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Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene.[5] And discovered, by determination and characterization in 1988,[6] and cloned in 1990 for the first time.[7][8][9] The human CB1 receptor is expressed in the peripheral nervous system and central nervous system.[5] It is activated by endogenous cannabinoids[10] called endocannabinoids, a group of retrograde neurotransmitters that include lipids, such as anandamide and 2-arachidonoylglycerol; plant phytocannabinoids, such as docosatetraenoylethanolamide found in wild daga, the compound tetrahydrocannabinol which is an active constituent of the psychoactive drug cannabis; and synthetic analogs of tetrahydrocannabinol. CB1 is antagonized by the phytocannabinoid tetrahydrocannabivarin at low doses and at higher doses, it activate the CB1 receptor as an agonist, but with less potency than tetrahydrocannabinol.[11][12][13]
The primary endogenous agonist of the human CB1 receptor is anandamide.[5]
- ^ a b c GRCh38: Ensembl release 89: ENSG00000118432 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000044288 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ a b c Abood M, Barth F, Bonner TI, Cabral G, Casellas P, Cravatt BF, et al. (22 August 2018). "CB1 Receptor". IUPHAR/BPS Guide to Pharmacology. International Union of Basic and Clinical Pharmacology. Retrieved 9 November 2018.
- ^ Devane WA, Dysarz FA, Johnson MR, Melvin LS, Howlett AC (1 November 1988). "Determination and characterization of a cannabinoid receptor in rat brain". Molecular Pharmacology. 34 (5): 605–613. ISSN 0026-895X. PMID 2848184.
- ^ Matsuda LA, Lolait SJ, Brownstein MJ, Young AC, Bonner TI (1990). "Structure of a cannabinoid receptor and functional expression of the cloned cDNA". Nature. 346 (6284): 561–564. doi:10.1038/346561a0. ISSN 1476-4687.
- ^ Matsuda LA, Lolait SJ, Brownstein M, Young AC, Bonner TI (1990). "Structure of a Cannabinoid Receptor and Functional Expression of the Cloned Cdna". ResearchGate.
- ^ Howlett AC, Abood ME (2017). "CB1 & CB2 Receptor Pharmacology". PubMed.
- ^ Busquets Garcia A, Soria-Gomez E, Bellocchio L, Marsicano G (24 May 2016). "Cannabinoid receptor type-1: breaking the dogmas". F1000Research. 5: 990. doi:10.12688/f1000research.8245.1. PMC 4879932. PMID 27239293.
- ^ Thomas A, Stevenson LA, Wease KN, Price MR, Baillie G, Ross RA, et al. (December 2005). "Evidence that the plant cannabinoid Delta9-tetrahydrocannabivarin is a cannabinoid CB1 and CB2 receptor antagonist". British Journal of Pharmacology. 146 (7): 917–926. doi:10.1038/sj.bjp.0706414. PMC 1751228. PMID 16205722.
- ^ Pertwee RG, Thomas A, Stevenson LA, Ross RA, Varvel SA, Lichtman AH, et al. (March 2007). "The psychoactive plant cannabinoid, Delta9-tetrahydrocannabinol, is antagonized by Delta8- and Delta9-tetrahydrocannabivarin in mice in vivo". British Journal of Pharmacology. 150 (5): 586–594. doi:10.1038/sj.bjp.0707124. PMC 2189766. PMID 17245367.
- ^ Pertwee RG (2008). "The diverse CB 1 and CB 2 receptor pharmacology of three plant cannabinoids: Δ 9 ‐tetrahydrocannabinol, cannabidiol and Δ 9 ‐tetrahydrocannabivarin". British Journal of Pharmacology. 153 (2): 199–215. doi:10.1038/sj.bjp.0707442. ISSN 0007-1188. PMC 2219532. PMID 17828291.