Pharmacological properties of 2-[(5-chloro-2-methoxyphenyl)azo]-1H-imidazole (M6434).
Pharmacological properties of 2-[(5-chloro-2-methoxyphenyl)azo]-1H-imidazole (M6434) were investigated in vivo and in vitro experiments. M6434 showed a dose-dependent pressor effect in conscious rats at oral doses ranging from 1 to 5 mg/kg. The pressor effect of M6434 was 10 times as potent as those of phenylephrine and methoxamine. M6434 also showed a dose-dependent pressor effect in anesthetized dogs at i.v. doses ranging from 3 to 30 micrograms/kg. The effect of M6434 returned to control level 30 to 45 min after i.v. injection. M6434 caused a contraction of isolated guinea-pig aortic spiral strip at concentrations ranging from 10(-8) to 10(-4) mol/l. pD2 value of M6434 was larger than those of the other sympathomimetics, yet the maximal response of M6434 was 83.4% of the maximal response of noradrenaline. Pretreatment with phentolamine caused a parallel shift of the concentration-response curve of M6434 to the right. However, this effect of M6434 on an isolated aorta was not diminished even in reserpinized guinea-pigs. Therefore, the pressor effect of M6434 may be due to the direct adrenergic alpha-stimulation. M6434 is expected to be effective for the oral treatment of hypotensive disorders.
D000273:Adipose Tissue / Q000166:cytology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D004285:Dogs; D004562:Electrocardiography; D005260:Female; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D007093:Imidazoles / Q000494:pharmacology*; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D051381:Rats; D012039:Regional Blood Flow / Q000187:drug effects; D012119:Respiration / Q000187:drug effects
D007093:Imidazoles; C032482:2-((5-chloro-2-methoxyphenyl)azo)-1H-imidazole