Cannabinoid Receptor
Cannabinoid receptors, located throughout the body, are part of the Endocannabinoid system which is involved in a variety of physiological processes including appetite, pain-sensation, mood, and memory.
Cannabinoid receptors are of a class of cell membrane receptors under the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids, produced by the mammillary body; plant cannabinoids; and synthetic cannabinoids. There are currently two known subtypes of cannabinoid receptors, termed CB1 and CB2.
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BML-190是一种选择性的cannabinoid CB2 receptor逆向激动剂,Ki为435 nM,比作用于CB1受体选择性高50倍。
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AM1241是一种选择性的cannabinoid CB2 receptor激动剂,Ki为3.4 nM,比作用于CB1受体选择性高82倍。
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GW842166X是一种有效的,高选择性cannabinoid receptor CB2受体激动剂,EC50为63 nM,对CB1受体没有显著的活性。
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AM251是CB1受体高效拮抗剂,IC50值为8nM,对CB2受体无作用,也是GPR55激动剂。
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Otenabant盐酸盐是CB1受体高亲和性拮抗剂,Ki为0.7 nM。
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