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HTS and Rational Drug Design to Generate a Class of 5‐HT 2C ‐Selective Ligands for Possible Use in Schizophrenia.
Author(s) -
Kozikowski Alan P.,
Cho Sung Jin,
Jensen Niels H.,
Allen John A.,
Svennebring Andreas M.,
Roth Bryan L.
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000186
Subject(s) - agonist , prepulse inhibition , 5 ht2c receptor , phencyclidine , schizophrenia (object oriented programming) , pharmacology , drug , drug class , drug discovery , neuroscience , receptor , medicine , psychology , biology , psychiatry , 5 ht receptor , bioinformatics , nmda receptor , serotonin
Treating neurological conditions: Optimization of a previously identified lead 5‐HT 2C agonist (left) led to the discovery of a highly selective 5‐HT 2C agonist (right). Importantly, this compound is a 5‐HT 2B receptor antagonist. Because of its selective 5‐HT 2C receptor activity, the compound was further evaluated in the phencyclidine model of disrupted prepulse inhibition, and found to exhibit normalizing effects comparable to those shown by the 5‐HT 2C agonist vabicaserin, a drug currently in phase II clinical studies for schizophrenia.