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Asenapine Sale

(Synonyms: 阿塞那平; Org 5222) 目录号 : GC11824

An atypical antipsychotic

Asenapine Chemical Structure

Cas No.:65576-45-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥998.00
现货
25mg
¥389.00
现货
100mg
¥1,565.00
现货
1g
¥3,927.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Animal experiment:

Rats: Asenapine maleate is suspended in 10% hydroxypropyl-β-cyclodextrin and administered in a volume of 1 mL/kg body weight . Rats are individually fear conditioned using electrical foot shock in a Skinner box. Animals are injected intraperitoneally (i.p.) with asenapine, clozapine, olanzapine, buspirone, or SB242084 at 30 min before freezing behaviour assessment[3]. Mice: Male ICR mice are repeatedly treated with 0.1 or 0.3mg/kg injections of asenapine and then tested in a battery of behavioural tests related to anxiety including the open-field test, elevated plus-maze (EPM), defensive marble burying and hyponeophagia tests[4].

References:

[1]. Stoner SC, et al. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40.
[2]. Shahid M, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.
[3]. Ohyama M,et al. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336.
[4]. Ene HM, et al. Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Acta Neuropsychiatr. 2016 Apr;28(2):85-91.

产品描述

Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.

Relative to its D2 receptor affinity, asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, α2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), α2A (7.3), α2B (8.3), α2C (6.8) and H1 (8.4) receptors[2].

Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats[3]. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice[4].

References:
[1]. Stoner SC, et al. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40.
[2]. Shahid M, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.
[3]. Ohyama M,et al. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336.
[4]. Ene HM, et al. Effects of repeated asenapine in a battery of tests for anxiety-like behaviours in mice. Acta Neuropsychiatr. 2016 Apr;28(2):85-91.

Chemical Properties

Cas No. 65576-45-6 SDF
别名 阿塞那平; Org 5222
化学名 (3aS,12bS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole fumarate
Canonical SMILES [H][C@@]1(C(C=C(Cl)C=C2)=C2OC3=C4C=CC=C3)[C@]4([H])CN(C)C1.OC(/C=C/C(O)=O)=O
分子式 C17H16ClNO.C4H4O4 分子量 401.84
溶解度 ≥ 20.092mg/mL in DMSO, ≥ 24.75 mg/mL in EtOH with ultrasonic, ≥ 3.025 mg/mL in Water with ultrasonic 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.4886 mL 12.4428 mL 24.8855 mL
5 mM 0.4977 mL 2.4886 mL 4.9771 mL
10 mM 0.2489 mL 1.2443 mL 2.4886 mL
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