Blonanserin | AD-5423 | 5-HT2A Antagonist | AmBeed-信号通路专用抑制剂

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布南色林 /Blonanserin {[allProObj[0].p_purity_real_show]}

货号：A461493 同义名： AD-5423;Lonasen

Blonanserin is a D2/5-HT2 receptor antagonist, atypical antipsychotic.

Blonanserin 化学结构
CAS号：132810-10-7

Blonanserin 3D分子结构
CAS号：132810-10-7

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Blonanserin 纯度/质量文件产品仅供科研

货号：A461493 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

5-羟色胺受体亚型比较
多巴胺受体亚型比较

产品名称	5-HT ↓ ↑	5-HT1 ↓ ↑	5-HT2 ↓ ↑	5-HT3 ↓ ↑	5-HT5 ↓ ↑	5-HT6 ↓ ↑	5-HT7 ↓ ↑	其他靶点	纯度
Desvenlafaxine	++ 5-HT, Ki: 40.2 nM								98%
Lamotrigine	+ 5-HT (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 μM								98%
Venlafaxine	✔								98%
Fluvoxamine maleate	✔								99%
Iloperidone	✔								98%
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								97%
Trazodone	✔								98+%
Clomipramine HCl	✔								98%
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								97%
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								98%
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								98%
Latrepirdine 2HCl	✔							GluR	98%
Fluoxetine HCl	✔								99.5%
Paroxetine hydrochloride	✔							AChR	97%
BMY 7378		++ 5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						98%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						98% HPLC
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						99%+
Loxapine succinate			++ 5-HT2 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 nM						99%
Agomelatine			✔						98%
Clozapine			✔						98%
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					98%
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					98%
VUF10166				++++ 5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
Asenapine maleate		+++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		97%
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		98%
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1D, pKi: 6 5-HT1B, pKi: 6.1	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	D1 receptor ↓ ↑	D2 receptor ↓ ↑	D3 receptor ↓ ↑	D4 receptor ↓ ↑	D5 receptor ↓ ↑	DAT ↓ ↑	Dopamine receptor ↓ ↑	其他靶点	纯度
Penfluridol	+ Dopamine receptor, Ki: 1.6 μM								98%
Ansofaxine HCl	++ Dopamine receptor, IC50: 491 nM								98%
Tetrahydroberberine,THB		+ D2 receptor, pKi: 6.08							98+%
Prochlorperazine Maleate		✔							95%
Olanzapine		✔							99+%
Trifluoperazine		++++ Dopamine D2 receptor, IC50: 1.1 nM							98%
Ropinirole hydrochloride		++ D2 receptor, Ki: 29 nM							99%
Lurasidone		++++ D2 receptor, Ki: 1 nM							98%
Levosulpiride		✔							99+%
Pridopidine		✔							95%
Metoclopramide		✔					✔		99+%
Molindone HCl		✔							98%
Sulpiride		✔							99+%
Perospirone		++++ D2 receptor, Ki: 1.4 nM							99%
Perospirone HCl		++++ D2 receptor, Ki: 1.4 nM							98+%
Phenothiazine		✔							98%
Pimozide	+ Dopamine D1 receptor, Ki: 6600 nM	+++ Dopamine D2 receptor, Ki: 3.0 nM	++++ Dopamine D3 receptor, Ki: 0.83 nM						98%
Rotundine	++ D1 receptor, IC50: 166 nM	+ D2 receptor, IC50: 1.47 μM	+ D3 receptor, IC50: 3.25 μM						98%
Domperidone		✔							99+%
ONC206		✔							97%
Pimethixene maleate	++ Dopamine D1 Receptor, pKi: 6.37	+++ Dopamine D2 Receptor, pKi: 8.19		++ Dopamine D4.4 Receptor, pKi: 7.54					97%
Loxapine succinate	++ D1 receptor (human), Ki: 26 nM D2 receptor (Human), Ki: 62 nM	++ D2 receptor (bovine), Ki: 26 nM D2 receptor (human), Ki: 24 nM		+++ D4 receptor (human), Ki: 7.5 nM					99%
Chlorprothixene	+++ D1 receptor, Ki: 18 nM	+++ D2 receptor, Ki: 2.96 nM	+++ D3 receptor, Ki: 4.56 nM		+++ D5 receptor, Ki: 9 nM				98%
SCH-23390 HCl	++++ D1 dopamine receptor, Ki: 0.2 nM				++++ D5 dopamine receptor, Ki: 0.3 nM				98%
MPP+ iodide						✔			97%
σ1 Receptor antagonist-1						+ DAT, pKi: 5.8			97%
Benztropine mesylate						++ DAT, IC50: 118 nM			98%
Azaperone							✔		98%
Ziprasidone HCl							✔		98+%
Paliperidone							✔		98%
Alizapride HCl							✔		99+%
Amisulpride							✔		98%
Quetiapine hemifumarate							✔	Adrenergic Receptor	98%
Clozapine N-oxide							✔		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Blonanserin 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].

Blonanserin 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	-	-

Blonanserin 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

Blonanserin 实验方案

计算器

存储液制备

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

Blonanserin 技术信息

CAS号	132810-10-7
分子式	C₂₃H₃₀FN₃
分子量	367.503

别名	AD-5423;Lonasen
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

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

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Blonanserin 参考文献

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