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Beschreibung

A selective 5-HT1B/1D receptor antagonist. Selectivity was found to be similar for B (pki = 9.2-9.8 )and D (pki = 8.6-9.1) receptor types. GR 127935 works well in vivo and was shown to block (+)-MDMA-induced hyperactivity in rats. It alters release of serotonin in the brain, as well as reducing drug-seeking behaviour in cocaine addicted rats. In transformed rat C5 glioma cells, this inhibitor blocked 5HT with an IC50 = 97 pM.