Page last updated: 2024-08-05 15:33:48

cannabinoid receptor agonist

An agonist that binds to and activates cannabinoid receptors.

ChEBI ID: 67072

Members (5)

MemberDefinitionClass
am 694A member of the class of indoles that is 1H-indole which is substituted at position 1 by a 5-fluoropentyl group and a position 3 by an o-fluorobenzoyl group. It is a selective agonist for the CB1 cannabinoid receptor; Ki values for the CB1 and CB2 receptors are 0.08 and 1.44 nM, respectively.1-(5-fluoropentyl)-3-(2-iodobenzoyl)indole
arachidonoyl amineA primary fatty amide resulting from the formal condensation of the carboxy group of arachidonic acid with ammonia.arachidonoyl amine
cannabigerolA member of the class of resorcinols that is resorcinol which is substituted by a (2E)-3,7-dimethylocta-2,6-dien-1-yl group at position 2 and by a pentyl group at position 5. It is a natural product found in Cannabis sativa and Helichrysum species.cannabigerol
dronabinolA diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.Delta(9)-tetrahydrocannabinol
n-arachidonoyl l-serineAn N-acyl-amino acid resulting from the formal condensation of the carboxy group of arachidonic acid with the amino group of L-serine. It is an endocannabinoid-like lipid isolated from bovine brains.N-arachidonoyl-L-serine

Research

Studies (7,896)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902,254 (28.55)18.7374
1990's842 (10.66)18.2507
2000's1,437 (18.20)29.6817
2010's2,041 (25.85)24.3611
2020's1,322 (16.74)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials788 (9.34%)5.53%
Reviews836 (9.91%)6.00%
Case Studies202 (2.40%)4.05%
Observational47 (0.56%)0.25%
Other6,561 (77.79%)84.16%

Protein Targets (49)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AR proteinHomo sapiens (human)Potency23.288022
aryl hydrocarbon receptorHomo sapiens (human)Potency8.690622
Ataxin-2Homo sapiens (human)Potency33.491511
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency33.491511
Cellular tumor antigen p53Homo sapiens (human)Potency28.600822
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency23.710111
estrogen nuclear receptor alphaHomo sapiens (human)Potency17.964433
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency24.786633
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency30.106511
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.481311
pregnane X nuclear receptorHomo sapiens (human)Potency7.943311
TDP1 proteinHomo sapiens (human)Potency23.872322
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency14.566822

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cannabinoid receptor 1Homo sapiens (human)IC501.656422
Cannabinoid receptor 1Rattus norvegicus (Norway rat)IC500.218011
Cannabinoid receptor 1Homo sapiens (human)Ki1.06032323
Cannabinoid receptor 1Mus musculus (house mouse)Ki0.040522
Cannabinoid receptor 1Rattus norvegicus (Norway rat)Ki1.50771314
Cannabinoid receptor 2Rattus norvegicus (Norway rat)IC500.218011
Cannabinoid receptor 2Mus musculus (house mouse)Ki0.030334
Cannabinoid receptor 2Rattus norvegicus (Norway rat)Ki0.046011
Cannabinoid receptor 2 Homo sapiens (human)IC501.734822
Cannabinoid receptor 2 Homo sapiens (human)Ki0.58362727
Diacylglycerol lipase-alphaHomo sapiens (human)IC50100.000011
Fatty acid-binding protein, liverMus musculus (house mouse)Ki1.000011
Fatty-acid amide hydrolase 1Homo sapiens (human)IC5043.600011
G-protein coupled receptor 55Homo sapiens (human)IC5014.200011
Inhibin alpha chainHomo sapiens (human)IC505.200011
L-lactate dehydrogenase A chainHomo sapiens (human)Ki14.000011
Lysophosphatidylserine lipase ABHD12Homo sapiens (human)IC5011.600011
Monoacylglycerol lipase ABHD6Homo sapiens (human)IC5048.200011
Monoglyceride lipaseHomo sapiens (human)IC50100.000011
N-acylethanolamine-hydrolyzing acid amidaseHomo sapiens (human)IC50100.000011
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)IC5013.000011
Transient receptor potential cation channel subfamily A member 1Rattus norvegicus (Norway rat)IC5013.000011
Transient receptor potential cation channel subfamily M member 8Homo sapiens (human)IC500.160011
Transient receptor potential cation channel subfamily M member 8Rattus norvegicus (Norway rat)IC500.160011
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)IC502.600022
Transient receptor potential cation channel subfamily V member 2Homo sapiens (human)IC501.500011
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)IC501.500011
Transient receptor potential cation channel subfamily V member 3Homo sapiens (human)IC5066.000011
Transient receptor potential cation channel subfamily V member 4Homo sapiens (human)IC501.300011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Cannabinoid receptor 1Homo sapiens (human)EC500.045833
Cannabinoid receptor 1Rattus norvegicus (Norway rat)EC500.073823
Cannabinoid receptor 2Mus musculus (house mouse)EC500.007311
Cannabinoid receptor 2 Homo sapiens (human)EC500.008633
D(3) dopamine receptorHomo sapiens (human)EC500.010211
G-protein coupled receptor 55Homo sapiens (human)EC5010.000011
Glutamate receptor 1Rattus norvegicus (Norway rat)EC500.199511
Glutamate receptor 2Rattus norvegicus (Norway rat)EC500.199511
Glutamate receptor 3Rattus norvegicus (Norway rat)EC500.199511
Glutamate receptor 4Rattus norvegicus (Norway rat)EC500.199511
Glycine receptor subunit alpha-1Homo sapiens (human)EC501.300011
N-arachidonyl glycine receptorHomo sapiens (human)EC504.610011
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC5018.933333
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC5015.700011
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC500.700011
Transient receptor potential cation channel subfamily A member 1Rattus norvegicus (Norway rat)EC501.443323
Transient receptor potential cation channel subfamily V member 1Homo sapiens (human)EC501.300022
Transient receptor potential cation channel subfamily V member 2Homo sapiens (human)EC501.700011
Transient receptor potential cation channel subfamily V member 2Rattus norvegicus (Norway rat)EC501.700011
Transient receptor potential cation channel subfamily V member 3Homo sapiens (human)EC501.000011
Transient receptor potential cation channel subfamily V member 4Homo sapiens (human)EC505.100011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Alpha-2A adrenergic receptorHomo sapiens (human)EC50.002011
Cannabinoid receptor 1Homo sapiens (human)K1.040011
Cannabinoid receptor 1Mus musculus (house mouse)K0.380011
Cannabinoid receptor 1Homo sapiens (human)Log Ki0.001611
Cannabinoid receptor 2 Homo sapiens (human)Log Ki0.001611
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)Km2.340011
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)Activity10.000011