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Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.721483-46-5
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $168 | In Stock | |
50 mg | $247 | In Stock | |
100 mg | $365 | In Stock | |
1 mL x 10 mM (in DMSO) | $80 | In Stock |
Description | Asenapine (Org 5222) is a 5-HT receptor, adrenergic receptor, dopamine receptor, and histamine receptor antagonist with antipsychotic effects that is used to treat schizophrenia and manic or mixed episodes associated with bipolar 1 disorder.721483-46-5 |
Targets&IC50 | 5-HT1A receptor:8.6 (pKi), 5-HT2A receptor:10.2 (pKi), 5-HT1B receptor:8.4 (pKi), 5-HT2B receptor:9.8 (pKi) |
In vitro | In comparison with the antipsychotics, asenapine showed high affinity and a different rank order of binding affinities (pKi) for serotonin receptors (5-HT1A [8.6], 5-HT1B [8.4], 5-HT2A [10.2], 5-HT2B [9.8], 5-HT2C [10.5], 5-HT5 [8.8], 5-HT6 [9.6] and 5-HT7 [9.9]), adrenoceptors (alpha1 [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])[2]. |
In vivo | Asenapine (0.05-0.2 mg/kg, s.c.) induced a dose-dependent suppression of CAR (no escape failures recorded) and did not induce catalepsy. Additionally, it increased dopamine efflux in both the medial prefrontal cortex (mPFC) and the nucleus accumbens (NAc)[2]. |
Alias | Org 5222, ME2136, HSDB 8061 |
Molecular Weight | 285.77 |
Formula | C17H16ClNO |
Cas No. | 65576-45-6 |
Smiles | [H][C@@]12CN(C)C[C@@]1([H])c1cc(Cl)ccc1Oc1ccccc21 |
Relative Density. | 1.231 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: Insoluble DMSO: 80 mg/mL (279.94 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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