BioCentury
ARTICLE | Distillery Therapeutics

Neurology

May 1, 2018 11:28 PM UTC

Rat studies identified a carboxamide-based 5-HT2C receptor positive allosteric modulator (PAM) that could help treat cocaine addiction. Chemical synthesis and in vitro activity testing of analogs of the 5-HT2C receptor PAM lincomycin yielded a carboxamide-based compound that increased 5-hydroxytryptamine (5-HT)-evoked intracellular calcium release in CHO cells expressing human 5-HTC2 receptor compared with 5-HT alone. In a rat model of cocaine addiction, the compound decreased relapse vulnerability compared with vehicle. Next steps include undisclosed preclinical and IND-enabling studies of the compound and other analogs in its series...

BCIQ Target Profiles

Serotonin (5-HT2C) receptor