Asenapine Maleate
Synonym(s):(3aRS,12bRS)-5-Chloro-2-methyl-2,3,3a,12btetrahydro-1Hdibenzo[2,3:6,7]oxepino[4,5-c]pyrrole (2Z)-2-butenedioate;Org 5222;trans-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz(2,3:6,7)oxepino(4,5-c)pyrrole maleate
- CAS NO.:85650-56-2
- Empirical Formula: C21H20ClNO5
- Molecular Weight: 401.84
- MDL number: MFCD00900588
- EINECS: 288-064-8
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-09-20 16:43:00
What is Asenapine Maleate?
Description
Asenapine, a dual antagonist of dopamine D2and serotonin 5-HT2receptors, was launched for the acute treatment of schizophreniaand manic or mixed episodes associated with bipolar I disorder in adults. Asenapine exhibits high affinity for serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors (Ki = 2.5, 4.0, 0.06, 0.16, 0.03, 1.6, 0.25, and 0.13 nM, respectively); dopamine D1, D2, D3, and D4 receptors (Ki = 1.4, 0.42, 1.1, and 1.3 nM, respectively); a1- and a2-adrenergic receptors (Ki = 1.2 and 1.2 nM, respectively); and histamine H1 receptors (Ki = 1.0 nM), and moderate affinity for H2 receptors (Ki = 6.2 nM). In in vitro assays, asenapine acts as an antagonist at these receptors. Asenapine has no appreciable affinity for muscarinic cholinergic receptors (e.g., Ki = 8128 nM for M1). Despite its potent binding affinity for multiple receptors, the efficacy of asenapine in schizophrenia is thought to be primarily mediated through a combination of antagonist activity at D2 and 5-HT2A receptors.
The Uses of Asenapine Maleate
Asenapine Maleate is a 5-HT receptor antagonist developed for the treatment of acute schizophrenia and bipolar mania.
Properties of Asenapine Maleate
Melting point: | 141-145° |
Flash point: | 9℃ |
storage temp. | 2-8°C |
solubility | H2O: ≥10mg/mL |
form | powder |
color | white to off-white |
Water Solubility | Water : 6.25 mg/mL (15.55 mM; Need ultrasonic and warming) |
Safety information for Asenapine Maleate
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 Environment GHS09 |
GHS Hazard Statements |
H301:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation H400:Hazardous to the aquatic environment, acute hazard |
Precautionary Statement Codes |
P273:Avoid release to the environment. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Asenapine Maleate
InChIKey | GMDCDXMAFMEDAG-CHHFXETESA-N |
Abamectin manufacturer
Honour Lab Limited
Apothecon Pharmaceuticals Pvt Ltd
Ralington Pharma
BDR Pharmaceuticals International Pvt Ltd
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