In vivo characterization of muscarinic receptors in peripheral tissues: Evaluation of bladder selectivity of anticholinergic agents to treat overactive bladder

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 377, Issue 4-6, 2008, Pages 463-471

  Maruyama, Shuji ^a   Hasuike, Naoki ^a   Suzuki, Kazuhiro ^a   Yamada, Shizuo ^a  

^a UNIVERSITY OF SHIZUOKA   (Japan)

Author keywords

3H QNB; In vivo muscarinic receptor binding; Oxybutynin; Propiverine; Submaxillary gland; Tolterodine; Urinary bladder

Indexed keywords

CHOLINERGIC RECEPTOR BLOCKING AGENT; MUSCARINIC RECEPTOR; OXYBUTYNIN; PROPIVERINE; QUINUCLIDINYL BENZILATE; TOLTERODINE; TRITIUM;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; BLADDER; COLON; CONFERENCE PAPER; CONTROLLED STUDY; DRUG DISTRIBUTION; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HEART; IN VIVO STUDY; MALE; MOUSE; NONHUMAN; OVERACTIVE BLADDER; RADIOACTIVITY; RECEPTOR BINDING; RECEPTOR INTRINSIC ACTIVITY; RECEPTOR OCCUPANCY; STOMACH; SUBMANDIBULAR GLAND; TISSUE DISTRIBUTION; TISSUE HOMOGENATE; XEROSTOMIA;

ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; BENZHYDRYL COMPOUNDS; BENZILATES; CHOLINERGIC ANTAGONISTS; CRESOLS; MALE; MANDELIC ACIDS; MICE; MUSCARINIC ANTAGONISTS; PHENYLPROPANOLAMINE; PROTEIN BINDING; QUINUCLIDINYL BENZILATE; RECEPTORS, MUSCARINIC; TIME FACTORS; URINARY BLADDER, OVERACTIVE;

EID: 45849153536     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-007-0207-1     Document Type: Conference Paper

References (31)

