-transparent.png){kind=logo}
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity. 2002
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
Drug Discovery, Johnson and Johnson Pharmaceutical Research and Development, Spring House, PA 19477-0776, USA.
The synthesis and biological testing of a novel series of nonpeptide vasopressin receptor antagonists, containing a bridged bicyclic nucleus, are reported. Variation of substituents (R(1)-R(3)) in general formula 3, and the configuration of the stereocenter, resulted in potent V(2)-selective (e.g., 5) and balanced dual V(1a)/V(2) (e.g., 10) compounds. Data from receptor binding, cell-based functional, and in vivo assays are presented [corrected]
Related Publications
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
August 2008,
European journal of pharmacology,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
November 2001,
Circulation,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
December 1986,
The Journal of pharmacology and experimental therapeutics,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
January 2002,
Bioorganic & medicinal chemistry letters,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
June 2002,
European journal of pharmacology,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
August 2000,
Bioorganic & medicinal chemistry letters,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
June 2000,
The Journal of pharmacology and experimental therapeutics,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
August 2002,
European journal of pharmacology,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
March 2017,
Bioorganic & medicinal chemistry letters,
Alexey B Dyatkin, and
William J Hoekstra, and
Dennis J Hlasta, and
Patricia Andrade-Gordon, and
Lawrence de Garavilla, and
Keith T Demarest, and
Joseph W Gunnet, and
William Hageman, and
Richard Look, and
Bruce E Maryanoff
April 2002,
British journal of pharmacology,
