Home Neuronal Signaling 5-HT Receptor antagonist - Adrenergic Receptor antagonist Asenapine maleate

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Asenapine maleate 5-HT Receptor antagonist

Cat.No.S1283

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 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 401.84

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Chemical Information, Storage & Stability

Molecular Weight 401.84 Formula

C17H16ClNO.C4H4O4

 Storage (From the date of receipt)
CAS No. 85650-56-2 Download SDF Storage of Stock Solutions

Synonyms Org 5222 Smiles CN1CC2C(C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24.C(=CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (199.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
5-HT2C [1]
10.46(pKi)
5-HT2A [1]
10.15(pKi)
5-HT7 [1]
9.94(pKi)
5-HT2B [1]
9.75(pKi)
5-HT6 [1]
9.6(pKi)
α2B-adrenergic receptor [1]
9.49(pKi)
D3 receptor [1]
9.38(pKi)
H1 receptor [1]
9(pKi)
D4 receptor [1]
8.95(pKi)
α1A-adrenergic receptor [1]
8.93(pKi)
α2C-adrenergic receptor [1]
8.91(pKi)
D2L Receptor [1]
8.9(pKi)
α2A-adrenergic receptor [1]
8.9(pKi)
D1 receptor [1]
8.85(pKi)
5-HT5A [1]
8.84(pKi)
D2S Receptor [1]
8.84(pKi)
5-HT1A [1]
8.6(pKi)
5-HT1B [1]
8.4(pKi)
H2 receptor [1]
8.21(pKi)
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
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]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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