Blonanserin - CAS 132810-10-7
Catalog number: 132810-10-7
Category: Inhibitor
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Molecular Formula:
C23H30FN3
Molecular Weight:
367.512
COA:
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Targets:
Dopamine Receptor
Description:
A 5-HT2 serotonin receptor and D2 dopamine receptor antagonist, used as an antipsychotic.
Purity:
0.99
Appearance:
white to off-white solid
Synonyms:
2-(4-ethylpiperazin-1-yl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
MSDS:
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InChIKey:
XVGOZDAJGBALKS-UHFFFAOYSA-N
InChI:
InChI=1S/C23H30FN3/c1-2-26-13-15-27(16-14-26)23-17-21(18-9-11-19(24)12-10-18)20-7-5-3-4-6-8-22(20)25-23/h9-12,17H,2-8,13-16H2,1H3
Canonical SMILES:
CCN1CCN(CC1)C2=NC3=C(CCCCCC3)C(=C2)C4=CC=C(C=C4)F
1.Dopamine D3 receptor antagonism contributes to blonanserin-induced cortical dopamine and acetylcholine efflux and cognitive improvement.
Huang M1, Kwon S1, Oyamada Y2, Rajagopal L1, Miyauchi M2, Meltzer HY3. Pharmacol Biochem Behav. 2015 Nov;138:49-57. doi: 10.1016/j.pbb.2015.09.011. Epub 2015 Sep 14.
Blonanserin is a novel atypical antipsychotic drug (APD), which, unlike most atypical APDs, has a slightly higher affinity for dopamine (DA) D2 than serotonin (5-HT)2A receptors, and is an antagonist at both, as well as at D3 receptors. The effects of atypical APDs to enhance rodent cortical, hippocampal, limbic, and dorsal striatal (dSTR) DA and acetylcholine (ACh) release, contribute to their ability to improve novel object recognition (NOR) in rodents treated with sub-chronic (sc) phencyclidine (PCP) and cognitive impairment associated with schizophrenia (CIAS). Here we determined the ability of blonanserin, the D3 antagonist NGB 2904, and the typical APD, haloperidol, a D2 antagonist, to enhance neurotransmitter efflux in the medial prefrontal cortex (mPFC) and dSTR of mice, and to ameliorate the scPCP-induced deficit in NOR in rats. Blonanserin, 10mg/kg, i.p., increased DA, norepinephrine (NE), and ACh efflux in mPFC and dSTR. NGB 2904, 3mg/kg, increased DA and ACh, but not NE, efflux in mPFC, and DA, but not ACh, efflux in dSTR.
2.One-Year Follow-Up of Serum Prolactin Level in Schizophrenia Patients Treated with Blonanserin: A Case Series.
Takahashi S1, Suzuki M1, Uchiyama M1. Psychiatry Investig. 2015 Oct;12(4):566-8. doi: 10.4306/pi.2015.12.4.566. Epub 2015 Sep 30.
In our previous study, a prolactin elevation was more frequently in risperidone than in blonanserin; however, it was more often in blonanserin than in olanzapine. Therefore, while a rate of PRL rising is low to moderate, hyperprolactinemia is a considerable adverse effect in the blonanserin treatment. In this study, to examine detailed characteristics of hyperprolactinemia of blonanserin, we analyzed the prolactin data in six schizophrenic patients who were switched to blonanserin from other antipsychotics and followed for one year. As a result, blonanserin dose was clearly associated with serum prolactin level. The average prolactin level was almost normal when the mean blonanserin dosage was 8.0 mg/day. Regardless of the dose decrease of blonanserin, there were no remarkable changes in symptoms and social functions. Based on our findings, we conclude that low dose blonanserin medication may be useful for schizophrenia maintenance treatment without hyperprolactinemia and a high rate of relapse.
3.The atypical antipsychotic blonanserin reverses (+)-PD-128907- and ketamine-induced deficit in executive function in common marmosets.
Kotani M1, Enomoto T2, Murai T1, Nakako T1, Iwamura Y1, Kiyoshi A1, Matsumoto K1, Matsumoto A1, Ikejiri M1, Nakayama T1, Ogi Y1, Ikeda K3. Behav Brain Res. 2016 May 15;305:212-7. doi: 10.1016/j.bbr.2016.02.031. Epub 2016 Mar 9.
Antagonism of the dopamine D3 receptor is considered a promising strategy for the treatment of cognitive impairment associated with schizophrenia. We have previously reported that the atypical antipsychotic blonanserin, a dopamine D2/D3 and serotonin 5-HT2A receptor antagonist, highly occupies dopamine D3 receptors at its antipsychotic dose range in rats. In the present study, we evaluated the effects of blonanserin on executive function in common marmosets using the object retrieval with detour (ORD) task. The dopamine D3 receptor-preferring agonist (+)-PD-128907 at 1mg/kg decreased success rate in the difficult trial, but not in the easy trial. Since the difference between the two trials is only cognitive demand, our findings indicate that excess activation of dopamine D3 receptors impairs executive function in common marmosets. Blonanserin at 0.1mg/kg reversed the decrease in success rate induced by (+)-PD-128907 in the difficult trial.
4.Clinical Assessment of Weight Gain with Atypical Antipsychotics - Blonanserin vs Amisulpride.
Deepak TS1, Raveesh BN2, Parashivamurthy BM3, Kumar MN4, Majgi SM5, Nagesh HN6. J Clin Diagn Res. 2015 Jun;9(6):FC07-10. doi: 10.7860/JCDR/2015/13007.6066. Epub 2015 Jun 1.
BACKGROUND: Atypical antipsychotics appear to have the greatest potential to induce weight gain. Antipsychotic-induced weight gain is the one of main cause of non-compliance and discontinuation of treatment, often resulting in the relapse of psychosis.
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CAS 132810-10-7 Blonanserin

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