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Can I read The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands on EtoBox?
The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands by Manish Tandon; Mary-Margaret O'Donnell; Alex Porte; David Vensel; Donglai Yang; Rocio Palma; Alan Beresford; Mark A. Ashwell is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands about?
New arylpiperazines related to buspirone, gepirone and NAN-190 were designed and screened in silico for their 5-HT 1A affinity and potential sites of metabolism by human cytochrome P450 (CYP3A4). Modifications to these structures were assessed in silico for their influence on both 5HT 1A affinity and metabolism. Selected new molecules were synthesized and purified in a parallel chemistry approach to determine structure activity relationships (SARs). The resulting molecules were assessed in vitro for their 5HT 1A affinity and half-life in a heterologously expressed human CYP3A4 assay. Molecular features responsible for 5-HT 1A affinity and CYP3A4 stability are described.
Who reads The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Manish Tandon; Mary-Margaret O'Donnell; Alex Porte; David Vensel; Donglai Yang; Rocio Palma; Alan Beresford; Mark A. Ashwell
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2004
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)