Home Neuronal Signaling 5-HT Receptor antagonist - Adrenergic Receptor antagonist Asenapine maleate For research use only.

Asenapine maleate

Synonyms: Org 5222

Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.

Asenapine maleate Chemical Structure

Asenapine maleate Chemical Structure

CAS No. 85650-56-2

Purity & Quality Control

Asenapine maleate Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

Biological Activity

Description Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
Targets
5-HT2C [1] 5-HT2A [1] 5-HT7 [1] 5-HT2B [1] 5-HT6 [1] Click to View More Targets
10.46(pKi) 10.15(pKi) 9.94(pKi) 9.75(pKi) 9.6(pKi)
In vitro
In vitro 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.[1]
In Vivo
In vivo 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.[1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01968161 Unknown status
Schizophrenia and Disorders With Psychotic Features|Disorders
Centre de Recherche de l''Institut Universitaire en Santé Mentale de Québec
 October 2013 Phase 4
NCT01734278 Completed
Manic Disorder
Professor Saad Shakir|Merck Sharp & Dohme LLC|Drug Safety Research Unit Southampton UK
 October 2012 --
NCT00281320 Completed
Psychosis
Organon and Co
 February 2006 Phase 3

Chemical Information & Solubility

Molecular Weight 401.84 Formula

C17H16ClNO.C4H4O4
CAS No. 85650-56-2 SDF Download Asenapine maleate SDF
Smiles CN1CC2C(C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (199.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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