2β-Propanoyl-3β-(2-naphthyl)-tropane explained
2β-Propanoyl-3β-(2-naphthyl)-tropane or WF-23 (Wake Forest-23, named after the university where it was first created) is a cocaine analogue. It is several hundred times more potent than cocaine at being a serotonin-norepinephrine-dopamine reuptake inhibitor.
As can be seen on PubMed, these acyl substituted phenyltropanes are highly potent MAT inhibitors and also have a very long half-life, spanning perhaps at least a few days;[1] [2] as the half-life of the dopamine transporter in rats was found to be 2–3 days under normal conditions (with agonists, antagonists, and transporter inhibitors altering the half-life),[3] it may be that WF-23 largely or mostly binds to its transporters until they are degraded.
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Notes and References
- Bennett BA, Wichems CH, Hollingsworth CK, Davies HM, Thornley C, Sexton T, Childers SR . Novel 2-substituted cocaine analogs: uptake and ligand binding studies at dopamine, serotonin and norepinephrine transport sites in the rat brain . The Journal of Pharmacology and Experimental Therapeutics . 272 . 3 . 1176–1186 . March 1995 . 7891330 .
- Daunais JB, Hart SL, Smith HR, Letchworth SR, Davies HM, Sexton T, Bennett BA, Childers SR, Porrino LJ . 6 . Long-acting blockade of biogenic amine transporters in rat brain by administration of the potent novel tropane 2beta-propanoyl-3beta-(2-Naphthyl)-tropane . The Journal of Pharmacology and Experimental Therapeutics . 285 . 3 . 1246–1254 . June 1998 . 9618429 .
- Kimmel HL, Carroll FI, Kuhar MJ . Withdrawal from repeated cocaine alters dopamine transporter protein turnover in the rat striatum . The Journal of Pharmacology and Experimental Therapeutics . 304 . 1 . 15–21 . January 2003 . 12490570 . 10.1124/jpet.102.038018 . 27253009 .