Noninvasive evaluation of brain muscarinic receptor occupancy of oxybutynin, darifenacin and imidafenacin in rats by positron emission tomography

Life Sciences

Volumn 87, Issue 5-6, 2010, Pages 175-180

  Yoshida, Akira ^a   Maruyama, Shuji ^a   Fukumoto, Dai ^b   Tsukada, Hideo ^b   Ito, Yoshihiko ^a   Yamada, Shizuo ^a  

^a UNIVERSITY OF SHIZUOKA   (Japan)

^b CENTRAL RESEARCH LABORATORY   (Japan)

Author keywords

Antimuscarinics; Brain receptor occupancy; Overactive bladder; Positron emission tomography; Quantitative autoradiography

Indexed keywords

DARIFENACIN; IMIDAFENACIN; MUSCARINIC RECEPTOR; OXYBUTYNIN; RADIOLIGAND;

ADVERSE OUTCOME; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BLADDER; BRAIN; BRAIN CORTEX; BRAIN RADIOGRAPHY; CONTROLLED STUDY; CORPUS STRIATUM; DISSOCIATION CONSTANT; DOSE RESPONSE; DRUG RECEPTOR BINDING; EX VIVO STUDY; IN VIVO STUDY; INJECTION; LIGAND BINDING; MALE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RAT;

ANIMALS; AUTORADIOGRAPHY; BENZOFURANS; BRAIN; DOSE-RESPONSE RELATIONSHIP, DRUG; IMIDAZOLES; MALE; MANDELIC ACIDS; MUSCARINIC ANTAGONISTS; POSITRON-EMISSION TOMOGRAPHY; PROTEIN BINDING; PYRROLIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, MUSCARINIC; URINARY BLADDER, OVERACTIVE;

ANIMALIA; RATTUS;

EID: 77954958782     PISSN: 00243205     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.lfs.2010.06.008     Document Type: Article

References (32)

