human)Ki0.000334
leucettamine bHomo sapiens (human)IC5010.000011
cp 945598Homo sapiens (human)Ki0.001045
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazoleHomo sapiens (human)IC500.631011
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazoleHomo sapiens (human)Ki0.829411
am 1241Homo sapiens (human)IC500.280011
am 1241Homo sapiens (human)Ki1.7524811
km-233Homo sapiens (human)Ki0.012355
1-(2,4-dichlorophenyl)-6-methyl-N-(1-piperidinyl)-4H-indeno[1,2-c]pyrazole-3-carboxamideHomo sapiens (human)Ki0.363033
jwh 018Homo sapiens (human)Ki0.005056
n-arachidonoyl l-serineHomo sapiens (human)Ki10.000011
n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamideHomo sapiens (human)IC500.00311818
n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamideHomo sapiens (human)Ki0.000311
pf 514273Homo sapiens (human)Ki1.667456
mk-9470Homo sapiens (human)IC500.000722
1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)ureaHomo sapiens (human)IC500.29661414
a-796260Homo sapiens (human)IC500.330022
a-796260Homo sapiens (human)Ki0.755847
cannabidivarinHomo sapiens (human)Ki14.710011
4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-n-(piperidin-1-yl)-1h-pyrazole-3-carboxamideHomo sapiens (human)Ki0.011011
omdm 169Homo sapiens (human)Ki10.000011
a 803467Homo sapiens (human)IC5010.000011
a-836339Homo sapiens (human)Ki0.271022
smm-189Homo sapiens (human)Ki3.194333
n-(adamantan-1-yl)-4-oxo-1-pentyl-6-phenyl-1,4-dihydroquinoline-3-carboxamideHomo sapiens (human)Ki10.000022
nitd 609Homo sapiens (human)IC5010.000011
ur-144Homo sapiens (human)Ki0.147312
misoprostolHomo sapiens (human)IC500.523077
am6545Homo sapiens (human)Ki0.001011
n,n-diallyl-5-methoxytryptamineHomo sapiens (human)Ki10.000011
s-777469Homo sapiens (human)IC502.000011
s-777469Homo sapiens (human)Ki4.424733
jd5037Homo sapiens (human)IC500.000511
((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one)Homo sapiens (human)IC500.314011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
am 251Homo sapiens (human)EC500.065123
cannabinolHomo sapiens (human)EC500.075011
dronabinolHomo sapiens (human)EC500.045833
magnololHomo sapiens (human)EC5018.300011
honokiolHomo sapiens (human)EC5010.000011
rimonabantHomo sapiens (human)EC500.010111
rimonabantHomo sapiens (human)Kd0.002511
sr141716Homo sapiens (human)EC500.06541516
sr141716Homo sapiens (human)Kd0.0027816
cp-55,940Homo sapiens (human)EC500.01324550
cp-55,940Homo sapiens (human)Kd0.0016210
1,1-dimethylheptyl-11-hydroxytetrahydrocannabinolHomo sapiens (human)EC500.000611
3-[[4-(2,3-dimethylphenyl)-1-piperazinyl]-oxomethyl]-N,N-dimethyl-4-(1-pyrrolidinyl)benzenesulfonamideHomo sapiens (human)EC5030.000011
lenabasumHomo sapiens (human)EC500.927011
glyceryl 2-arachidonateHomo sapiens (human)EC500.023011
nabiloneHomo sapiens (human)EC500.004011
(3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanoneHomo sapiens (human)EC500.18681414
CB-13Homo sapiens (human)EC500.050433
am-411Homo sapiens (human)EC501.530011
hu 210Homo sapiens (human)EC500.020322
slv 319Homo sapiens (human)Kd0.000133
1-(2,3-dichlorobenzoyl)-5-methoxy-2-methyl-(2-(mopholin-4-yl)ethyl)-1h-indoleHomo sapiens (human)EC5016.100011
am 1241Homo sapiens (human)EC501.038011
gw 842166xHomo sapiens (human)EC5018.571477
jwh 018Homo sapiens (human)EC500.022435
n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamideHomo sapiens (human)EC500.002422
1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)ureaHomo sapiens (human)EC500.127944
a-796260Homo sapiens (human)EC500.811011
misoprostolHomo sapiens (human)EC502.014588
AKB48Homo sapiens (human)EC500.038011
sdb-001Homo sapiens (human)EC500.055334

