Novel,highly potent,selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics |
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| Authors: | Lee Taekyu Robichaud Albert J Boyle Kristopher E Lu Yimin Robertson David W Miller Keith J Fitzgerald Larry W McElroy John F Largent Brian L |
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| Affiliation: | Discovery Chemistry, Bristol-Myers Squibb Company, Wilmington, DE 19880, USA. taekyu.lee@bms.com |
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| Abstract: | The discovery of N-substituted-pyridoindolines and their binding affinities at the 5-HT(2A), 5-HT(2C) and D(2) receptors, and in vivo efficacy as 5-HT(2A) antagonists is described. The structure-activity relationship of a series of core tetracyclic derivatives with varying butyrophenone sidechains is also discussed. This study has led to the identification of potent, orally bioavailable 5-HT(2A)/D(2) receptor dual antagonists as potential atypical antipsychotics. |
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