Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine.
作者： Shinya Uchida , Yasuhiro Kato , Kazufumi Hirano , Yoshiyuki Kagawa , Shizuo Yamada
DOI: 10.1016/J.LFS.2007.01.038
关键词:
摘要: The present study was conducted to characterize the binding of neurotransmitter receptors (dopamine D(2), serotonin 5-HT(2), histamine H(1), adrenaline alpha(1) and muscarine M(l) receptors) in rat's brain after oral administration haloperidol, risperidone, olanzapine. Haloperidol at 1 3 mg/kg displayed significant activity bind D(2) receptor (increase Kd value for [(3)H]raclopride binding) corpus striatum with little change toward 5-HT(2) (binding parameters [(3)H]ketanserin). In contrast, risperidone (0.1-3 mg/kg) showed roughly 30 times more affinity than receptor. Also, olanzapine (1-10 most active H(1) cerebral cortex, striatum, hippocampus, less receptors, least M(1) receptors. conclusion, haloperidol administered orally selectively respectively, rat brain, while binds
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Elliott Richelson, Terry Souder, Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sciences. ,vol. 68, pp. 29- 39 ,(2000) , 10.1016/S0024-3205(00)00911-5
Yoshihisa Nozawa, Hidekazu Miyake, Shizuo Yamada, Ryohei Kimura, Receptor Occupancy in Myocardium, Adrenal Cortex, and Brain by TH-142177, a Novel AT1 Receptor Antagonist in Rats, in Relation to Its Plasma Concentration and Hypotensive Effect Pharmaceutical Research. ,vol. 15, pp. 911- 917 ,(1998) , 10.1023/A:1011932800729
A. Lewis Farr, Oliver H. Lowry, Rose J. Randall, Nira J. Rosebrough, Protein Measurement with the Folin Phenol Reagent Journal of Biological Chemistry. ,vol. 193, pp. 265- 275 ,(1951)
A. Eens, P. A. J. Janssen, W. Gommeren, J. E. Leysen, J. C. Stoof, D. De Chaffoy De Courcelles, Biochemical profile of risperidone, a new antipsychotic. Journal of Pharmacology and Experimental Therapeutics. ,vol. 247, pp. 661- 670 ,(1988)
Gerald Zernig, James H. Woods, John W. Lewis, Timothy Burke, Mechanism of clocinnamox blockade of opioid receptors: evidence from in vitro and ex vivo binding and behavioral assays. Journal of Pharmacology and Experimental Therapeutics. ,vol. 279, pp. 23- 31 ,(1996)
S H Zorn, D W Schulz, P A Seymour, A W Schmidt, H R Howard, J A Lowe, V Guanowsky, T F Seeger, S McLean, L A Lebel, Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity. Journal of Pharmacology and Experimental Therapeutics. ,vol. 275, pp. 101- 113 ,(1995)
Raymond S.L. Chang, Vinh Tan Tran, Solomon H. Snyder, Histamine H1-receptors in brain labeled with 3H-mepyramine European Journal of Pharmacology. ,vol. 48, pp. 463- 464 ,(1978) , 10.1016/0014-2999(78)90177-2
Hannah E. Rosenthal, A graphic method for the determination and presentation of binding parameters in a complex system Analytical Biochemistry. ,vol. 20, pp. 525- 532 ,(1967) , 10.1016/0003-2697(67)90297-7
Kazufumi Hirano, Ryohei Kimura, Yumi Sugimoto, Jun Yamada, Shinya Uchida, Yasuhiro Kato, Hisakuni Hashimoto, Shizuo Yamada, Relationship between brain serotonin transporter binding, plasma concentration and behavioural effect of selective serotonin reuptake inhibitors British Journal of Pharmacology. ,vol. 144, pp. 695- 702 ,(2005) , 10.1038/SJ.BJP.0706108
F P Bymaster, C C Felder, Role of the cholinergic muscarinic system in bipolar disorder and related mechanism of action of antipsychotic agents. Molecular Psychiatry. ,vol. 7, ,(2002) , 10.1038/SJ.MP.4001019