product name Asenapine maleate
Description: Asenapine maleate, also known as Org 5222 and HSDB 8061, is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors. Asenapine is an atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder. Preliminary data indicate that it has minimal anticholinergic and cardiovascular side effects, as well as minimal weight gain. It was approved by FDA in August 2009.
References: J Psychopharmacol. 2009 Jan;23(1):65-73; Psychopharmacology (Berl). 2008 Feb;196(3):417-29.
401.84
Formula
C17H16ClNO.C4H4O4
CAS No.
85650-56-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 80 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
Org 5222 and HSDB 8061
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397637
| In Vitro |
In vitro activity: Asenapine shows 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]). Asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, alpha2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), alpha2A (7.3), alpha2B (8.3), alpha2C (6.8) and H1 (8.4) receptors. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Psychopharmacol. 2009 Jan;23(1):65-73; Psychopharmacology (Berl). 2008 Feb;196(3):417-29. |
Related Posts
product name Asenapine maleate
Description: Asenapine maleate, also known as Org 5222 and HSDB 8061, is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors. Asenapine is an atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder. Preliminary data indicate that it has minimal anticholinergic and cardiovascular side effects, as well as minimal weight gain. It was approved by FDA in August 2009.
References: J Psychopharmacol. 2009 Jan;23(1):65-73; Psychopharmacology (Berl). 2008 Feb;196(3):417-29.
401.84
Formula
C17H16ClNO.C4H4O4
CAS No.
85650-56-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 80 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
Org 5222 and HSDB 8061
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397637
| In Vitro |
In vitro activity: Asenapine shows 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]). Asenapine has a higher affinity for 5-HT2C, 5-HT2A, 5-HT2B, 5-HT7, 5-HT6, alpha2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pKB) at 5-HT1A (7.4), 5-HT1B (8.1), 5-HT2A (9.0), 5-HT2B (9.3), 5-HT2C (9.0), 5-HT6 (8.0), 5-HT7 (8.5), D2 (9.1), D3 (9.1), alpha2A (7.3), alpha2B (8.3), alpha2C (6.8) and H1 (8.4) receptors. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Psychopharmacol. 2009 Jan;23(1):65-73; Psychopharmacology (Berl). 2008 Feb;196(3):417-29. |