Structure-Function Relationships of 1,4-Dihydropyridines: Ligand and Receptor Perspectives
Are there specific 1,4-dihydropyridine sites?
How many classes of such sites exist?
What are the structural demands at these sites?
- 4.How may activator and antagonist ligands be differentiated?
What is the relationship of binding sites to the Ca2+ channel and channel permeation processes?
What relationship does this site(s) have to the actions of other structural categories of Ca2+ channel ligands?
What is the basis for any tissue selectivity of the 1,4-dihydropyridines?
Are there endogenous ligands for the Ca2+ channel?
KeywordsPyridine Verapamil Nifedipine Ileal Phen
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- Bean B (1984) Nitrendipine block of cardiac calcium channels: high affinity binding to the inactivated state. Proc Nat Acad Sci USA.Google Scholar
- Bolger GT, Gengo P, Klockowski R, Luchowski E, Siegel H, Janis RA, Triggle AM, Triggle DJ (1983) Characterization of binding of the Ca2+-channel antagonist [3H]nitrendipine, to guinea pig ileal smooth muscle. J Pharmacol Exptl Therap 225:291–310.Google Scholar
- Hess P, Lansman JB, Tsien RW (1984) Different modes of Ca channel gating behaviour favored by dihydropyridine Ca agonists and antagonists. Nature.Google Scholar
- Janis RA, Sarmiento JG, Maurer SC, Bolger GT, Triggle DJ (1984) Characteristics of the binding of [3H]nitrendipine to rabbit ventricular membranes: modification by other Ca++ channel antagonists and by the Ca2+ channel agonist BAY K 8644. J Pharmacol Exptl Therap 231:8–15.Google Scholar
- Langs DA, Triggle DJ (1984) Chemical structure and pharmacologic activities of Ca2+ channel antagonists. In: Proc 9th International Congress of Pharmacology, London, 1984.Google Scholar
- Mannhold R, Rodenkirchen R, Bayer R (1982) Qualitative and quantitative structure-activity relationships of specific Ca antagonists. Prog Pharmacol 5:25–52.Google Scholar
- Rosenberger LB, Triggle DJ (1978) Calcium, calcium translocation and specific calcium antagonists. In: Weiss GB (ed) Calcium and drug action. Plenum Press, New York, pp 3–31.Google Scholar
- Seidel W, Meyer H, Born L, Kazda S, Dompert W (1984) Rigid calcium antagonists of the nifedipine type: geometrical requirements for the dihydropyridine receptor. Abs 14 Div Med Chem American Chemical Society, 187th National Meeting, St. Louis, MO, April 8-13.Google Scholar