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Studies on the effects of piperidine derivatives on blood pressure and smooth muscles contractions.

Ten substituted phenacyl derivatives of 4-hydroxypiperidine were synthesized and studied for their effects on the mean arterial blood pressure (MABP) in normotensive anaesthetized rats and smooth muscles contractions of isolated rabbit jejunum. Two derivatives caused fall in blood pressure at the dose of 10-20 mg/kg and one rise in blood pressure at the dose of 20 mg/kg. Two compounds exhibited biphasic response (hypotensive followed by hypertensive) and one gave triphasic response at 10 mg/kg dose. Rest of four derivatives were found devoid of any effect on mean arterial blood pressure up to the dose of 30 mg/kg. All the derivatives except two caused relaxant effect on the spontaneous contraction of rabbit jejunum at the dose range of 0.1-2 mg/kg.

Animals↗

Assessment of the chloroethyl analog of 3-PPP (N-n-propyl-3-(3-hydroxyphenyl)-piperidine), 3-PPP-C1 as an irreversible ligand for central dopaminergic recognition sites.

NCA, the chloro analog of the potent dopamine agonist NPA is an irreversible ligand at dopamine receptors in mammalian brain. The chloroethyl analog of the recently described putative dopamine autoreceptor agonist 3-PPP, 3-PPP-C1, was evaluated for its potential use as an irreversible autoreceptor ligand. N-Chloroethylation of 3-PPP reduced the intrinsic affinity of the agonist seven-fold and, consequently, in contrast to NCA, it was found that 3-PPP-C1 was not a good irreversible ligand at dopamine receptors.

Animals↗