Synthesis and NK-2 antagonist effect of 1,6-diphenyl-pyrazolo [3,4-d]-thiazolo[3,2-a]4H-pyrimidin-4-one
Salvatore Guccione
1
,
MARIA ASSUNTA MODICA
1
,
Jeanette Longmore
2
,
David A. Shaw
2
,
Gloria Uccello Barretta
3
,
Andrea Santagati
1
,
M. G. Santagati
1
,
Filippo Russo
1
2
Merck, Sharp and Dohme Research Laboratories (MSDRL), Neuroscience Research Centre, Terlings Park, Harlow Essex CM20 2QR, U.K.
|
Publication type: Journal Article
Publication date: 1996-01-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
1,6-Diphenyl-pyrazolo[3,4-d]thiazolo[3,2-a]4H-pyrimidin-4-one caused parallel displacement 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-1 and NK-3 receptor binding assays. A Ca ++ channel blocking action at the voltage-operated channels (L-type) was observed. Graphic
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GOST
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Guccione S. et al. Synthesis and NK-2 antagonist effect of 1,6-diphenyl-pyrazolo [3,4-d]-thiazolo[3,2-a]4H-pyrimidin-4-one // Bioorganic and Medicinal Chemistry Letters. 1996. Vol. 6. No. 1. pp. 59-64.
GOST all authors (up to 50)
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Guccione S., MODICA M. A., Longmore J., Shaw D. A., Uccello Barretta G., Santagati A., Santagati M. G., Russo F. Synthesis and NK-2 antagonist effect of 1,6-diphenyl-pyrazolo [3,4-d]-thiazolo[3,2-a]4H-pyrimidin-4-one // Bioorganic and Medicinal Chemistry Letters. 1996. Vol. 6. No. 1. pp. 59-64.
Cite this
RIS
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TY - JOUR
DO - 10.1016/0960-894X(95)00558-B
UR - https://doi.org/10.1016/0960-894X(95)00558-B
TI - Synthesis and NK-2 antagonist effect of 1,6-diphenyl-pyrazolo [3,4-d]-thiazolo[3,2-a]4H-pyrimidin-4-one
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Guccione, Salvatore
AU - MODICA, MARIA ASSUNTA
AU - Longmore, Jeanette
AU - Shaw, David A.
AU - Uccello Barretta, Gloria
AU - Santagati, Andrea
AU - Santagati, M. G.
AU - Russo, Filippo
PY - 1996
DA - 1996/01/01
PB - Elsevier
SP - 59-64
IS - 1
VL - 6
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (up to 50 authors)
Copy
@article{1996_Guccione,
author = {Salvatore Guccione and MARIA ASSUNTA MODICA and Jeanette Longmore and David A. Shaw and Gloria Uccello Barretta and Andrea Santagati and M. G. Santagati and Filippo Russo},
title = {Synthesis and NK-2 antagonist effect of 1,6-diphenyl-pyrazolo [3,4-d]-thiazolo[3,2-a]4H-pyrimidin-4-one},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {1996},
volume = {6},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/0960-894X(95)00558-B},
number = {1},
pages = {59--64},
doi = {10.1016/0960-894X(95)00558-B}
}
Cite this
MLA
Copy
Guccione, Salvatore, et al. “Synthesis and NK-2 antagonist effect of 1,6-diphenyl-pyrazolo [3,4-d]-thiazolo[3,2-a]4H-pyrimidin-4-one.” Bioorganic and Medicinal Chemistry Letters, vol. 6, no. 1, Jan. 1996, pp. 59-64. https://doi.org/10.1016/0960-894X(95)00558-B.