货号:A147384
同义名:
去敏灵;盐酸曲吡那敏
/ Pyribenzamine HCl; Tripelennamine hydrochloride
Tripelennamine HCl 是H1受体拮抗剂,作为一种精神活性化合物,具有抗瘙痒作用。


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| 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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Tripelennamine (Hydrochloride) is a widely used H1 antagonist, inhibiting PhIP (glucuronidation of 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine) glucuronidation with IC50 of 30 μM[3]. Tripelennamine (0.3-10.0 mg/kg) produced only saline-appropriate responding and dose-related decreases in response rates. Tripelennamine does not enhance the morphine-like discriminative stimulus properties of pentazocine in the pigeon, as it does in the rat[4]. Tripelennamine (10 and 20 mg/kg i.p.) showed some antinociceptive activity, which was not antagonized by naloxone. Pentazocine antinociception was potentiated by simultaneous administration of a large dose (20 mg/kg) but not a small dose (5 mg/kg) of tripelennamine. The effect of tripelennamine on pentazocine antinociception is additive; very little was through a mechanism of inhibition of pentazocine metabolism[5]. Tripelennamine (1.25 mg/kg, IV) produced antinociception, mydriasis and tachycardia without affecting behavior[6]. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00316381 | Myocardial Infarction | Not Applicable | Completed | - | Poland ... 展开 >> III Division of Cardiology Silesian School of Medicine Katowice, Poland, 40-653 Jagiellonian University Institute of Cardiology Krakow, Poland, 31-202 Poznan University of Medical Sciences II Clinic of Cardiology Poznan, Poland, 61-701 National Institute of Cardiology Warszawa, Poland, 04-628 收起 << |
| NCT01861548 | - | Completed | - | Poland ... 展开 >> Nofer Institute of Occupational Medicine, Department of Environmental Epidemiology Lodz, Poland, 91-348 Department of Pediatrics and Allergy, Medical University of Lodz, N. Copernicus Hospital, Lodz, Poland Lodz, Poland, 93-513 收起 << | |
| NCT00620217 | Coronary Artery Disease | Phase 2 | Completed | - | Poland ... 展开 >> Institute of Cardiology Warsaw, Poland, 04-628 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.43mL 0.69mL 0.34mL |
17.13mL 3.43mL 1.71mL |
34.27mL 6.85mL 3.43mL |
|
| CAS号 | 154-69-8 |
| 分子式 | C16H22ClN3 |
| 分子量 | 291.82 |
| SMILES Code | CN(C)CCN(CC1=CC=CC=C1)C2=NC=CC=C2.[H]Cl |
| MDL No. | MFCD00012815 |
| 别名 | 去敏灵;盐酸曲吡那敏;扑敏宁;盐酸吡甲胺;盐酸吡苯胺 ;Pyribenzamine HCl; Tripelennamine hydrochloride |
| 运输 | 蓝冰 |
| InChI Key | FSSICIQKZGUEAE-UHFFFAOYSA-N |
| Pubchem ID | 9066 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, room temperature |
| 溶解方案 |
DMSO: 25 mg/mL(85.67 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 H2O: 100 mg/mL(342.68 mM),配合低频超声助溶 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
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