SYNTHESIS AND NK-2 ANTAGONIST EFFECT OF -PYRAZOLO[3,4-D]-THIAZOLO[3,2-A]4H-PYRIMIDIN-4-ONE

Authors
GUCCIONE S MODICA M LONGMORE J SHAW D BARRETTA GU SANTAGATI A SANTAGATI M RUSSO F
Citation
S. Guccione et al., SYNTHESIS AND NK-2 ANTAGONIST EFFECT OF -PYRAZOLO[3,4-D]-THIAZOLO[3,2-A]4H-PYRIMIDIN-4-ONE, Bioorganic & medicinal chemistry letters, 6(1), 1996, pp. 59-64
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
1
Year of publication
1996
Pages
59 - 64
Database
ISI
SICI code
0960-894X(1996)6:1<59:SANAEO>2.0.ZU;2-N
Abstract
l-pyrazolo[3,4-d]thiazolo[3,2-a]4H-pyrimidin-4-one caused parallel dis placement of the dose-response -curve to the NK-2 receptor agonist in the guinea pig trachea suggesting it acts as a competitive antagonist. It is not active in the NK-I and NK-3 receptor binding assays. A Ca+ channel blocking action at the voltage-operated channels (L-type) was observed.