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DJ-7141, a new alpha-2 agonist with only a mild hypotensive action.

Abstract
The pharmacological profile of a newly synthesized imidazole derivative, DJ-7141, was examined with special reference to alpha-2 adrenoceptors. In the rat vas deferens and dog mesenteric artery, DJ-7141 at concentrations over 10(-9) M selectively acted on the presynaptic alpha-2 adrenoceptors on the sympathetic nerve terminals and inhibited the contractions induced by electrical transmural stimulation. The potency of DJ-7141 was almost the same as those of clonidine and guanabenz. DJ-7141 also acted on the postsynaptic alpha-2 adrenoceptors to contract the dog saphenous vein. However, no alpha-1 agonist and antagonist actions were found at concentrations showing presynaptic alpha-2 agonist activity. In contrast to DJ-7141, clonidine produced an apparent contraction in the dog mesenteric artery, and the response was inhibited by prazosin. In urethane-anesthetized rats, clonidine at doses ranging from 0.003 mg/kg to 0.03 mg/kg produced a marked and prolonged hypotension, while DJ-7141 at such doses failed to produce a reduction of blood pressure. From these results, it is suggested that, in contrast to clonidine and other alpha-2 agonists, DJ-7141 is a unique alpha-2 agonist which shows high affinity to peripheral alpha-2 adrenoceptors but only a mild hypotensive activity.
AuthorsI Muramatsu, M Oshita, S Hashimoto, S Kigoshi
JournalJapanese journal of pharmacology (Jpn J Pharmacol) Vol. 41 Issue 1 Pg. 61-8 (May 1986) ISSN: 0021-5198 [Print] Japan
PMID2874252 (Publication Type: Journal Article)
Chemical References
  • Adrenergic alpha-Agonists
  • Antihypertensive Agents
  • Imidazoles
  • Receptors, Adrenergic, alpha
  • DJ 7141
  • Clonidine
  • Norepinephrine
Topics
  • Adrenergic alpha-Agonists (pharmacology)
  • Animals
  • Antihypertensive Agents
  • Blood Pressure (drug effects)
  • Clonidine (pharmacology)
  • Dogs
  • Female
  • Imidazoles (pharmacology)
  • Male
  • Mesenteric Arteries (drug effects, physiology)
  • Muscle Contraction (drug effects)
  • Muscle, Smooth (drug effects, physiology)
  • Muscle, Smooth, Vascular (drug effects, physiology)
  • Norepinephrine (pharmacology)
  • Rats
  • Rats, Inbred Strains
  • Receptors, Adrenergic, alpha (drug effects, physiology)
  • Saphenous Vein (drug effects)
  • Vas Deferens (drug effects, physiology)
  • Vasoconstriction (drug effects)

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