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Titolo:
Muscarinic receptor binding characteristics in rat tissues after oral administration of oxybutynin and propiverine
Autore:
Oki, T; Yamada, S; Tohma, A; Kimura, R;
Indirizzi:
Univ Shizouka, Sch Pharmaceut Sci, Dept Biopharm, Shizouka 4228526, Japan Univ Shizouka Shizouka Japan 4228526 t Biopharm, Shizouka 4228526, Japan
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 5, volume: 24, anno: 2001,
pagine: 491 - 495
SICI:
0918-6158(200105)24:5<491:MRBCIR>2.0.ZU;2-P
Fonte:
ISI
Lingua:
ENG
Soggetto:
CALCIUM-ANTAGONIST; 6-HYDROXYDOPAMINE TREATMENT; ANTIMUSCARINIC AGENT; PLASMA-CONCENTRATION; URINARY-BLADDER; CHOLINE UPTAKE; PHARMACOKINETICS; OCCUPANCY; DIISOPROPYLFLUOROPHOSPHATE; TOLTERODINE;
Keywords:
oxybutynin; propiverine; bladder; submaxillary gland; muscarinic receptor binding;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
27
Recensione:
Indirizzi per estratti:
Indirizzo: Yamada, S Univ Shizouka, Sch Pharmaceut Sci, Dept Biopharm, 52-1 Yada, Shizouka 4228526, Japan Univ Shizouka 52-1 Yada Shizouka Japan 4228526 a 4228526, Japan
Citazione:
T. Oki et al., "Muscarinic receptor binding characteristics in rat tissues after oral administration of oxybutynin and propiverine", BIOL PHAR B, 24(5), 2001, pp. 491-495

Abstract

Ex vivo muscarinic receptor binding of oxybutynin and propiverine, the most commonly used anticholinergic agents for the treatment In patients with urinary incontinence, was investigated in rat tissues. The oral administration of oxybutynin (50.8 and 127 mu mol/kg) caused a significant increase in the apparent dissociation constant (K-d) for specific (-)-/H-3/QNB binding in the rat bladder, prostate, submaxillary gland, heart and cerebral col-tcs, compared with each of the control values. Also, in the submaxillary gland of these rats, there was a reduction in the maximal number of binding sites (B-max) for (-)-/H-3/QNB binding. Similarly. oral administration of propiverine at doses of 74.3-297 mu mol/kg bl-ought about a significant increase in the K-d values for (-)-/H-3/QNB binding in rat tissues including the bladder, and greater increase in K-d values was seen in the rat prostate, heart and submaxillary gland. On the other hand, oral administration of propiverine, unlike oxybutynin, resulted in very little reduction in the B-max valules fur (-)-/H-3/QNB binding in the submaxillary gland. In conclusion, the present study has 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 oxybutynin appears to exhibit long-term binding to muscarinic receptors in the salivary gland.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/01/20 alle ore 07:28:17