Asenapine citrate

Names

[ CAS No. ]:
1411867-74-7

[ Name ]:
Asenapine citrate

Biological Activity

[Description]:

Asenapine citrate, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine citrate can be used in the research of schizophrenia and bipolar disorder[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor
Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

5-HT1A Receptor:8.6 (pKi)

5-HT1B Receptor:8.4 (pKi)

5-HT2A Receptor:10.2 (pKi)

5-HT2B Receptor:9.8 (pKi)

5-HT2C Receptor:10.5 (pKi)

5-HT5 Receptor:8.8 (pKi)

5-HT6 Receptor:9.6 (pKi)

5-HT7 Receptor:9.9 (pKi)

α1-adrenergic receptor:8.9 (pKi)

Alpha-2A adrenergic receptor:8.9 (pKi)

Alpha-2B adrenergic receptor:9.5 (pKi)

Alpha-2C adrenergic receptor:8.9 (pKi)

D1 Receptor:8.9 (pKi)

D2 Receptor:8.9 (pKi)

D3 Receptor:9.4 (pKi)

D4 Receptor:9.0 (pKi)

H1 Receptor:9.0 (pKi)

H2 Receptor:8.2 (pKi)


[In Vivo]

Asenapine (0.05-0.2 mg/kg; s.c.) induces a dose-dependent suppression of conditioned avoidance response (CAR) and does not induce catalepsy[2].

[References]

[1]. M Shahid, et al. Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73.

[2]. Olivia Frånberg, et al. Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology (Berl). 2008 Feb;196(3):417-29.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H24ClNO8

[ Molecular Weight ]:
477.89

Related Compounds