1. Abrams P., Andersson K.E. Muscarinic receptor antagonists for overactive bladder. BJU International 2007, 100:987-1006.
2. Ancelin M.L., Artero S., Portet F., Dupuy A.M., Touchon J., Ritchie K. Non-degenerative mild cognitive impairment in elderly people and use of anticholinergic drugs: longitudinal cohort study. BMJ 2006, 332:455-459.
3. Anderson K.E. Pharmacology of lower urinary tract smooth muscles and penile erectile tissues. Pharmacological Reviews 1993, 45:253-308.
4. Beauchamp H.T., Chang R.S., Siegl P.K., Gibson R.E. In vivo receptor occupancy of the angiotensin II receptor by nonpeptide antagonists: relationship to in vitro affinities and in vivo pharmacologic potency. The Journal of Pharmacology and Experimental Therapeutics 1995, 272:612-618.
5. Borella T.L., De Luca L.A., Colombari D.S., Menani J.V. Central muscarinic receptor subtypes involved in pilocarpine-induced salivation, hypertension and water intake. British Journal of Pharmacology 2008, 155:1256-1263.
6. 2 subtypes of muscarinic binding sites in rat brain. The Journal of Pharmacology and Experimental Therapeutics 1990, 255:1148-1157.
7. Homma Y., Yamaguchi O. Long-term safety, tolerability, and efficacy of the novel anti-muscarinic agent imidafenacin in Japanese patients with overactive bladder. International Journal of Urology 2008, 15:986-991.
8. Homma Y., Yamaguchi O. A randomized, double-blind, placebo- and propiverine-controlled trial of the novel antimuscarinic agent imidafenacin in Japanese patients with overactive bladder. International Journal of Urology 2009, 16:499-506.
9. Homma Y., Yamaguchi T., Yamaguchi O. A randomized, double-blind, placebo-controlled phase II dose-finding study of the novel anti-muscarinic agent imidafenacin in Japanese patients with overactive bladder. International Journal of Urology 2008, 15:809-815.
10. Innis R.B., Cunningham V.J., Delforge J., Fujita M., Gjedde A., Gunn R.N., Holden J., Houle S., Huang S.C., Ichise M., Iida H., Ito H., Kimura Y., Koeppe R.A., Knudsen G.M., Knuuti J., Lammertsma A.A., Laruelle M., Logan J., Maguire R.P., Mintun M.A., Morris E.D., Parsey R., Price J.C., Slifstein M., Sossi V., Suhara T., Votaw J.R., Wong D.F., Carson R.E. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. Journal of Cerebral Blood Flow and Metabolism 2007, 27:1533-1539.
11. Katz I.R., Sands L.P., Bilker W., DiFilippo S., Boyce A., D'Angelo K. Identification of medications that cause cognitive impairment in older people: the case of oxybutynin chloride. Journal of the American Geriatrics Society 1998, 46:8-13.
12. Kay G.G., Abou-Donia M.B., Messer W.S., Murphy D.G., Tsao J.W., Ouslander J.G. Antimuscarinic drugs for overactive bladder and their potential effects on cognitive function in older patients. Journal of the American Geriatrics Society 2005, 53:2195-2201.
13. Kay G., Crook T., Rekeda L., Lima R., Ebinger U., Arguinzoniz M., Steel M. Differential effects of the antimuscarinic agents darifenacin and oxybutynin ER on memory in older subjects. European Urology 2006, 50:317-326.
14. 1 receptor subtypes and selectivity for urinary bladder over salivary gland. Arzneimittel-Forschung 2007, 57:92-100.
15. Kobayashi F., Yageta Y., Yamazaki T., Wakabayashi E., Inoue M., Segawa M., et al. Pharmacological effects of imidafenacin (KRP-197/ONO-8025), a new bladder selective anti-cholinergic agent, in rats. Comparison of effects on urinary bladder capacity and contraction, salivary secretion and performance in the Morris water maze task. Arzneimittel-Forschung 2007, 57:147-154.
16. Kornblum H.I., Araujo D.M., Annala A.J., Tatsukawa K.J., Phelps M.E., Cherry S.R. In vivo imaging of neuronal activation and plasticity in the rat brain by high resolution positron emission tomography (microPET). Nature Biotechnology 2000, 18:655-660.
17. Lopes de Almeida R., De Luca L.A., de Almeida Colombari D.S., Menani J.V., Renzi A. Damage of the medial preoptic area impairs peripheral pilocarpine-induced salivary secretion. Brain Research 2006, 1085:144-148.
18. Maruyama S., Oki T., Otsuka A., Shinbo H., Ozono S., Kageyama S., Mikami Y., Araki I., Takeda M., Masuyama K., Yamada S. Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. The Journal of Urology 2006, 175:365-369.
19. Maruyama S., Tsukada H., Nishiyama S., Kakiuchi T., Fukumoto D., Oku N., Yamada S. In vivo quantitative autoradiographic analysis of brain muscarinic receptor occupancy by antimuscarinic agents for overactive bladder treatment. The Journal of Pharmacology and Experimental Therapeutics 2008, 325:774-781.
20. Mizuta T., Kitamura K., Iwata H., Yamagishi Y., Ohtani A., Tanaka K., Inoue Y. Performance evaluation of a high-sensitivity large-aperture small-animal PET scanner: ClairvivoPET. Annals of Nuclear Medicine 2008, 22:447-455.
21. Ohno T., Nakade S., Nakayama K., Kitagawa J., Ueda S., Miyabe H., Miyata Y. Absolute bioavailability of imidafenacin after oral administration to healthy subjects. British Journal of Clinical Pharmacology 2008, 65:197-202.
22. Oki T., Kageyama A., Takagi Y., Uchida S., Yamada S. Comparative evaluation of central muscarinic receptor binding activity by oxybutynin, tolterodine and darifenacin used to treat overactive bladder. The Journal of Urology 2007, 177:766-770.
23. Ouslander J.G. Management of overactive bladder. The New England Journal of Medicine 2004, 350:786-799.
24. Pakulski C., Drobnik L., Millo B. Age and sex as factors modifying the function of the blood-cerebrospinal fluid barrier. Medical Science Monitor 2000, 6:314-318.
25. Scheife R., Takeda M. Central nervous system safety of anticholinergic drugs for the treatment of overactive bladder in the elderly. Clinical Therapeutics 2005, 27:144-153.
26. Skerjanec A. The clinical pharmacokinetics of darifenacin. Clinical Pharmacokinetics 2006, 45:325-350.
27. Suzuki M., Noguchi Y., Okutsu H., Ohtake A., Sasamata M. Effect of antimuscarinic drugs used for overactive bladder on learning in a rat passive avoidance response test. European Journal of Pharmacology 2007, 557:154-158.
28. Takakura A.C., Moreira T.S., Laitano S.C., De Luca Júnior L.A., Renzi A., Menani J.V. Central muscarinic receptors signal pilocarpine-induced salivation. Journal of Dental Research 2003, 82:993-997.
29. 11C]4-MPB. Synapse 2001, 39:182-192.
30. Wein A.J., Rovner E.S. Definition and epidemiology of overactive bladder. Urology 2002, 60:7-12.
31. 35S]GTPgammaS in rat brain and spinal cord. British Journal of Pharmacology 2003, 139:1462-1468.
32. Yarker Y.E., Goa K.L., Oxybutynin Fitton A. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability. Drugs Aging 1995, 6:243-262.