Calcium channel agonist and antagonist effects of the stereoisomers of the dihydropyridine 202-791 - PubMed (original) (raw)
Calcium channel agonist and antagonist effects of the stereoisomers of the dihydropyridine 202-791
S Kongsamut et al. Biochem Biophys Res Commun. 1985.
Abstract
The effects of the pure stereoisomers of the novel dihydropyridine 202-791 on voltage sensitive calcium channels in nerve and cardiac muscle were examined. The (-)-isomer blocked depolarization-induced uptake of 45Ca2+ into NG108-15 neuroblastoma X glioma cells, blocked the depolarization-induced release of [3H]-norepinephrine from PC12 cells and reduced the Vmax of the slow response action potential recorded from guinea pig papillary muscle. In contrast, the (+)-isomer enhanced these same processes. In papillary muscle, greater enhancement of the slow responses was observed at lower stimulation frequencies. Thus, the (-) and (+) stereoisomers of 202-791 can be shown to be calcium channel antagonist and agonist respectively.
Similar articles
- The effect of dihydropyridine calcium agonists and antagonists on neuronal voltage sensitive calcium channels.
Creba JA, Karobath M. Creba JA, et al. Biochem Biophys Res Commun. 1986 Feb 13;134(3):1038-47. doi: 10.1016/0006-291x(86)90356-6. Biochem Biophys Res Commun. 1986. PMID: 2418832 - Interaction of steroidal alkaloid toxins with calcium channels in neuronal cell lines.
Kongsamut S, Freedman SB, Simon BE, Miller RJ. Kongsamut S, et al. Life Sci. 1985 Apr 15;36(15):1493-501. doi: 10.1016/0024-3205(85)90058-x. Life Sci. 1985. PMID: 2580208 - Calcium channel activation: a different type of drug action.
Freedman SB, Miller RJ. Freedman SB, et al. Proc Natl Acad Sci U S A. 1984 Sep;81(17):5580-3. doi: 10.1073/pnas.81.17.5580. Proc Natl Acad Sci U S A. 1984. PMID: 6206501 Free PMC article. - Antiarrhythmic agents: the modulated receptor mechanism of action of sodium and calcium channel-blocking drugs.
Hondeghem LM, Katzung BG. Hondeghem LM, et al. Annu Rev Pharmacol Toxicol. 1984;24:387-423. doi: 10.1146/annurev.pa.24.040184.002131. Annu Rev Pharmacol Toxicol. 1984. PMID: 6203481 Review. No abstract available. - Differential sensitivity of calcium channels to dihydropyridines. The modulated receptor hypothesis.
Chin JH. Chin JH. Biochem Pharmacol. 1986 Dec 1;35(23):4115-20. doi: 10.1016/0006-2952(86)90684-2. Biochem Pharmacol. 1986. PMID: 2431688 Review. No abstract available.
Cited by
- Mechanisms of dihydropyridine agonists and antagonists in view of cryo-EM structures of calcium and sodium channels.
Tikhonov DB, Zhorov BS. Tikhonov DB, et al. J Gen Physiol. 2023 Nov 6;155(11):e202313418. doi: 10.1085/jgp.202313418. Epub 2023 Sep 20. J Gen Physiol. 2023. PMID: 37728574 Free PMC article. - Biphasic inotropic effects of a Ca2+ channel activator CGP28392 in rat myocardium: possible relation to intracellular Ca2+ release.
Kobrinsky E, Saxon M. Kobrinsky E, et al. Br J Pharmacol. 1987 Nov;92(3):499-504. doi: 10.1111/j.1476-5381.1987.tb11349.x. Br J Pharmacol. 1987. PMID: 3427265 Free PMC article. - The dihydropyridine derivative 202-791: interpretation of the effects of the racemate considering inverse agonistic enantiomers.
Damarowsky M, Lüllmann H, Ravens U. Damarowsky M, et al. Br J Pharmacol. 1988 Dec;95(4):1125-32. doi: 10.1111/j.1476-5381.1988.tb11747.x. Br J Pharmacol. 1988. PMID: 3219483 Free PMC article. - Calcium channels: molecular pharmacology, structure and regulation.
Hosey MM, Lazdunski M. Hosey MM, et al. J Membr Biol. 1988 Sep;104(2):81-105. doi: 10.1007/BF01870922. J Membr Biol. 1988. PMID: 2903935 Review. No abstract available. - Modulation of the delayed rectifier potassium current in frog cardiomyocytes by beta-adrenergic agonists and magnesium.
Duchatelle-Gourdon I, Hartzell HC, Lagrutta AA. Duchatelle-Gourdon I, et al. J Physiol. 1989 Aug;415:251-74. doi: 10.1113/jphysiol.1989.sp017721. J Physiol. 1989. PMID: 2561787 Free PMC article.