Basic information Safety Supplier Related

Saphris hydrochloride

Basic information Safety Supplier Related

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
Mol File:
1412458-61-7.mol
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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
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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 hydrochlorideSupplier

BOC Sciences
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1-631-485-4226; 16314854226
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info@bocsci.com
Haoyuan Chemexpress Co., Ltd.
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021-58950125
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info@chemexpress.com
AdooQ BioScience, LLC
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+1 (866) 930-6790
Email
info@adooq.com
ShangHai Caerulum Pharma Discovery Co., Ltd.
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18149758185
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sales-cpd@caerulumpharma.com
LETOPHARM LIMITED
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+86-21-5821 5861
Email
sales@letopharm.com
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