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
cannabinolHomo sapiens (human)Log Ki0.002511
dronabinolHomo sapiens (human)Log Ki0.001611
sr141716Homo sapiens (human)Kb0.000711
sr141716Homo sapiens (human)Ke1.429477
sr141716Homo sapiens (human)Kieq0.012011
sr141716Homo sapiens (human)Log Ki0.001111
cp-55,940Homo sapiens (human)Kb0.093011
cannabidiolHomo sapiens (human)Log Ki0.003611
sr 144528Homo sapiens (human)Kieq2.820011
jhw 015Homo sapiens (human)Log Ki0.002611
anandamideHomo sapiens (human)Log Ki0.002011
(3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanoneHomo sapiens (human)Log Ki0.000311
cannabigerolHomo sapiens (human)K1.040011
cp 945598Homo sapiens (human)Ke0.005933
1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)ureaHomo sapiens (human)Kb0.054222
n-(adamantan-1-yl)-4-oxo-1-pentyl-6-phenyl-1,4-dihydroquinoline-3-carboxamideHomo sapiens (human)Kieq10.000011
misoprostolHomo sapiens (human)Kb0.217233
((5z)5-(1,3-benzodioxol-5-yl)methylene-2-phenylamino-3,5-dihydro-4h-imidazol-4-one)Homo sapiens (human)Kb2.200011

Enables

This protein enables 4 target(s):

TargetCategoryDefinition
cannabinoid receptor activitymolecular functionCombining with a cannabinoid to initiate a change in cell activity. Cannabinoids are a class of diverse chemical compounds that include the endocannabinoids and the phytocannabinoids. [GOC:dph, IUPHAR_GPCR:1279, Wikipedia:Cannabinoid]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]
G protein-coupled receptor activitymolecular functionCombining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR]

Located In

This protein is located in 8 target(s):

TargetCategoryDefinition
mitochondrial outer membranecellular componentThe outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
actin cytoskeletoncellular componentThe part of the cytoskeleton (the internal framework of a cell) composed of actin and associated proteins. Includes actin cytoskeleton-associated complexes. [GOC:jl, ISBN:0395825172, ISBN:0815316194]
growth conecellular componentThe migrating motile tip of a growing neuron projection, where actin accumulates, and the actin cytoskeleton is the most dynamic. [GOC:aruk, GOC:bc, ISBN:0815316194, PMID:10082468]
presynaptic membranecellular componentA specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194]
membrane raftcellular componentAny of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567]
glutamatergic synapsecellular componentA synapse that uses glutamate as a neurotransmitter. [GOC:dos]
GABA-ergic synapsecellular componentA synapse that uses GABA as a neurotransmitter. These synapses are typically inhibitory. [GOC:dos]

Active In

This protein is active in 2 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]

Involved In

This protein is involved in 34 target(s):

