Unknown

Dataset Information

0

CB1 and CB2 Receptor Pharmacology.

ABSTRACT: The CB1 and CB2 cannabinoid receptors (CB1R, CB2R) are members of the G protein-coupled receptor (GPCR) family that were identified over 20 years ago. CB1Rs and CB2Rs mediate the effects of ?9-tetrahydrocannabinol (?9-THC), the principal psychoactive constituent of marijuana, and subsequently identified endogenous cannabinoids (endocannabinoids) anandamide and 2-arachidonoyl glycerol. CB1Rs and CB2Rs 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.

SUBMITTER: Howlett AC 

PROVIDER: S-EPMC5812699 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

CB<sub>1</sub> and CB<sub>2</sub> Receptor Pharmacology.

Howlett Allyn C AC   Abood Mary E ME  

Advances in pharmacology (San Diego, Calif.) 20170612

The CB<sub>1</sub> and CB<sub>2</sub> cannabinoid receptors (CB<sub>1</sub>R, CB<sub>2</sub>R) are members of the G protein-coupled receptor (GPCR) family that were identified over 20 years ago. CB<sub>1</sub>Rs and CB<sub>2</sub>Rs mediate the effects of Δ<sup>9</sup>-tetrahydrocannabinol (Δ<sup>9</sup>-THC), the principal psychoactive constituent of marijuana, and subsequently identified endogenous cannabinoids (endocannabinoids) anandamide and 2-arachidonoyl glycerol. CB<sub>1</sub>Rs and CB<  ...[more]

Similar Datasets

Unknown Cannabinoid CB<sub>1</sub> and CB<sub>2</sub> Receptor Signaling and Bias.
| S-EPMC5436336 | biostudies-literature
Unknown The peripheral CB<sub>1</sub> receptor antagonist JD5037 attenuates liver fibrosis via a CB<sub>1</sub> receptor/β-arrestin1/Akt pathway.
| S-EPMC7236068 | biostudies-literature
Unknown Cannabichromene is a cannabinoid CB<sub>2</sub> receptor agonist.
| S-EPMC6932936 | biostudies-literature
Unknown In vivo evaluation of the CB<sub>1</sub> allosteric modulator LDK1258 reveals CB<sub>1</sub>-receptor independent behavioral effects.
| S-EPMC8791624 | biostudies-literature
Unknown Cholesterol as a modulator of cannabinoid receptor CB<sub>2</sub> signaling.
| S-EPMC7881127 | biostudies-literature
Unknown Different receptor mechanisms underlying phytocannabinoid- versus synthetic cannabinoid-induced tetrad effects: Opposite roles of CB<sub>1</sub> /CB<sub>2</sub> versus GPR55 receptors.
| S-EPMC7070166 | biostudies-literature
Unknown Discovery of Homobivalent Bitopic Ligands of the Cannabinoid CB<sub>2</sub> Receptor*.
| S-EPMC7756656 | biostudies-literature
Unknown Opposite effects of cannabinoid CB<sub>1</sub> and CB<sub>2</sub> receptors on antipsychotic clozapine-induced cardiotoxicity.
| S-EPMC6433645 | biostudies-literature
Unknown Cannabinoid CB<sub>2</sub> receptor ligand profiling reveals biased signalling and off-target activity.
| S-EPMC5216056 | biostudies-literature
Unknown Optimization of the Heterologous Expression of the Cannabinoid Type-1 (CB<sub>1</sub>) Receptor.
| S-EPMC8564136 | biostudies-literature