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Submit ReviewAsenapine maleate
Description: Non-selective 5-HT, dopamine, adrenalin and histamine receptor antagonist; antipsychotic agent
Chemical Name: (3aR*,12bR*)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole maleate
Purity: ≥98% (HPLC)
Biological Activity for Asenapine maleate
Asenapine maleate is a novel psychopharmacologic agent. Displays antagonist activity at 5-HT, dopamine, noradrenalin and histamine receptor subtypes (pKi values are 8.60, 8.40, 10.15, 9.75, 10.46, 8.84, 9.60, 9.94, 8.85, 8.90, 8.84, 9.38, 8.95, 8.93, 8.9, 9.49, 8.91, 9.00 and 8.21 for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, 5-HT7, D1, D2L, D2S, D3, D4, α1A, α2A, α2B, α2C, H1 and H2 receptors respectively). Displays no appreciable affinity for muscarinic receptors. Exhibits potent activity in animal models predictive of antipsychotic efficacy.
Compound Libraries for Asenapine maleate
Asenapine maleate is also offered as part of the Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Asenapine maleate
| M. Wt | 401.84 |
| Formula | C17H16ClNO.C4H4O4 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 85650-56-2 |
| PubChem ID | 73416848 |
| InChI Key | QGBIWSABMNWWNB-FGYPTBLJSA-N |
| Smiles | CN2C[C@]1([H])C3=C(C=CC=C3)OC4=C(C=C(Cl)C=C4)[C@]([H])1C2.CN6C[C@@]5([H])C7=C(C=CC=C7)OC8=C(C=C(Cl)C=C8)[C@@]([H])5C6 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Asenapine maleate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.18 | 100 | |
| ethanol | 20.09 | 50 |
Preparing Stock Solutions for Asenapine maleate
The following data is based on the product molecular weight 401.84. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.49 mL | 12.44 mL | 24.89 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.98 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.49 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets for Asenapine maleate
References for Asenapine maleate
References are publications that support the biological activity of the product.
Shahid et al (2009) Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J.Psychopharmacol. 23 65 PMID: 18308814
Meltzer et al (2009) Asenapine. Nat.Rev.Drug Discov. 8 843 PMID: 19876039
Marston et al (2009) Asenapine effects in animal models of psychosis and cognitive function. Psychopharmacol. 206 699 PMID: 19462162
If you know of a relevant reference for Asenapine maleate, please let us know.
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Keywords: Asenapine maleate, Asenapine maleate supplier, antipsychotics, 5-HT, serotonin, receptors, dopamine, alpha-adrenoceptors, a-adrenoceptors, α-adrenoceptors, a-adrenergic, alpha-adrenergic, α-adrenergic, antagonists, Non-selective, Dopamine, Adrenergic, Alpha, Receptors, 3737, Tocris Bioscience
1 Citation for Asenapine maleate
Citations are publications that use Tocris products. Selected citations for Asenapine maleate include:
Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.