Possible mechanism underlying the potent vasoconstrictor actions of cyclopiazonic acid on dog cerebral arteries. 1998

M Asano, and M Kuwako, and Y Nomura, and Y Suzuki, and M Shibuya
Department of Pharmacology, Nagoya City University Medical School, Nagoya, Japan.

A sustained Ca2+ influx via L-type Ca2+ channels has been shown in the resting state of dog cerebral arteries. Sarcoplasmic reticulum is now recognized to serve as a buffer barrier to Ca2+ entry in vascular smooth muscle cells. To clarify whether sarcoplasmic reticulum of the cerebral arteries can buffer the sustained Ca2+ influx, effects of cyclopiazonic acid (CPA), an inhibitor of sarcoplasmic reticulum Ca2+-ATPase, were determined in endothelium-denuded strips of the cerebral (basilar, posterior communicating, middle cerebral), mesenteric and coronary arteries of the dog. The addition of CPA (0.1-10 microM) during the resting state of the strips caused a concentration-dependent contraction in the three cerebral arteries. The CPA-induced contraction was extremely small in the mesenteric or coronary artery. The CPA-induced contractions in the cerebral arteries were inhibited concentration-dependently by nifedipine (1-100 nM). Nifedipine itself induced relaxation from the resting state of cerebral arteries, suggesting a maintenance of basal tone. The CPA-induced potent contraction seen in the cerebral arteries could be mimicked in the mesenteric artery by elevating the extracellular K+ concentration (14.9 mM) or adding Bay K 8644 [methyl-1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoromethylphenyl)-pyr idine-5-carboxylate] (100 nM) to produce an increase in Ca2+ influx via L-type Ca2+ channels. We conclude that, in the resting state of dog cerebral arteries, (1) the greater part of the sustained Ca2+ influx is buffered by Ca2+ uptake into the sarcoplasmic reticulum, (2) therefore, the inhibition of sarcoplasmic reticulum Ca2+-ATPase by CPA causes a potent contraction, and (3) the maintenance of basal tone suggests that some Ca2+ that entered via L-type Ca2+ channels always reaches the myofilaments in the resting state.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D007537 Isometric Contraction Muscular contractions characterized by increase in tension without change in length. Contraction, Isometric,Contractions, Isometric,Isometric Contractions
D008297 Male Males
D008638 Mesenteric Arteries Arteries which arise from the abdominal aorta and distribute to most of the intestines. Arteries, Mesenteric,Artery, Mesenteric,Mesenteric Artery
D009543 Nifedipine A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. Adalat,BAY-a-1040,Bay-1040,Cordipin,Cordipine,Corinfar,Fenigidin,Korinfar,Nifangin,Nifedipine Monohydrochloride,Nifedipine-GTIS,Procardia,Procardia XL,Vascard,BAY a 1040,BAYa1040,Bay 1040,Bay1040,Monohydrochloride, Nifedipine,Nifedipine GTIS
D011188 Potassium An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
D002120 Calcium Channel Agonists Agents that increase calcium influx into calcium channels of excitable tissues. This causes vasoconstriction in VASCULAR SMOOTH MUSCLE and/or CARDIAC MUSCLE cells as well as stimulation of insulin release from pancreatic islets. Therefore, tissue-selective calcium agonists have the potential to combat cardiac failure and endocrinological disorders. They have been used primarily in experimental studies in cell and tissue culture. Calcium Channel Activators,Calcium Channel Agonists, Exogenous,Calcium Channel Agonist,Exogenous Calcium Channel Agonists,Activators, Calcium Channel,Agonist, Calcium Channel,Agonists, Calcium Channel,Channel Activators, Calcium,Channel Agonist, Calcium,Channel Agonists, Calcium
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
D002536 Cerebral Arteries The arterial blood vessels supplying the CEREBRUM. Arteries, Cerebral,Artery, Cerebral,Cerebral Artery
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog

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