Tripelennamine HCl

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Chemical Structure| 154-69-8 同义名 : 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
CAS号 : 154-69-8
货号 : A147384
分子式 : C16H22ClN3
纯度 : 98%
分子量 : 291.82
MDL号 : MFCD00012815
存储条件：

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
生物活性
靶点

  • H1 receptor

    H1 receptor, IC50:30 μM
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].
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
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 <<
实验方案
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
参考文献

[1]Manohar M, Goetz TE, Humphrey S, Depuy T. H1-receptor antagonist, tripelennamine, does not affect arterial hypoxemia in exercising Thoroughbreds. J Appl Physiol (1985). 2002 Apr;92(4):1515-23.

[2]Wasfi IA, Abdel Hadi AA, et al. Comparative disposition of tripelennamine in horses and camels after intravenous administration. J Vet Pharmacol Ther. 2000 Jun;23(3):145-52.

[3]Styczynski PB, Blackmon RC, Groopman JD, Kensler TW. The direct glucuronidation of 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine (PhIP) by human and rabbit liver microsomes. Chem Res Toxicol. 1993 Nov-Dec;6(6):846-51

[4]Oliveto AH, Slifer BL, Dykstra LA. Tripelennamine fails to enhance the morphine-like stimulus effects of pentazocine. Pharmacol Biochem Behav. 1988 Feb;29(2):397-401

[5]Yeh SY. Potentiation of pentazocine antinociception by tripelennamine in the rat. J Pharmacol Exp Ther. 1985 Dec;235(3):683-9

[6]Vaupel DB. Tripelennamine interactions with the psychotomimetic sigma agonist N-allylnormetazocine. Pharmacol Biochem Behav. 1989 Jul;33(3):717-20