Blonanserin dihydrochloride

Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension[1][2].

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 >> Sigma Receptor

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

D2 Receptor:0.142 nM (Ki)

D3 Receptor:0.494 nM (Ki)

D4 Receptor:150 nM (Ki)

D1 Receptor:1070 nM (Ki)

5-HT2A Receptor:0.812 nM (Ki)

5-HT2C Receptor:26.4 nM (Ki)

5-HT6 Receptor:11.7 nM (Ki)

α1-adrenergic receptor:26.7 nM (Ki)

α2-adrenergic receptor:530 nM (Ki)

Blonanserin dihydrochloride exerts some blockade of α1-adrenergic receptors (Ki=26.7 nM) and also shows significant affinity for the D3 receptor (Ki=0.494 nM). Blonanserin dihydrochloride possesses low affinity for the sigma receptor (IC50=286 nM), but lacks significant affinity for numerous other sites including the 5-HT1A, 5-HT3, D1, α2-adrenergic, β-adrenergic, H1, and mACh receptors and the monoamine transporters[1].

Blonanserin dihydrochloride (Oral gavage; 1 mg/kg; once a day for 14 days) significantly ameliorates the social deficit observed in PCP-administered mice and inhibits the decrease in the levels of Ser897-phosphorylation, but preatment with blonanserin does not affect the social behaviors in saline-administered mice[2]. Animal Model: Mice received saline or phencyclidine once a day for 14 consecutive days[2] Dosage: 1 mg/kg Administration: Oral gavage; once a day for 14 days Result: Had an effect on the social deficit in mice that received repeated PCP administration.

[1]. Blonanserin

[2]. Saori Takeuchi, et al. Blonanserin ameliorates social deficit through dopamine-D 3 receptor antagonism in mice administered phencyclidine as an animal model of schizophrenia. Neurochem Int. 2019 Sep;128:127-134.