General pharmacological action of 4- (o-benzylphenoxy) -N-methylbutylamine hydrochloride (MCI-2016, bifemelane hydrochloride) . Influence on respiratory and cardiovascular systems, renal function, autonomic nervous system, isolated smooth muscle and digestive organs

Narimatsu, A.; Nakao, K.; Ikoma, H.; Egawa, M.; Kitada, Y.; Yamazaki, S.; Umezu, K.; Miyake, M.; Nishimura, E.; Hashimoto, N.

Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 87(2): 223-251

1986


ISSN/ISBN: 0015-5691
PMID: 3754532
Accession: 005508855

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Abstract
MCI-2016 at 3 mg/kg, i.v., caused slight changes in systemic blood pressure (SBP), heart rate (HR), respiratory rate (RR) and ECG but at 10 mg/kg i.v., it caused a significant increased in RR, decrease in SBP, increase or decrease in HR and a moderate change in ECG. Biphasic changes in SBP, HR and blood flow were sometimes observed after high doses. MCI-2016 also decreased SBP at 30 mg/kg, i.p., in SHR. MCI-2016 (50 mg/kg, p.o./day) showed little influence on SBP, HR and ECG in conscious beagle dogs. In isolated hearts, MCI-2016 decreased HR and contractility at the concentrations above 10-5 g/ml, and 30 .mu.g, i.a. MCI-2016 prolonged the AVCT at 10 mg/kg, i.v. MCI-2016 (i.v. or i.a.) moderately increased cerebral and femoral artery blood flows. MCI-2016 did not change CMRO2, but decreased MVO2. Coronary and renal artery flows were moderately increased by 10 mg/kg, i.v., of MCI-2016. Renal function was suppressed after 10 mg/kg i.v., or 300 mg/kg, p.o., of MCI-2016. MCI-2016 potentiated that action of NE (increased in SBP, contractions of nictitating membrane and vas deferens), but showed little anti-cholinergic action. In contrast, MCI-2016 moderately increased gastrointestinal motility and salivatory response. As for the influence on isolated smooth muscles, MCI-2016 antagonized the contraction of blood vessles by high K+ at 10-6 g/ml, or more, and it depessed the contractions by ACh, 5-HT, histamine and BaCL2 and also depressed spontaneous movements of uterus and ileum at 10-5 M or more, in a nonspecific manner. MCI-2016 had no influence on liver damage and bile secretion, but inhibited stress ulcer and gastric acid secretion on the one hand, and caused gastric damage (125 mg/kg p.o., or more) on the other hand.