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Blonanserin

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Chemical Structure| 132810-10-7 同义名 : AD-5423;Lonasen
CAS号 : 132810-10-7
货号 : A461493
分子式 : C23H30FN3
纯度 : 98% HPLC
分子量 : 367.503
MDL号 : MFCD00893838
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(10.88 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • 5-HT2

    5-HT2, Ki:3.98 nM
描述 Blonanserin is an atypical antipsychotic drug (APD) which, compared to other atypical APDs, is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist. Blonanserin, 1mg/kg, but not 0.3mg/kg, improved the PCP-induced NOR (novel object recognition) deficit[3]. Blonanserin (oral gavage; 1 mg/kg; 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[4]. Blonanserin transdermal patch improved the symptoms of acute schizophrenia with acceptable tolerability[5]. Given the higher affinity of blonanserin at dopamine D3 receptors than haloperidol, antagonism of blonanserin at dopamine D3 receptors may play a role in lack of dopamine supersensitivity after chronic administration[6]. Blonanserin ameliorates the methamphetamine-induced disruption of LI, as other antipsychotics do, and a neuronal activation and/or modulation of neurotransmission in the nucleus accumbens is related to the disruption of LI by methamphetamine and to its amelioration by blonanserin[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01516424 Schizophrenia Phase 3 Completed - China, Beijing ... 展开 >> Beijing Anding Hospital Beijing, Beijing, China, 100088 Beijing Huilongguan Hospital Beijing, Beijing, China, 100096 Peking University Sixth Hospital Beijing, Beijing, China, 100191 China, Guangdong Guangzhou Brain Hospital Guangzhou, Guangdong, China, 510170 China, Hebei Hebei Province Mental Health Center Baoding, Hebei, China, 071000 China, Heilongjiang The First Affiliated Hospital of Harbin Medical University Harbin, Heilongjiang, China, 150001 China, Henan Henan Provincial Mental Hospital Xinxiang, Henan, China, 453002 China, Hunan The Second Xiangya Hospital of Central South University Changsha, Hunan, China, 410000 Hunan Province Brain Hospital Changsha, Hunan, China, 410007 China, Jiangsu Nanjing Brain Hospital Nanjing, Jiangsu, China, 210029 Wuxi Mental Health Center Wuxi, Jiangsu, China, 214000 China, Shanghai Shanghai Mental Health Center Shang Hai, Shanghai, China, 200030 China, Shanxi Xi'an Mental Health Center Xi'an, Shanxi, China, 710061 China, Sichuan West China Hospital, Sichuan University Chengdu, Sichuan, China, 610041 China, Tianjin Tianjin Anding Hospital Tianjin, Tianjin, China, 300222 China, Yunnan First Affiliated Hospital of Kunming Medical University Kun Ming, Yunnan, China, 650032 收起 <<
NCT01516424 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.61mL

2.72mL

1.36mL

27.21mL

5.44mL

2.72mL
参考文献

[1]Huang M, Panos JJ, et al. Comparative effect of lurasidone and blonanserin on cortical glutamate, dopamine, and acetylcholine efflux: role of relative serotonin (5-HT)2A and DA D2 antagonism and 5-HT1A partial agonism. J Neurochem. 2014 Mar;128(6):938-49.

[2]Ohoyama K, Yamamura S, et al. Effect of novel atypical antipsychotic, blonanserin, on extracellular neurotransmitter level in rat prefrontal cortex. Eur J Pharmacol. 2011 Feb 25;653(1-3):47-57.

[3]Horiguchi M, Meltzer HY. Blonanserin reverses the phencyclidine (PCP)-induced impairment in novel object recognition (NOR) in rats: role of indirect 5-HT(1A) partial agonism. Behav Brain Res. 2013 Jun 15;247:158-64

[4]Takeuchi S, Hida H, Uchida M, Naruse R, Yoshimi A, Kitagaki S, Ozaki N, Noda Y. Blonanserin ameliorates social deficit through dopamine-D3 receptor antagonism in mice administered phencyclidine as an animal model of schizophrenia. Neurochem Int. 2019 Sep;128:127-134

[5]Iwata N, Ishigooka J, Kim WH, Yoon BH, Lin SK, Sulaiman AH, Cosca R, Wang L, Suchkov Y, Agarkov A, Watabe K, Matsui T, Sato T, Inoue Y, Higuchi T, Correll CU, Kane JM. Efficacy and safety of blonanserin transdermal patch in patients with schizophrenia: A 6-week randomized, double-blind, placebo-controlled, multicenter study. Schizophr Res. 2020 Jan;215:408-415

[6]Hashimoto T, Baba S, Ikeda H, Oda Y, Hashimoto K, Shimizu I. Lack of dopamine supersensitivity in rats after chronic administration of blonanserin: Comparison with haloperidol. Eur J Pharmacol. 2018 Jul 5;830:26-32

[7]Kuramashi A, Abe H, Koganemaru G, Matsuo H, Ikeda T, Ebihara K, Funahashi H, Takeda R, Nishimori T, Ishida Y. Effect of blonanserin on methamphetamine-induced disruption of latent inhibition and c-Fos expression in rats. Neurosci Lett. 2013 Aug 9;549:97-102