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(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
Cannabinoid Receptor
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AEF0117
产品货号 : M37258
cas no: 1610878-71-1
AEF0117 是大麻素受体 (cannabinoid receptor) 1 (CB1-SSi) 的信号传导特异性抑制剂。 AEF0117 在大麻滥用 (CUD) 中发挥着重要作用。 -
JHU 75528
产品货号 : M37005
cas no: 947696-17-5
JHU 75528 (JHU-75528) is a novel PET tracer with inhibitory effects on CB that can be used to study the cannabinoid system in schizophrenic patients. -
CB2R/FAAH modulator-3
产品货号 : M35955
cas no: 2876918-67-9
CB2R/FAAH modulator-3 (compound 27) 是一种双重靶向调节剂,可以作为 CB2R激动剂和 FAAH 抑制剂。CB2R/FAAH modulator-3 作用于 CB2R 和 CB1R 的 Ki 值分别是 20.1 和 67.6 nM,作用于 FAAH 的IC50值为 3.4 μM。CB2R/FAAH modulator-3 可用于癌症、神经退行性疾病中发生的有害炎症级联反应以及 COVID-19 感染相关研究。 -
CB2R/FAAH?modulator-2
产品货号 : M35953
cas no: 2876918-68-0
CB2R/FAAH modulator-2 (compound 26) 是一种双重靶向调节剂,可以作为 CB2R激动剂和 FAAH 抑制剂。CB2R/FAAH modulator-2 作用于 CB2R 和 CB1R 的 Ki 值分别是 10.8 和 152.9 nM,作用于FAAH 的 IC50 值为 6.2 μM。CB2R/FAAH modulator-2 可用于癌症、神经退行性疾病中发生的有害炎症级联反应以及 COVID-19 感染相关研究。 -
GW 833972A
产品货号 : M35825
cas no: 1092502-33-4
GW 833972A 是一种选择性的 CB2 受体激动剂。GW 833972A 抑制受诱导神经去极化,并在动物模型中抑制柠檬酸引起的咳嗽。