Stereoselective inhibition of thromboxane-induced coronary vasoconstriction by 1,4-dihydropyridine calcium channel antagonists

The biological activity of the (+)‐S‐ and (−)‐R‐enantiomers of niguldipine, of the (−)‐S‐ and (+)‐R‐enantiomers of felodipine and nitrendipine, and of rac‐nisoldipine and rac‐nimodipine was investigated in vitro and in vivo. Inhibition of coronary vasoconstriction due to the thromboxane A2 (TxA2)‐mi...

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Veröffentlicht in:	Chirality (New York, N.Y.) N.Y.), 1990, Vol.2 (4), p.233-240
Hauptverfasser:	Eltze, Manfrid, Sanders, Karl H., Boss, Hildegard, Boer, Rainer, Ulrich, Wolf-Rüdiger, Flockerzi, Dieter
Format:	Artikel
Sprache:	eng
Schlagworte:	1,4‐dihydropypyridine enantiomers 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid 4-dihydropypyridine enantiomers 550201 - Biochemistry- Tracer Techniques ANIMALS ARTERIES AZINES BASIC BIOLOGICAL SCIENCES Binding, Competitive BIOCHEMICAL REACTION KINETICS BLOOD PRESSURE BLOOD VESSELS BODY calcium channel binding Calcium Channel Blockers - pharmacology Calcium Channels - drug effects Calcium Channels - metabolism CARDIOVASCULAR DISEASES CARDIOVASCULAR SYSTEM CELL CONSTITUENTS Cell Membrane - metabolism CELL MEMBRANES CORONARIES coronary vasoconstriction Dihydropyridines - metabolism Dihydropyridines - pharmacology DISEASES GUINEA PIGS HEART Heart - drug effects Heart - physiology HETEROCYCLIC COMPOUNDS HYDROGEN COMPOUNDS HYPERTENSION IN VITRO In Vitro Techniques IN VIVO INHIBITION ISOTOPE APPLICATIONS Isradipine KINETICS Male MAMMALS MEMBRANE PROTEINS MEMBRANES MUSCLES Muscles - metabolism ORGANIC COMPOUNDS ORGANIC NITROGEN COMPOUNDS ORGANS PORINS Prostaglandin Endoperoxides, Synthetic - pharmacology PROSTAGLANDINS PROTEINS PYRIDINES Pyridines - metabolism Radioligand Assay RATS Rats, Inbred SHR REACTION KINETICS RECEPTORS RODENTS Stereoisomerism stereoselectivity Structure-Activity Relationship STRUCTURE-ACTIVITY RELATIONSHIPS SYMPTOMS thromboxane A2 (TxA2) Thromboxane A2 - physiology TRACER TECHNIQUES Tritium TRITIUM COMPOUNDS VASCULAR DISEASES VASOCONSTRICTION Vasoconstriction - drug effects VERTEBRATES
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Zusammenfassung:	The biological activity of the (+)‐S‐ and (−)‐R‐enantiomers of niguldipine, of the (−)‐S‐ and (+)‐R‐enantiomers of felodipine and nitrendipine, and of rac‐nisoldipine and rac‐nimodipine was investigated in vitro and in vivo. Inhibition of coronary vasoconstriction due to the thromboxane A2 (TxA2)‐mimetic U‐46619 in guinea pig Langendorff hearts, displacement of (+)‐[3H]isradipine from calcium channel binding sites of guinea pig skeletal muscle T‐tubule membranes, and blood pressure reduction in spontaneously hypertensive rats were determined. The enantiomers were obtained by stereoselective synthesis. Cross‐contamination was
ISSN:	0899-0042 1520-636X
DOI:	10.1002/chir.530020408