TargetCategoryDefinition
positive regulation of acute inflammatory response to antigenic stimulusbiological processAny process that activates or increases the frequency, rate, or extent of an acute inflammatory response to an antigenic stimulus. [GOC:add]
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerbiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194]
adenylate cyclase-modulating G protein-coupled receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194]
spermatogenesisbiological processThe developmental process by which male germ line stem cells self renew or give rise to successive cell types resulting in the development of a spermatozoa. [GOC:jid, ISBN:9780878933846, PMID:28073824, PMID:30990821]
axonal fasciculationbiological processThe collection of axons into a bundle of rods, known as a fascicle. [GOC:dgh]
response to nutrientbiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nutrient stimulus. [GOC:go_curators]
memorybiological processThe activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089]
positive regulation of neuron projection developmentbiological processAny process that increases the rate, frequency or extent of neuron projection development. Neuron projection development is the process whose specific outcome is the progression of a neuron projection over time, from its formation to the mature structure. A neuron projection is any process extending from a neural cell, such as axons or dendrites (collectively called neurites). [GOC:dph, GOC:tb]
negative regulation of serotonin secretionbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of serotonin. [GOC:ef]
positive regulation of fever generationbiological processAny process that activates or increases the frequency, rate, or extent of fever generation. [GOC:add]
negative regulation of fatty acid beta-oxidationbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of fatty acid beta-oxidation. [GOC:mah]
regulation of synaptic transmission, GABAergicbiological processAny process that modulates the frequency, rate or extent of GABAergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter gamma-aminobutyric acid (GABA). [GOC:mah]
response to lipopolysaccharidebiological processAny process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464]
negative regulation of mast cell activationbiological processAny process that stops, prevents, or reduces the frequency, rate, or extent of mast cell activation. [GOC:mah]
negative regulation of dopamine secretionbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of the regulated release of dopamine. [GOC:sl]
response to nicotinebiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nicotine stimulus. [GOC:bf, GOC:ef, ISBN:0198506732, ISBN:0582227089]
cannabinoid signaling pathwaybiological processA G protein-coupled receptor signaling pathway initiated by a cannabinoid binding to its receptor on the cell surface, and ending with the regulation of a downstream cellular process, e.g. transcription. Cannabinoids are a class of diverse chemical compounds that include the endocannabinoids and the phytocannabinoids. [GOC:bf, GOC:jc, GOC:signaling, Wikipedia:Cannabinoid]
response to cocainebiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl]
glucose homeostasisbiological processAny process involved in the maintenance of an internal steady state of glucose within an organism or cell. [GOC:go_curators]
positive regulation of apoptotic processbiological processAny process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
response to ethanolbiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ethanol stimulus. [GOC:go_curators]
negative regulation of action potentialbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of action potential creation, propagation or termination. This typically occurs via modulation of the activity or expression of voltage-gated ion channels. [GOC:go_curators]
negative regulation of blood pressurebiological processAny process in which the force of blood traveling through the circulatory system is decreased. [GOC:go_curators, GOC:mtg_cardio]
positive regulation of blood pressurebiological processAny process in which the force of blood traveling through the circulatory system is increased. [GOC:go_curators, GOC:mtg_cardio]
regulation of insulin secretionbiological processAny process that modulates the frequency, rate or extent of the regulated release of insulin. [GOC:ai]
regulation of synaptic transmission, glutamatergicbiological processAny process that modulates the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai]
maternal process involved in female pregnancybiological processA reproductive process occurring in the mother that allows an embryo or fetus to develop within it. [GOC:dph]
regulation of feeding behaviorbiological processAny process that modulates the rate, frequency or extent of the behavior associated with the intake of food. [GOC:BHF, GOC:dph, GOC:tb]
regulation of penile erectionbiological processAny process that modulates the rate, frequency or extent of penile erection. Penile erection is the hardening, enlarging and rising of the penis which often occurs in the sexually aroused male and enables sexual intercourse. Achieved by increased inflow of blood into the vessels of erectile tissue, and decreased outflow. [GOC:add, GOC:dph, GOC:tb]
retrograde trans-synaptic signaling by endocannabinoidbiological processCell-cell signaling from postsynapse to presynapse, across the synaptic cleft, mediated by an endocannabinoid ligand. [GOC:dos]
regulation of presynaptic cytosolic calcium ion concentrationbiological processAny process that regulates the concentration of calcium in the presynaptic cytosol. [GOC:dos]
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionbiological processCell-cell signaling between presynapse and postsynapse, via the release and reception of endocannabinoid ligands, that modulates the synaptic transmission properties of the synapse. [GOC:dos, PMID:21531987]
adenylate cyclase-activating G protein-coupled receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194]
regulation of metabolic processbiological processAny process that modulates the frequency, rate or extent of the chemical reactions and pathways within a cell or an organism. [GOC:go_curators]