Cannabinoid Receptor
Cannabinoids have typically been assumed to originate from the plant Cannabis, however, broadly speaking cannabinoids are the group of chemical structures that mainly act in the body through cannabinoid receptors (CB); CB1 (Central receptor) and CB2 (Peripheral receptor) CB1 and CB2 receptors belong to the large family of G-protein-coupled receptors (GPCRs) that mediate almost all actions of exogenous and endogenous cannabinoids. These GPCRs consist of seven transmembrane domains, three extracellular loops and three intracellular loops, an extracellular N-terminal tail and an intracellular C-terminal tail that join to form a transmembrane domain. CB1 receptors are rich in the central nervous system (CNS), especially in the cortex, hippocampus, and basal ganglia.
A large portion of CB1 receptors is following reduction o expressed on cholecystokinin-expressing GABAergic interneurons in cortical areas. Low levels of CB1 receptors are present glutamatergic or serotoninergic neurons. CB1 receptors also exist at low levels in non-neuronal cells of the brain such as astrocytes. the activated CB1 receptors by endogenous or exogenous ligands contribute to inhibiting adenylate cyclase (AC) activity with following the reduction of intracellular levels of cyclic adenosine monophosphate (cAMP) production.CB1 receptors play a crucial role in controlling cell destiny and function particularly neuronal electrical activity. CB2 receptors were presumably through the DA-dependent mechanism to participate in the modulation of cocaine's rewarding and locomotor-stimulating effects. CB2 receptors may participate in neuroinflammation which gradually develops into one of the inducements of neurodegeneration.
References
1.Han QW,et al. Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jan 10;96:109745.
2.Das S,et al. Adv Exp Med Biol. 2019;1162:51-61.
A large portion of CB1 receptors is following reduction o expressed on cholecystokinin-expressing GABAergic interneurons in cortical areas. Low levels of CB1 receptors are present glutamatergic or serotoninergic neurons. CB1 receptors also exist at low levels in non-neuronal cells of the brain such as astrocytes. the activated CB1 receptors by endogenous or exogenous ligands contribute to inhibiting adenylate cyclase (AC) activity with following the reduction of intracellular levels of cyclic adenosine monophosphate (cAMP) production.CB1 receptors play a crucial role in controlling cell destiny and function particularly neuronal electrical activity. CB2 receptors were presumably through the DA-dependent mechanism to participate in the modulation of cocaine's rewarding and locomotor-stimulating effects. CB2 receptors may participate in neuroinflammation which gradually develops into one of the inducements of neurodegeneration.
References
1.Han QW,et al. Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jan 10;96:109745.
2.Das S,et al. Adv Exp Med Biol. 2019;1162:51-61.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(471)
Bombesin Receptor(11)
Bradykinin Receptor(18)
Calcium Channel(137)
cAMP(9)
Cannabinoid Receptor(69)
CaSR(17)
CGRP Receptor(14)
Chemokine Receptor(104)
Cholecystokinin Receptor(17)
CRF Receptor(13)
Dopamine Receptor(145)
Endothelin Receptor(20)
FFAR(5)
Galanin Receptor(1)
GHSR(16)
Glucagon Receptor(36)
GPCR19(7)
GPR119(3)
Hedgehog (Hh)(27)
Histamine Receptor(110)
Imidazoline Receptor(1)
Leukotriene Receptor(9)
LHR(1)
LPA Receptor(12)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(6)
Melanocortin Receptor(22)
Melatonin Receptor(5)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(34)
Neuropeptide Y Receptor(36)
Neurotensin Receptor(8)
Orexin Receptor(14)
Other Targets(3)
OXTR(2)
P2Y Receptor(8)
PAR(24)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(60)
PTH Receptor(1)
S1P Receptor(22)
SGLT(22)
Somatostatin Receptor(11)
Urotensin Receptor(4)
Vasopressin Receptor(16)
Cannabinoid Receptor
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RVD-Hpα
catalog no : M30820
cas no: 1193362-76-3
N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki = 50 nM). -
Hemopressin (rat)
catalog no : M30668
cas no: 568588-77-2
Bioactive endogenous peptide substrate for endopeptidase 24.15 (ep24.15), neurolysin (ep24.16) and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively. Potent hypotensive in vivo. Also acts as a selective CB1 receptor inverse agonist. Displays antinociceptive activity and induces hypophagia in vivo. -
Hemopressin (human, mouse)
catalog no : M30667
cas no: 1314035-51-2
Bioactive endogenous peptide substrate for endopeptidase 24.15 (ep24.15), neurolysin (ep24.16) and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively. Potent hypotensive in vivo. Also acts as a selective CB1 receptor inverse agonist. Displays antinociceptive activity in vivo. -
Tetrahydrocannabivarin
catalog no : M29348
cas no: 31262-37-0
Tetrahydrocannabivarin is a neutral cannabis receptor subtype (CB1) receptor antagonist, it can increases neural responding to rewarding and aversive stimuli, this effect profile suggests therapeutic activity in obesity, perhaps with a lowered risk of depressive side effects. Tetrahydrocannabivarin exhibits anticonvulsant effects in a piriform cortical brain slice model of epileptiform activity. -
COR659
catalog no : M28071
cas no: 544450-68-2
COR659 is a 2-acylaminothiophene derivative able to suppress alcohol and chocolate self-administration in rats, likely via positive allosteric modulation of the GABAB receptor and antagonism/inverse agonism at the cannabinoid CB1 receptor.