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| | Saphris hydrochloride Basic information |
| Product Name: | Saphris hydrochloride | | Synonyms: | Asenapine (hydrochloride);Saphris hydrochloride;(3aS,12bS)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole hydrochloride (1:1);Asenapine HCl;(3AS,12BS)-5-CHLORO-2-METHYL-2,3,3A,12B-TETRAHYDRO-1H-DIBENZO[2,3:6,7]OXEPINO[4,5-C]PYRROLE HYDROCHLORIDE;Asenapine HCl (Org 5222 HCl) | | CAS: | 1412458-61-7 | | MF: | C17H17Cl2NO | | MW: | 322.23 | | EINECS: | | | Product Categories: | | | Mol File: | 1412458-61-7.mol |  |
| | Saphris hydrochloride Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 50 mg/mL (155.17 mM; Need ultrasonic) | | form | Powder | | color | White to off-white |
| | Saphris hydrochloride Usage And Synthesis |
| Uses | Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively. | | in vivo | 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]. | | IC 50 | sPLA2: 2.5 nM (Ki); 5-HT2A Receptor: 0.06 nM (Ki); 5-HT2C Receptor: 0.03 nM (Ki); 5-HT7 Receptor: 0.13 nM (Ki); D2 Receptor: 1.3 nM (Ki); D3 Receptor: 0.42 nM (Ki); D4 Receptor: 1.1 nM (Ki) | | References | [1] Stoner SC, Pace HA. Asenapine: a clinical review of a second-generation antipsychotic. Clin Ther. 2012 May;34(5):1023-40. DOI:10.1016/j.clinthera.2012.03.002
[2] Shahid M, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. DOI:10.1177/0269881107082944
[3] Ohyama M,et al. Asenapine reduces anxiety-related behaviours in rat conditioned fear stress model. Acta Neuropsychiatr. 2016 Dec;28(6):327-336. DOI:10.1017/neu.2016.17
[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. DOI:10.1017/neu.2015.53 |
| | Saphris hydrochloride Preparation Products And Raw materials |
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