85650-56-2
Asenapine Maleate
CAS: 85650-56-2
Molecular Formula: C21H20ClNO5
85650-56-2 - Names and Identifiers
| Name | Asenapine Maleate |
| Synonyms | Org 5222 Org5222 Maleate Unii-cu9463U2E2 Org 5222 Maleate Einecs 288-064-8 Asenapine maleate Asenapine Maleate |
| CAS | 85650-56-2 |
| EINECS | 288-064-8 |
| InChIKey | GMDCDXMAFMEDAG-CHHFXETESA-N |
85650-56-2 - Physico-chemical Properties
| Molecular Formula | C21H20ClNO5 |
| Molar Mass | 401.84 |
| Melting Point | 141-145° |
| Flash Point | 9℃ |
| Water Solubility | H2O: ≥10mg/mL |
| Solubility | H2O: ≥10mg/mL |
| Appearance | Morphological powder color white to off-white |
| Color | white to off-white |
| pKa | pK1 <3, pK2 7.52, pK3 8.51(at 25℃) |
| Storage Condition | 2-8°C |
| Use | Acenapine maleate is a drug suitable for the treatment of schizophrenia, suitable for the acute treatment of bipolar disorder type I mania or mixed episodes. |
| In vitro study | Asenapine shows high affinity and differential rank order (pKi) for serotonin receptor binding affinity (5-HT1A[8.6],5-HT1B[8.4],5-HT 2A[10.2],5-HT 2B[9.8],5-HT 2C[10.5],5-HT5[8.8],5-HT 6[9.6] and 5-HT 7[9.9]), adrenergic receptor (α1[8.9],alpha2A[8.9],alpha2B[9.5] and alpha2C[8.9]), dopamine receptors (D1[8.9],D2[8.9],D3 [9.4] and D4[9.0]) and histamine receptors (H1 [9.0] and H2[8.2]). Asenapine has higher affinity with 5-HT 2C,5-HT 2A,5-HT 2B,5-HT 7,5-HT 6,alpha2B and D3 receptors, indicating that these target molecules are involved in therapy. Asenapine appears to be a potent antagonist (pKB),5-HT 1A(7.4),5-HT1B(8.1),5-HT 2A(9.0),5-HT 2B(9.3),5-HT 2C(9.0),5-HT 6(8.0 ),5-HT 7(8.5),D 2(9.1),D3(9.1),alpha2A(7.3),alpha2B(8.3),alpha2C(6.8) and H 1 receptor (8.4). |
| In vivo study | In free-moving rats, Asenapine(0.05-0.2 mg/kg, S.C.) induced dose-dependent CAR inhibition (no escape failure recording) and did not induce catalepsy. In rats, Asenapine(0.05-0.2 mg/kg, S.C.) simultaneously increased dopamine efflux in the medial prefrontal cortex (mPFC) and nucleus accumbens. Asenapine(0.01 mg/kg, iv) increased dopamine efflux preferentially compared to volt-septum core, whereas at higher doses (0.05 mg/kg, I. v.), the difference disappeared. In pyramidal cells of the medial prefrontal cortex, Asenapine significantly enhanced NMDA-induced responses. |
85650-56-2 - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. R50/53 - Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. R39/23/24/25 - R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S60 - This material and its container must be disposed of as hazardous waste. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. |
| UN IDs | UN1230 - class 3 - PG 2 - Methanol, solution |
| WGK Germany | 3 |
| HS Code | 29339900 |
85650-56-2 - Upstream Downstream Industry
| Downstream Products | Asenapine |
85650-56-2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.489 ml | 12.443 ml | 24.886 ml |
| 5 mM | 0.498 ml | 2.489 ml | 4.977 ml |
| 10 mM | 0.249 ml | 1.244 ml | 2.489 ml |
| 5 mM | 0.05 ml | 0.249 ml | 0.498 ml |
Last Update：2024-01-02 23:10:35
85650-56-2 - Biological activity
Asenapine maleate (Org 5222) is a high-affinity antagonist of multiple receptors including serotonin, norepinephrine, dopamine and histamine receptors, used to treat schizophrenia and depressive manic depression.
Last Update：2024-04-09 20:52:54
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View History
85650-56-2
aldol
Ammonium chromate
hydroxyzine hydrochloride
939986-40-0
EA
usafa-18103
Acetic acid, phenoxy-, methyl ester
1-Pentene
33151-94-9
aldol
Ammonium chromate
hydroxyzine hydrochloride
939986-40-0
EA
usafa-18103
Acetic acid, phenoxy-, methyl ester
1-Pentene
33151-94-9
Downstream Products for 85650-56-2