Central and peripheral cardiovascular effects of the enantiomers of the calcium antagonist PN 200-110. 1988

V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
Laboratoire de Pharmacologie Cardiovasculaire, INSERM U 228, Paris, France.

The negative inotropic effects and the central and peripheral hypotensive effects of (+) and (-) PN 200-110 were investigated in cultured chick heart cells and in spontaneously hypertensive rats, respectively. There was a large difference in negative inotropic potency between the two enantiomers in cultured chick embryo ventricular cells: the (+) enantiomer was 140 fold more potent (IC50 = 1.1 +/- 0.2 nM) than the (-) enantiomer (IC50 = 160 +/- 20 nM). (+) PN 200-110 was 10 fold more potent than (-) PN 200-110 in lowering blood pressure after intravenous injection and only three fold more potent after intra-cerebroventricular injection (i.c.v.) into pentobarbital-anaesthetized spontaneously hypertensive rats. I.c.v. administered (+) PN 200-110 (1 microgram/kg) partially antagonized the hypertensive response to i.c.v. administered BAY K 8644 (30 micrograms/kg), a calcium channel agonist, while the same dose of the (-) enantiomer did not change the i.c.v. BAY-induced increase in blood pressure. These results suggest that the dihydropyridine calcium channel antagonist, PN 200-110, may act centrally and stereoselectively at the level of the dihydropyridine receptor sites involved in the control of blood pressure in spontaneously hypertensive rats.

UI MeSH Term Description Entries
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D007276 Injections, Intraventricular Injections into the cerebral ventricles. Intraventricular Injections,Injection, Intraventricular,Intraventricular Injection
D008297 Male Males
D010069 Oxadiazoles Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms. Oxadiazole
D011918 Rats, Inbred SHR A strain of Rattus norvegicus with elevated blood pressure used as a model for studying hypertension and stroke. Rats, Spontaneously Hypertensive,Rats, SHR,Inbred SHR Rat,Inbred SHR Rats,Rat, Inbred SHR,Rat, SHR,Rat, Spontaneously Hypertensive,SHR Rat,SHR Rat, Inbred,SHR Rats,SHR Rats, Inbred,Spontaneously Hypertensive Rat,Spontaneously Hypertensive Rats
D012039 Regional Blood Flow The flow of BLOOD through or around an organ or region of the body. Blood Flow, Regional,Blood Flows, Regional,Flow, Regional Blood,Flows, Regional Blood,Regional Blood Flows
D001794 Blood Pressure PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS. Systolic Pressure,Diastolic Pressure,Pulse Pressure,Pressure, Blood,Pressure, Diastolic,Pressure, Pulse,Pressure, Systolic,Pressures, Systolic
D002121 Calcium Channel Blockers A class of drugs that act by selective inhibition of calcium influx through cellular membranes. Calcium Antagonists, Exogenous,Calcium Blockaders, Exogenous,Calcium Channel Antagonist,Calcium Channel Blocker,Calcium Channel Blocking Drug,Calcium Inhibitors, Exogenous,Channel Blockers, Calcium,Exogenous Calcium Blockader,Exogenous Calcium Inhibitor,Calcium Channel Antagonists,Calcium Channel Blocking Drugs,Exogenous Calcium Antagonists,Exogenous Calcium Blockaders,Exogenous Calcium Inhibitors,Antagonist, Calcium Channel,Antagonists, Calcium Channel,Antagonists, Exogenous Calcium,Blockader, Exogenous Calcium,Blocker, Calcium Channel,Blockers, Calcium Channel,Calcium Blockader, Exogenous,Calcium Inhibitor, Exogenous,Channel Antagonist, Calcium,Channel Blocker, Calcium,Inhibitor, Exogenous Calcium
D002642 Chick Embryo The developmental entity of a fertilized chicken egg (ZYGOTE). The developmental process begins about 24 h before the egg is laid at the BLASTODISC, a small whitish spot on the surface of the EGG YOLK. After 21 days of incubation, the embryo is fully developed before hatching. Embryo, Chick,Chick Embryos,Embryos, Chick
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response

Related Publications

V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
March 1991, Brain research bulletin,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
January 1991, Acta radiologica. Supplementum,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
August 1987, Journal of cardiovascular pharmacology,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
December 1986, European journal of pharmacology,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
January 1984, Journal of cardiovascular pharmacology,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
January 1987, The American journal of cardiology,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
September 1985, British journal of pharmacology,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
January 1987, The American journal of cardiology,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
January 1987, European journal of clinical pharmacology,
V Briand, and S Laurent, and D Tsoucaris-Kupfer, and M Legrand, and A M Brisac, and H Schmitt
January 1987, The American journal of cardiology,
Copied contents to your clipboard!