-transparent.png){kind=logo}
A new series of 4-alkyl-1,4-dihydropyridines (1,4-DHP) were synthesized and evaluated for their ability to inhibit washed rabbit platelet aggregation induced by PAF-acether (1-O-hexadecyl/octadecyl-2-O-acetyl-sn-glycero-3-phosphorylcholine) and to reverse PAF-induced hypotension in anesthetized rats. Additionally, compounds were evaluated for their ability to inhibit the binding of radiolabeled PAF to its receptor on rabbit platelets. Among these compounds, 6I and 6L were the most potent and specific antagonists. At concentrations up to 100 microM, neither compound 6I nor compound 6L caused platelet aggregation nor did they inhibit platelet aggregation induced by collagen or adenosine diphosphate. Compound 6L did not show in vitro calcium channel blocker activity measured on vascular smooth muscle preparations of rabbit aorta and on [3H]nitrendipine binding assays. The compound did not show any cardiovascular effects in anesthetized rat at iv doses up to 1000 micrograms/kg, and the Ki value was 568.62 nmol. These results indicate that compound 6L is a potent and specific PAF antagonist with 1,4-dihydropyridine structure but devoid of a significant cardiovascular activity related to calcium-antagonist properties.
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
August 1988,
Journal of medicinal chemistry,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
December 2019,
The Journal of organic chemistry,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
January 1992,
Advances in experimental medicine and biology,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
October 1988,
Biochemistry,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
July 1993,
Journal of photochemistry and photobiology. B, Biology,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
August 1992,
Journal of medicinal chemistry,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
January 1987,
Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
October 2021,
Organic & biomolecular chemistry,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
January 1987,
Advances in prostaglandin, thromboxane, and leukotriene research,
C E Sunkel, and
M F de Casa-Juana, and
L Santos, and
M M Gómez, and
M Villarroya, and
M A González-Morales, and
J G Priego, and
M P Ortega
November 2020,
Chemical communications (Cambridge, England),
