The hypotensive action of 4-(5,6-dimethyl-2-benzofuranyl) piperidine HCl (CGP 6085 A) in spontaneously hypertensive rats.
CGP 6085 A, [4-(5,6-dimethyl-2-benzofuranyl)piperidine HCl], has been found to be a mild to moderately potent hypotensive agent. One hour following CGP 6085 A administration (10 mg/kg, i.p.), a maximal reduction in blood pressure of approximately 20-30 mm Hg is observed in spontaneously hypertensive rats. The maximal reduction in blood pressure was observed at a dose of 3 mg/kg. CGP 6085 A blocks 5-HT uptake in the brainstem when assessed in vivo by use of the serotonin depletor, H 75/12 (3-hydroxy-4-methyl-alpha-ethyl-phenylethylamine). The maximal inhibitory effect on 5-HT uptake occurred at 10 mg/kg CGP 6085 A. The reduction in blood pressure correlates well with the ability of the drug to inhibit 5-HT uptake as assayed by H 75/12, with a correlation coefficient of 0.71 for SH rats. However, since the drug has not been widely characterized, alternate explanations for the cardiovascular pharmacological properties of CGP 6085 A are also proposed.
E C
EC
Kulakowski
J H
JH
Hurst
M
M
Scheinin
M
M
Linnoila
W
W
Lovenberg
D000662:Amphetamines / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D001933:Brain Stem / Q000378:metabolism; D006339:Heart Rate / Q000187:drug effects; D006897:Hydroxyindoleacetic Acid / Q000378:metabolism; D006973:Hypertension / Q000188:drug therapy*; D008297:Male; D009599:Nitroprusside / Q000494:pharmacology; D010880:Piperidines / Q000627:therapeutic use*; D051381:Rats; D011918:Rats, Inbred SHR; D012701:Serotonin / Q000378:metabolism
D000662:Amphetamines; D010880:Piperidines; D009599:Nitroprusside; C001632:4-methyl-alpha-ethyl-m-tyramine; D012701:Serotonin; D006897:Hydroxyindoleacetic Acid; C015613:4-(5,6-dimethyl-2-benzofuranyl)piperidine