1. Abrams P, Freeman R, Anderström C, Mattiasson A (1998) Tolterodine, a new antimuscarinic agent: as effective but better tolerated than oxybutynin in patients with an overactive bladder. Br J Urol 81:801-810
2. Andersson K-E (2004) Antimuscarinics for treatment of overactive bladder. The Lancet Neurol 3:46-53
3. Hegde SS (2006) Muscarinic receptors in the bladder: from basic research to therapeutics. Br J Pharmacol 147:S80-S87
4. Hirano K, Maruyama S, Kimura R, Kagawa Y, Yamada S (2004) In vivo identification and characterization of binding sites for selective serotonin reuptake inhibitors in mouse brain. Life Sci 75:2933-2945
5. 3H-QNB in mouse brain. J Neural Trans 106:583-592
6. Madersbacher H, Mürtz G (2001) Efficacy, tolerability and safety profile of propiverine in the treatment of the overactive bladder (non-neurogenic and neurogenic). World J Urol 19:324-335
7. Madersbacher H, Halaska M, Voigt R, Alloussi S, Höfner K (1999) A placebo-controlled, multicentre study comparing the tolerability and efficacy of propiverine and oxybutynin in patients with urgency and urge incontinence. BJU International 84:646-651
8. Michel MC, Hedge SS (2006) Treatment of the overactive bladder syndrome with muscarinic receptor antagonists-a matter of metabolites? Naunyn-Schmiedebergs Arch Pharmacol 374:79-85
9. Mayuzumi K, Watanabe K, Tamaru K, Kasama T (1986) Effects of oxybutynin hydrochloride on the urinary bladder and urethra in in situ preparations. Nippon Yakurigaku Zasshi 87:557-571
10. Nilvebrant L, Andersson K-E, Gillberg PG, Stahl M, Sparf B (1997a) Tolterodine-a new bladder-selective antimuscarinic agent. Eur J Pharmacol 327:195-207
11. Nilvebrant L, Gillberg PG, Sparf B (1997b) Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol 81:169-172
12. Nomura N, Kaneko S, Hamakawa T, Nagai M, Iriki M (1989) Effects of propiverine hydrochloride (P-4) and its metabolites on urinary bladder function in anesthetized rats. Nippon Yakurigaku Zasshi 94:173-180
13. Oki T, Thoma A, Yamada S, Kimura R (2001) Muscarinic receptor binding characteristics in rat tissues after oral administration of oxybutynin and propiverine. Biol Pharam Bull 24:491-495
14. Oki T, Maruyama S, Takagi Y, Yamamura HI, Yamada S (2006) Characterization of muscarinic receptor binding and inhibition of salivation after oral administration of tolterodine in mice. Eur J Pharmacol 529:157-163
15. Påhlman I, Gozzi P (1999) Serum protein binding of tolterodine and its major metabolites in humans and several animal species. Biopharm Drug Dispos 20:91-99
16. Påhlman I, D'Argy R, Nilvebrant L (2001) Tissue distribution of tolterodine, a muscarinic receptor antagonist, and transfer into fetus and milk in mice. Arzneim Forsch/Drug Res 51:125-133
17. 3H]quinuclidinyl benzilate binding in rats. Brain Res 171:473-480
18. Postlind H, Danielson A, Lindgren A, Andersson SH (1998) Tolterodine: a new muscarinic receptor antagonist, is metabolized by cytochrome P450 2D6 and 3A4 in human liver microsomes. Drug Metab Disp 26:289-293
19. Terai T, Deguchi Y, Ohtsuka M, Kumada S (1991) Effects of the anticholinergic drug prifinium bromide on urinary bladder contractions in rat in vivo and in guinea-pig in vitro. Arzneimittelforschung 41:417-420
20. Todorova A, Vonderheid-Guth B, Dimpfel W (2001) Effects of tolterodine, trospium chloride, and oxybutynin on the central nervous system. J Clin Pharmacol 41:636-644
21. Uchida S, Yamada S, Nagai K, Deguchi Y, Kimura R (1997) Brain pharmacokinetics and in vivo receptor binding of 1,4-dihydropyridine calcium channel antagonists. Life Sci 61:2083-2090
22. Uchida S, Yamada S, Deguchi Y, Yamamoto M, Kimura R (2000) In vivo specific binding characteristics and pharmacokinetics of a 1,4-dihydropyridine calcium channel antagonist in the senescent mouse brain. Pharm Res 17:844-850
23. Uchida S, Kurosawa S, Fujino (Oki) T, Kato Y, Nanri M, Yoshida K, Yamada S (2007) Binding activities by propiverine and its N-oxide metabolites of L-type calcium channel antagonist receptors in the rat bladder and brain. Life Sci 80:2454-2460
24. Weizman R, Weifman A, Kook KA, Vocci F, Deutsh SI, Paul SM (1989) Repeated swim stress alters brain benzodiazepine receptors measured in vivo. J Pharmacol Exp Ther 249:701-707
25. Wuest M, Weiss A, Waelbroeck M, Braeter M, Kelly LU, Hakenberg OW, Ravens U (2006) Propiverine and metabolites: differences in binding to muscarinic receptors and in functional models of detrusor contraction. Naunyn-Schmiedebergs Arch Pharmacol 374:87-97
26. 1 adrenoceptors of in tissues in relation to the pharmacokinetics. J Pharmacol Exp Ther 289:1575-1583
27. 1-adrenoceptor subtype selectivity of KMD-3213 in rat tissues. J Pharmacol Exp Ther 296:160-167
28. Yamada S, Nakajima M, Kusaka T, Uchida S, Kimura R (2002) In vivo receptor binding of benidipine and amlodipine in mesenteric arteries other tissues of spontaneously hypertensive rats. Life Sci 70:1999-2011
29. 3 muscarinic receptor subtype selectivity of darifenacin in mice. Life Sci 80:127-132
30. Yamamoto Y, Tsuda M, Uda K, Matsushita H, Shindo T, Kawaguchi Y (1995) Pharmacokinetic studies on propiverine hydrochloride. Metabolites in urinary bladder, other tissues and urine of rats. Xenobiotic Metabol Dispos 10:205-210
31. Yamamura HI, Kuhar MJ, Snyder SH (1974) In vivo identification of muscarinic cholinergic receptor binding in rat brain. Brain Res 80:170-176