Asenapine Maleate

SKU: orb1306997

Description

Asenapine Maleate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

−

Key Properties

−

CAS Number	85650-56-2
MW	401.84
Purity	99.73%
Formula	C₂₁H₂₀ClNO₅
SMILES	OC(=O)\C=C/C(O)=O.[H][C@@]12CN(C)C[C@@]1([H])c1cc(Cl)ccc1Oc1ccccc21
Target	5-HT Receptor
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.98 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:60 mg/mL (149.31 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

−

Target IC50	sPLA2:2.5 nM (Ki)\|D3 receptor:0.42 nM (Ki)\|D4 Receptor:1.1 nM (Ki)\|5-HT7:9.94(pKi)\|5-HT2A:10.15(pKi)\|5-HT6:9.6(pKi)\|D2 Receptor:1.3 nM (Ki)\|5-HT2C:10.46(pKi)\|5-HT2B:9.75(pKi) Read more...
In Vivo	Asenapine demonstrates a higher affinity for 5-HT 2C, 5-HT 2A, 5-HT 2B, 5-HT 7, 5-HT 6, alpha2B, and D3 receptors compared to its affinity for D2 receptors, indicating a closer interaction with these targets at therapeutic doses. Asenapine is an effective antagonist for a range of receptors, including 5-HT 1A (7.4), 5-HT 1B (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), D2 (9.1), D3 (9.1), alpha2A (7.3), alpha2B (8.3), alpha2C (6.8), and H 1 receptors (8.4), as indicated by their respective pKB values. Read more...
In Vitro	Asenapine (0.01 mg/kg, i.v.) preferentially increased dopamine outflow in the shell compared to the nucleus accumbens (NAc) core, with no difference observed at a higher dosage (0.05 mg/kg, i.v.). Asenapine significantly enhanced the response to NMDA in pyramidal cells within the medial prefrontal cortex. In freely moving rats, Asenapine (0.05-0.2 mg/kg, subcutaneous injection) induced dose-dependent conditioned avoidance response (CAR) inhibition (without recording escape failures) and did not induce cataleptic fainting. Moreover, Asenapine (0.05-0.2 mg/kg, subcutaneous injection) increased dopamine outflow in both the medial prefrontal cortex and the nucleus accumbens in rats. Read more...

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

5-HT2C, 5-HT2A, 5-HT2B, 5-HT Receptor, 5-HT6, 5-HT7, 5HT Receptor, 5-hydroxytryptamine Receptor, 5HTReceptor, Asenapine, Asenapine Maleate, Inhibitor, inhibit, Org 5222, Org 5222 maleate, Org 5222 Maleate, Org5222, Org-5222, Serotonin Receptor

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

6440510 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols