A 5-HT1A and 5-HT1B receptor agonist
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RU-24969 is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT1B.1 It binds to 5-HT1A and 5-HT1B receptors (IC50s = 9.5 and 6.6 nM, respectively) and is selective for these receptors over 5-HT2 receptors in cell-free assays (IC50 = 5,120 nM). RU-24969 inhibits tritium efflux induced by the 5-HT antagonist methiothepin in tritium-preloaded rat frontal cortex slices (pA2 = 6.27). In vivo, RU-24969 (3 mg/kg) potentiates cocaine-induced increases in nucleus accumbens dopamine levels, as well as the reinforcing effects of cocaine self-administration, in rats.2
1.Middlemiss, D.N.The putative 5-HT1 receptor agonist, RU 24969, inhibits the efflux of 5-hydroxytryptamine from rat frontal cortex slices by stimulation of the 5-HT autoreceptorJ. Pharm. Pharmacol.37(6)434-437(1985) 2.Parsons, L.H., Koob, G.F., and Weiss, F.RU 24969, a 5-HT1B/1A receptor agonist, potentiates cocaine-induced increases in nucleus accumbens dopamineSynapse32(2)132-135(1999)
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