Azetidinones as vasopressin V1a antagonists.

Azetidinones as vasopressin V1a antagonists. Research Abstract Details 

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Azetidinones as vasopressin V1a antagonists. Abstract Text:

Christophe D Guillon,Gary A Koppel,Michael J Brownstein,Michael O Chaney,Craig F Ferris,Shi-Fang Lu,Karine M Fabio,Marvin J Miller,Ned D Heindel,David C Hunden,Robin D G Cooper,Stephen W Kaldor,Jeffrey J Skelton,Bruce A Dressman,Michael P Clay,Mitchell I Steinberg,Robert F Bruns,Neal G Simon,

The azetidinone LY307174 (1) was identified as a screening lead for the vasopressin V1a receptor (IC50 45 nM at the human V1a receptor) based on molecular similarity to ketoconazole (2), a known antagonist of the luteinizing hormone releasing hormone receptor. Structure-activity relationships for the series were explored to optimize receptor affinity and pharmacokinetic properties, resulting in compounds with Ki values <1nM and brain levels after oral dosing approximately 100-fold higher than receptor affinities.

Azetidinones as vasopressin V1a antagonists. Publishing Authors By Initials

CD Guillon,GA Koppel,MJ Brownstein,MO Chaney,CF Ferris,SF Lu,KM Fabio,MJ Miller,ND Heindel,DC Hunden,RD Cooper,SW Kaldor,JJ Skelton,BA Dressman,MP Clay,MI Steinberg,RF Bruns,NG Simon,

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PUBMED ID PMID:

MEDLINE DATE:

Azetidinones as vasopressin V1a antagonists. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 2054-80

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 23

MONTH: 12

YEAR: 2006

Azetidinones as vasopressin V1a antagonists. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9413298

Azetidinones as vasopressin V1a antagonists. Keywords Mesh Terms:

KEYWORDS: Spectrometry, Mass, Fast Atom Bombardmen

MESH TERMS: antagonists & inhibitors

Chemical & Substance for Abstract: Azetidinones as vasopressin V1a antagonists. Information

Substance Name: Receptors, Vasopressin

Registry Number: 0

Grant and Affiliation Information for Azetidinones as vasopressin V1a antagonists.

AFFILIATION: Department of Chemistry, 6 East Packer Avenue, Lehigh University, Bethlehem, PA 18015, USA. chg3@lehigh.edu

Country: England

AGENCY: United States NIMH

GRANT: R44 MH063663-04

ACRONYM: MH

MEDLINETA: Bioorg Med Chem

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