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- Iloperidone 133454-47-4
- Iloperidone 133454-47-4
Iloperidone 133454-47-4
产品描述 描述 Iloperidone is an atypical antipsychotic for the treatment of schizophrenia symptoms. Hoechst Marion Roussel Inc. made initial inquiries into the drug; however, in May 1996, they discontinued research, and in June 1997 gave research rights to Titan Pharmaceuticals. Titan then handed over worldwide development, manufacturing and marketing rights to Novartis in August 1998. On June 9, 2004, Titan Pharmaceuticals announced that the Phase III development rights have been acquired by Vanda Pharmaceuticals. FDA approved on May 9, 2009.
纯度 ＞98%储存/保存方法 Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.基本信息 别名 伊潘立酮；HP 873外观 白色至灰白色结晶粉末可溶性/溶解性 DMSO : 26 mg/mL (61 mM)
Ethanol : 4 mg/mL (9.37 mM)生物活性 靶点 5-HTIn vitro(体外研究) Iloperidone displays high affinity (Ki Iloperidone displays higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 nM and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM). Iloperidone significantly increases dopa accumulation, an index of dopamine turnover in response to D2 receptor blockade, at doses from 0.3 mg/kg to 10 mg/kg i.p. in the striatum and from 1 mg/kg to 10 mg/kg in the nucleus accumbens.In vivo(体内研究) Iloperidone exerts behavioral effects in pharmacological rats models of disrupted sensorimotor gating consistent with "atypical" antipsychotics, mediated by antagonism of dopaminergic and noradrenergic receptors. Iloperidone (1 and 3 mg/kg) prevents the PPI-disruptive effects of treatment with 1 mg/kg PCP. Iloperidone (0.3 mg/kg) prevents cirazoline-induced PPI deficits, independent of its effects on startle magnitude. Iloperidone (10 mg/kg) and Melperone (10 mg/kg) produce an equivalent or a smaller increase in DA release in the nucleus accumbens (NAC) of rats, respectively, compared to the mPFC, whereas none of them increase acetylcholine (ACh) release in the NAC.参考文献 参考文献 1. George M, et al. Eur J Clin Pharmacol. 2013 Apr 2.
2. Kongsamut S, et al. Eur J Pharmacol. 1996 Dec 19;317(2-3):417-23.
3. Bobo WV. Expert Rev Clin Pharmacol. 2013 Jan;6(1):61-91.
研究领域 研究领域 MetabolismTypes of diseaseObesityNeuroscienceProcessesNeuroscienceNeurology processMetabolismNeuroscienceNeurotransmissionReceptors / ChannelsGPCRSerotonin ReceptorsSignal TransductionSignaling PathwayG Protein SignalingGPCRDrug DiscoverySmall Molecule DrugLead Compound DiscoveryIloperidone 133454-47-4温馨提示：本产品仅作科研实验使用，不支持临床等研究