Cyproheptadine hydrochloride | Cyproheptadine HCl;Periactin | 5-HT Receptor | Histamine Receptor

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货号：A359851 同义名： Cyproheptadine HCl;Periactin

Cycloheptadine HCl is a 5-HT2A receptor antagonist which can inhibit serotonin-enhanced platelet function.

Cyproheptadine hydrochloride 化学结构
CAS号：969-33-5

Cyproheptadine hydrochloride 3D分子结构
CAS号：969-33-5

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Cyproheptadine hydrochloride 纯度/质量文件产品仅供科研

货号：A359851 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: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

5-羟色胺受体亚型比较
组胺受体亚型比较

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 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 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, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 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-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 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-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 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	H1 receptor ↓ ↑	H2 receptor ↓ ↑	H3 receptor ↓ ↑	H4 receptor ↓ ↑	Histamine receptor ↓ ↑	其他靶点	纯度
Hydroxyzine 2HCl							99+%
Cyclizine	✔						97%
Loratadine	+ B(0)AT2, IC50: 4 μM						98%
Desloratadine	++ Histamine H1 receptor, IC50: 51 nM						98%
Doxylamine succinate	✔						99%
Ebastine	✔						98%
Tripelennamine HCl	+ H1 receptor, IC50: 30 μM						98%
Meclizine dihydrochloride	✔						98%
Chlorpheniramine maleate	+++ Histamine H1 receptor, IC50: 12 nM						99%
Diphenhydramine HCl	✔						99%
Alcaftadine	++++ H1 receptor, pKi: 8.5	++ H2 receptor, pKi: 7.2					99%+
Fexofenadine HCl	++ Histamine H1 receptor, IC50: 246 nM						99%+
Bilastine	+++ H1 receptor, Ki: 44.15 nM						98%
Pemirolast potassium	✔						98%
Bepotastine besilate	+ Histamine H1 receptor, pIC50: 5.7						98%
Mizolastine	+++ Histamine H1 receptor, IC50: 47 nM						98%
Brompheniramine maleate	✔						98%
Carbinoxamine maleate salt	✔						99+%
Clemastine fumarate	++++ Histamine H1 receptor, IC50: 3 nM						98%
Ketotifen fumarate salt	✔						95%
Rupatadine Fumarate	++ Histamine H1 receptor, Ki: 102 nM					PAFR	98%
Famotidine		✔					97%
Roxatidine Acetate HCl		+ Histamine H2 receptor, IC50: 3.2 μM					98%
Lafutidine		✔					99%
Cimetidine		✔					98%
Nizatidine		++++ Histamine H2 receptor, IC50: 0.9 nM				AChE	98%
Ranitidine		✔					98%
Betahistine			+ Histamine H3 receptor, IC50: 1.9 μM				98%
Ciproxifan maleate			+++ Histamine H3 receptor, IC50: 9.2 nM				99%+
S 38093			++ human H3 receptor, Ki: 1.2 μM rat H3 receptor, Ki: 1.44 μM				98%
JNJ-7777120				++++ Histamine H4 receptor, Ki: 4.5 nM			98%
Azelastine HCl					✔		98%
Epinastine HCl					✔		98%
Levodropropizine					✔		97%
Cyproheptadine hydrochloride					✔		98%
Hesperetin					✔		97%
Olopatadine HCl					✔		98%
Mianserin hydrochloride					✔		99+%
Buclizine 2HCl					✔		97%
Latrepirdine 2HCl					✔	GluR	98%
Cetirizine 2HCl					✔		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。

Cyproheptadine hydrochloride 生物活性

靶点

Histamine receptor

描述

Cyproheptadine Hydrochloride is a serotonin and histamine antagonist approved by the FDA for use in children for allergic rhinitis, allergic conjunctivitis, urticaria, dermatographism and mild angioedema. Cyproheptadine Hydrochloride at a dose of 0.25 mg/kg/day was associated with a statistically significant weight gain in approximately 76% of evaluable patients^[3]. Cyproheptadine (Hydrochloride) do exert antiplatelet and thromboprotective effects as antidepressant 5-HT2A antagonists^[4]. Both the intracellular and extracellular application of cyproheptadine (10 µM) enhance the IK (the delayed rectifier potassium current )^[5].

Cyproheptadine hydrochloride 参考文献

[1]Calka O, Metin A, et al. Effect of cyproheptadine on serum leptin levels. Adv Ther. 2005 Sep-Oct;22(5):424-8.

[2]Honda M, Nishida T, et al. Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003 Jan 1;458(1-2):91-9.

[3]Couluris M, Mayer JL, Freyer DR, Sandler E, Xu P, Krischer JP. The effect of cyproheptadine hydrochloride (periactin) and megestrol acetate (megace) on weight in children with cancer/treatment-related cachexia. J Pediatr Hematol Oncol. 2008 Nov;30(11):791-7. doi: 10.1097/MPH.0b013e3181864a5e. PMID: 18989154; PMCID: PMC2917791.

[4]Lin OA, Karim ZA, Vemana HP, Espinosa EV, Khasawneh FT. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026. doi: 10.1371/journal.pone.0087026. PMID: 24466319; PMCID: PMC3900701.

[5]He YL, Zhang CL, Gao XF, Yao JJ, Hu CL, Mei YA. Cyproheptadine enhances the I(K) of mouse cortical neurons through sigma-1 receptor-mediated intracellular signal pathway. PLoS One. 2012;7(7):e41303. doi: 10.1371/journal.pone.0041303. Epub 2012 Jul 23. PMID: 22844454; PMCID: PMC3402501.

Cyproheptadine hydrochloride 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.09mL

0.62mL

0.31mL

15.44mL

3.09mL

1.54mL

30.88mL

6.18mL

3.09mL

Cyproheptadine hydrochloride 技术信息

CAS号	969-33-5
分子式	C₂₁H₂₂ClN
分子量	323.859

别名	Cyproheptadine HCl;Periactin
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 50 mg/mL(154.39 mM)，配合低频超声助溶，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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