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Effects of VA-045, a novel apovincaminic acid derivative, on isolated blood vessels: cerebroarterial selectivity.

Abstract
We investigated the effects of VA-045, an apovincaminic acid derivative, on isolated blood vessels. VA-045 (10(-7)-10(-5) M) and vinpocetine (10(-7)-10(-5) M) inhibited the 64 mM KCl-induced and 10(-6)M norepinephrine (NE)-induced contraction of rat aortic strips. VA-045 (10(-7)-10(-4) M) and vinpocetine (10(-7)-10(-4) M) inhibited the activity of cyclic AMP and cyclic GMP phosphodiesterase in porcine coronary artery. VA-045 (3 x 10(-9-3 x 10(-6) M) relaxed the 64 mM KCl-induced contraction of the canine basilar artery without affecting the peripheral arteries. These results indicate that VA-045 selectively dilates canine cerebral artery, and that it may be a useful agent for the treatment of cerebrovascular diseases such as stroke.
AuthorsN Miyata, H Yamaura, M Tanaka, M Muramatsu, K Tsuchida, S Okuyama, S Otomo
JournalLife sciences (Life Sci) Vol. 52 Issue 18 Pg. PL181-6 ( 1993) ISSN: 0024-3205 [Print] Netherlands
PMID8387130 (Publication Type: Journal Article)
Chemical References
  • Vasodilator Agents
  • Vinca Alkaloids
  • 2-(nitrooxy)ethyl apovincaminate
  • 8-Bromo Cyclic Adenosine Monophosphate
  • 8-bromocyclic GMP
  • vinpocetine
  • Potassium Chloride
  • 3',5'-Cyclic-GMP Phosphodiesterases
  • Cyclic GMP
  • Norepinephrine
Topics
  • 3',5'-Cyclic-GMP Phosphodiesterases (antagonists & inhibitors)
  • 8-Bromo Cyclic Adenosine Monophosphate (pharmacology)
  • Animals
  • Aorta (drug effects, physiology)
  • Basilar Artery (drug effects, physiology)
  • Blood Vessels (drug effects, physiology)
  • Cerebral Arteries (drug effects, physiology)
  • Coronary Vessels (drug effects, enzymology, physiology)
  • Cyclic GMP (analogs & derivatives, pharmacology)
  • Dogs
  • Female
  • In Vitro Techniques
  • Male
  • Muscle Contraction (drug effects)
  • Muscle, Smooth, Vascular (drug effects, physiology)
  • Norepinephrine (pharmacology)
  • Potassium Chloride (pharmacology)
  • Rats
  • Rats, Wistar
  • Sensitivity and Specificity
  • Vasodilator Agents (pharmacology)
  • Vinca Alkaloids (pharmacology)

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