Howlett Allyn C, Abood Mary E
Center for Research on Substance Use and Addiction, Wake Forest University Health Sciences, Winston-Salem, NC, United States.
Center for Substance Abuse Research, Lewis Katz School of Medicine at Temple University, Philadelphia, PA, United States.
Adv Pharmacol. 2017;80:169-206. doi: 10.1016/bs.apha.2017.03.007. Epub 2017 Jun 12.
The CB and CB cannabinoid receptors (CBR, CBR) are members of the G protein-coupled receptor (GPCR) family that were identified over 20 years ago. CBRs and CBRs mediate the effects of Δ-tetrahydrocannabinol (Δ-THC), the principal psychoactive constituent of marijuana, and subsequently identified endogenous cannabinoids (endocannabinoids) anandamide and 2-arachidonoyl glycerol. CBRs and CBRs have both similarities and differences in their pharmacology. Both receptors recognize multiple classes of agonist and antagonist compounds and produce an array of distinct downstream effects. Natural polymorphisms and alternative splice variants may also contribute to their pharmacological diversity. As our knowledge of the distinct differences grows, we may be able to target select receptor conformations and their corresponding pharmacological responses. This chapter will discuss their pharmacological characterization, distribution, phylogeny, and signaling pathways. In addition, the effects of extended agonist exposure and how that affects signaling and expression patterns of the receptors are considered.
CB和CB大麻素受体（CBR、CBR）是20多年前被鉴定出的G蛋白偶联受体（GPCR）家族成员。CBR和CBR介导Δ-四氢大麻酚（Δ-THC，大麻的主要精神活性成分）的作用，随后鉴定出内源性大麻素（内源性大麻素）花生四烯乙醇胺和2-花生四烯酰甘油。CBR和CBR在药理学方面既有相似之处，也有不同之处。两种受体都识别多种类型的激动剂和拮抗剂化合物，并产生一系列不同的下游效应。天然多态性和可变剪接变体也可能导致它们的药理学多样性。随着我们对这些明显差异的了解不断增加，我们或许能够针对特定的受体构象及其相应的药理反应。本章将讨论它们的药理学特征、分布、系统发育和信号通路。此外，还将考虑延长激动剂暴露的影响以及这如何影响受体的信号传导和表达模式。
