Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics

Taekyu Lee; Albert J. Robichaud; Kristopher E. Boyle; Yimin Lu; David W. Robertson; Keith J. Miller; Larry W. Fitzgerald; John F. McElroy; Brian L. Largent

doi:10.1016/S0960-894X(02)01028-4

Novel, highly potent, selective 5-HT_2A/D₂ receptor antagonists as potential atypical antipsychotics

Taekyu Lee
, Albert J. Robichaud
, Kristopher E. Boyle
, Yimin Lu
, David W. Robertson
, Keith J. Miller
, Larry W. Fitzgerald
, John F. McElroy
, Brian L. Largent

Research output: Contribution to journal › Article › peer-review

Abstract

The discovery of N-substituted-pyridoindolines and their binding affinities at the 5-HT_2A, 5-HT_2C and D₂ 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/D₂ receptor dual antagonists as potential atypical antipsychotics.

Original language	English
Pages (from-to)	767-770
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	13
Issue number	4
DOIs	https://doi.org/10.1016/S0960-894X(02)01028-4
State	Published - Feb 2003

ASJC Scopus Subject Areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(02)01028-4

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Cite this

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title = "Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics",

abstract = "The discovery of N-substituted-pyridoindolines and their binding affinities at the 5-HT2A, 5-HT2C and D2 receptors, and in vivo efficacy as 5-HT2A 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-HT2A/D2 receptor dual antagonists as potential atypical antipsychotics.",

author = "Taekyu Lee and Robichaud, \{Albert J.\} and Boyle, \{Kristopher E.\} and Yimin Lu and Robertson, \{David W.\} and Miller, \{Keith J.\} and Fitzgerald, \{Larry W.\} and McElroy, \{John F.\} and Largent, \{Brian L.\}",

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AU - Robichaud, Albert J.

AU - Boyle, Kristopher E.

AU - Lu, Yimin

AU - Robertson, David W.

AU - Miller, Keith J.

AU - Fitzgerald, Larry W.

AU - McElroy, John F.

AU - Largent, Brian L.

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