Chemistry:RB-64
From HandWiki
Short description: Chemical compound
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| Formula | C24H27NO8S |
| Molar mass | 489.54 g·mol−1 |
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RB-64 is a semi-synthetic derivative of salvinorin A. It is an irreversible agonist, with a reactive thiocyanate group that forms a bond to the κ-opioid receptor (KOR), resulting in very high potency.[1] It is functionally selective, activating G proteins more potently than β-arrestin-2.[2] RB-64 has a bias factor of up to 96 and is analgesic with fewer of the side-effects associated with unbiased KOR agonists.[3] The analgesia is long-lasting. Compared with unbiased agonists, RB-64 evokes considerably less receptor internalization.
See also
References
- ↑ "Structure-based design, synthesis, and biochemical and pharmacological characterization of novel salvinorin A analogues as active state probes of the kappa-opioid receptor". Biochemistry 48 (29): 6898–6908. July 2009. doi:10.1021/bi900605n. PMID 19555087.
- ↑ "Identification of novel functionally selective κ-opioid receptor scaffolds". Molecular Pharmacology 85 (1): 83–90. January 2014. doi:10.1124/mol.113.089649. PMID 24113749.
- ↑ "The G protein-biased κ-opioid receptor agonist RB-64 is analgesic with a unique spectrum of activities in vivo". The Journal of Pharmacology and Experimental Therapeutics 352 (1): 98–109. January 2015. doi:10.1124/jpet.114.216820. PMID 25320048.
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