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/ Cyproheptadine HCl/盐酸赛庚啶

Cyproheptadine HCl/盐酸赛庚啶 {[allProObj[0].p_purity_real_show]}

货号：A359851 同义名： Cyproheptadine HCl; Periactin

Cyproheptadine hydrochloride是一种口服活性 5-HT2A 受体拮抗剂，IC50 为 0.6 nM，具有抗抑郁和抗血清素作用，并能抑制血清素增强的血小板功能，适用于血栓栓塞性疾病研究。

Cyproheptadine HCl/盐酸赛庚啶 化学结构 CAS号：969-33-5
Cyproheptadine HCl/盐酸赛庚啶 化学结构
CAS号：969-33-5
Cyproheptadine HCl/盐酸赛庚啶 3D分子结构
CAS号：969-33-5
Cyproheptadine HCl/盐酸赛庚啶 化学结构 CAS号：969-33-5
Cyproheptadine HCl/盐酸赛庚啶 3D分子结构 CAS号：969-33-5
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Cyproheptadine HCl/盐酸赛庚啶 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]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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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 (rat brain synaptosomes), IC50: 474 μM

5-HT (human platelets), IC50: 240 μM

 		98%
Venlafaxine ✔ 99%
Fluvoxamine maleate ✔ 99%
Iloperidone ✔ 99%
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 ✔ 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

 		98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

 		98%
Latrepirdine 2HCl ✔ GluR 99%
Fluoxetine HCl ✔ 99.5%
Paroxetine HCl ✔ AChR 99%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

 		+

5-HT2, pIC50: 5.5

 		97%
Flibanserin +++

5-HT1A, Ki: 1 nM

 		+

5-HT2A, Ki: 49 nM

 		95%
LY310762 +

5-HT1D, Ki: 249 nM

 		99%+
Cyclobenzaprine HCI ✔ 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

 		99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

 		99+%
Olanzapine ✔ 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

 		99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

 		99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

 		98%
Agomelatine ✔ 98%
Clozapine ✔ 98%
Amitriptyline +

5-HT2, Ki: 235 nM

 		SERT 99%
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%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

 		98%
Ondansetron ✔ 99%
Granisetron ✔ 98%
Alosetron HCl ✔ 98%
Ondansetron HCl dihydrate ✔ 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

 		99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

 		99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

 		++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

 		+++

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

 		95%
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 2HCl ✔ 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 ✔ 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		99%
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

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine HCl ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin HCl ✔ 99+%
Buclizine 2HCl ✔ 95%
Latrepirdine 2HCl ✔ GluR 99%
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 HCl/盐酸赛庚啶 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 HCl/盐酸赛庚啶 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Nialamide-treated mice Subcutaneous injection 0.1mg/kg Single dose, 90 minutes before Prevention of 5-HTP-induced hypoglycemia and head-twitching response Br J Pharmacol. 1974 Apr;50(4):575-80
Male ddY mice Mouse ear oedema model Oral 20 mg/kg Single administration Cyproheptadine significantly inhibited the ear oedema induced by neuropeptides such as SP, CGRP, NKA, and VIP. Br J Pharmacol. 1993 Dec;110(4):1614-20
Mice Mouse paw oedema model Intraperitoneal injection 5 mg/kg Single dose, 30 minutes before To evaluate the involvement of histamine/5-HT in H2S-induced oedema, results showed CPR did not affect NaHS or L-cysteine-induced oedema Br J Pharmacol. 2010 Dec;161(8):1835-42
Mice Mouse behavioral activity model Intraperitoneal injection 10 mg/kg Single dose, observed for 2 hours To study the effect of cyproheptadine on DMT-induced behavioral activity in mice, results showed that cyproheptadine enhanced DMT-induced activity. Br J Pharmacol. 1980 May;69(1):69-80
Mice Nitrazepam-induced sleep model Intraperitoneal injection 5-10 mg/kg Single dose To investigate the effect of cyproheptadine on nitrazepam-induced sleep, results showed that cyproheptadine partially antagonized the hypnotic effect of nitrazepam. Br J Pharmacol. 1985 Jan;84(1):185-91
Female MF1 mice Mouse marble-burying behavior model Intraperitoneal injection 2 mg/kg Single dose Cyproheptadine at 2 mg/kg significantly inhibited marble burying without affecting runway activity. Br J Pharmacol. 1991 Sep;104(1):105-12

Cyproheptadine HCl/盐酸赛庚啶 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 HCl/盐酸赛庚啶 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 HCl/盐酸赛庚啶 技术信息

CAS号969-33-5
分子式C21H22ClN
分子量 323.86
SMILES Code CN1CCC(CC1)=C2C3=CC=CC=C3C=CC4=CC=CC=C24.[H]Cl
MDL No. MFCD00012538
别名 Cyproheptadine HCl; Periactin
运输蓝冰
InChI Key ZPMVNZLARAEGHB-UHFFFAOYSA-N
Pubchem ID 13770
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Cyproheptadine hydrochloride | Cyproheptadine HCl;Periactin | 5-HT Receptor | Histamine Receptor | AmBeed-信号通路专用抑制剂 | Cyproheptadine HCl/盐酸赛庚啶 纯度/质量文件 | Cyproheptadine HCl/盐酸赛庚啶 亚型比较 | Cyproheptadine HCl/盐酸赛庚啶 生物活性 | Cyproheptadine HCl/盐酸赛庚啶 参考文献 | Cyproheptadine HCl/盐酸赛庚啶 实验方案 | Cyproheptadine HCl/盐酸赛庚啶 技术信息

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