[Effects of propiverine hydrochloride (P-4) and its metabolites on urinary bladder function in anesthetized rats].

  title={[Effects of propiverine hydrochloride (P-4) and its metabolites on urinary bladder function in anesthetized rats].},
  author={Norikazu Nomura and Shuji Kaneko and Toshihiro Hamakawa and Masanori Nagai and Masami Iriki},
  journal={Nihon yakurigaku zasshi. Folia pharmacologica Japonica},
  volume={94 3},
  • N. Nomura, S. Kaneko, +2 authors M. Iriki
  • Published 1 September 1989
  • Chemistry, Medicine
  • Nihon yakurigaku zasshi. Folia pharmacologica Japonica
The effects of P-4 and its active metabolites, 1-methyl-4-piperidyl diphenylpropoxyacetate N-oxide[P-4(N----O)], 1-methyl-4-piperidyl benzilate N-oxide [DPr-P-4 (N----O)] and 1-methyl-4-piperidyl benzilate hydrochloride (DPr-P-4), on urinary bladder function were investigated in urethane anesthetized rats. By cystometrography, P-4 (2, 4 mg/kg, i.v.) and P-4 (N----O) (4 mg/kg, i.v.), which have direct action on smooth muscles, significantly increased the maximum vesical volume. As for rhythmic… 
Binding activities by propiverine and its N-oxide metabolites of L-type calcium channel antagonist receptors in the rat bladder and brain.
It is shown that propiverine and P-4(N-->O) exert a significant binding activity of L-type calcium channel antagonist receptors in the bladder and these effects may be pharmacologically relevant in the treatment of overactive bladder after oral administration of propivine.
The N-Oxide Metabolite Contributes to Bladder Selectivity Resulting from Oral Propiverine: Muscarinic Receptor Binding and Pharmacokinetics
M-2 may contribute greatly to the relatively selective and long-lasting occupation of bladder muscarinic receptors after oral administration of propiverine, indicating specific distribution of this metabolite into the target organ.
Effect of α1-adrenoceptor antagonists on urinary bladder function in urethane-anesthetized rats
Abstract 1. 1. We investigated the effects of selective α 1 -adrenoceptor antagonists on rhythmic bladder contraction and cystometrograms as representative of urinary bladder function in
Muscarinic receptor binding characteristics in rat tissues after oral administration of oxybutynin and propiverine.
It is shown that oxybutynin and propiverine, after oral administration, bind significantly to muscarinic receptors in tissues such as the bladder, which is the target organ for the treatment of urinary incontinence, and that oxy butynin appears to exhibit long-term binding to musCarinic receptor in the salivary gland.
The role of species-dependent metabolism in the regional brain retention of 18F-labeled muscarinic acetylcholine receptor ligands.
A radiolabeled metabolite for 2b which was formed to a much greater extent in mice than rats and may have a higher receptor binding affinity than authentic 2b, and thus be responsible for the apparent receptor-mediated binding in the mouse brain.
In vivo bladder selectivity of imidafenacin, a novel antimuscarinic agent, assessed by using an effectiveness index for bladder capacity in rats
Imidafenacin shows the most highly selective for bladder over the tissues related to major antimuscarinic side effects, compared to the other three well-known antimus carinics tested in the rat.
Kinetics of propiverine as assessed by radioreceptor assay in poor and extensive metabolizers of debrisoquine
The poor and extensive metabolizers of debrisoquine did not differ significantly with regard to the concentration time behaviour of the active drug components, pattern of major metabolites, adverse drug reactions or any pharmacodynamic parameters measured.
In vivo characterization of muscarinic receptors in peripheral tissues: evaluation of bladder selectivity of anticholinergic agents to treat overactive bladder
It is demonstrated that [3H]QNB may be a useful ligand for in vivo characterization of muscarinic receptor binding of anticholinergic agents to treat overactive bladder.
The forefront for novel therapeutic agents based on the pathophysiology of lower urinary tract dysfunction: bladder selectivity based on in vivo drug-receptor binding characteristics of antimuscarinic agents for treatment of overactive bladder.
In vivo quantitative autoradiography using (+)N-[(11)C]methyl-3-piperidyl benzilate in rats showed significant occupancy of brain muscarinic receptors on intravenous injection of oxybutynin, propiverine, solifenacin, and tolterodine, and the newer generation of antimuscarinic agents may be advantageous in the bladder selectivity after systemic administration.
Basic and clinical aspects of antimuscarinic agents used to treat overactive bladder
Basic and clinical aspects of eight antimuscarinic agents clinically used to treat urinary dysfunction in patients with OAB are highlighted and the measurement of drug‐receptor binding after oral administration of these agents allows for clearer understanding of bladder selectivity by the integration of pharmacodynamics and pharmacokinetics under in vivo conditions.