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Iloperidone hydrochloride Sale

(Synonyms: 盐酸伊潘立酮; HP 873 hydrochloride) 目录号 : GC10799

An atypical antipsychotic

Iloperidone hydrochloride Chemical Structure

Cas No.:1299470-39-5

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10mg
¥347.00
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25mg
¥704.00
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100mg
¥2,247.00
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产品描述

Iloperidone (hydrochloride) is a D(2)/5-HT(2) receptor antagonistis, which is an atypical antipsychotic for the treatment of schizophrenia symptoms.Target: 5-HT receptor; Dopamine receptorIloperidone (hydrochloride) is the hydrochloride of iloperidone, iloperidone (HP 873; 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy] -3- methoxyphenyl]ethanone) is a compound currently in clinical trials for the treatment of schizophrenia. Iloperidone displays affinity for dopamine D2 receptors and for 5-HT2A receptors and has a variety of in vivo activities suggestive of an atypical antipsychotic. Iloperidone displayed higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displayed high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 and 21.6 nM, respectively), and was found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM) [1]. Iloperidone was eliminated slowly, with a mean t1/2 of 13.5 to 14.0 hours. Coadministration with food did not significantly affect AUC, tmax, or Cmax. These results indicate that the rate of iloperidone's absorption is decreased, but the overall bioavailability is unchanged, when the drug is taken with food. Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events [2]. Iloperidone pharmacokinetics and pharmacodynamics are presented herein, together with an evaluation of clinical safety and efficacy results [3].Clinical indications: Post traumatic stress disorder; Schizophrenia Toxicity: Commonly observed adverse reactions (incidence ≥5% and two-fold greater than placebo) were: dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, and weight increased.

References:
[1]. Kongsamut, S., et al., Iloperidone binding to human and rat dopamine and 5-HT receptors. Eur J Pharmacol, 1996. 317(2-3): p. 417-23.
[2]. Sainati, S.M., et al., Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic. J Clin Pharmacol, 1995. 35(7): p. 713-20.
[3]. Albers, L.J., A. Musenga, and M.A. Raggi, Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market Expert Opin Investig Drugs, 2008. 17(1): p. 61-75.

Chemical Properties

Cas No. 1299470-39-5 SDF
别名 盐酸伊潘立酮; HP 873 hydrochloride
化学名 1-(4-(3-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)propoxy)-3-methoxyphenyl)ethanone hydrochloride
Canonical SMILES CC(C1=CC(OC)=C(OCCCN2CCC(C3=NOC4=C3C=CC(F)=C4)CC2)C=C1)=O.Cl
分子式 C24H28ClFN2O4 分子量 462.94
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 2.1601 mL 10.8005 mL 21.6011 mL
5 mM 0.432 mL 2.1601 mL 4.3202 mL
10 mM 0.216 mL 1.0801 mL 2.1601 mL
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