Tripelennamine HCl |
Catalog No.GC12061 |
Tripelennamine HCl, un derivado de etilendiamina, es un potente antagonista del receptor H1 de histamina.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 154-69-8
Sample solution is provided at 25 µL, 10mM.
Tripelennamine hydrochloride, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine.IC50 Value:Target: Histamine H1 receptorTripelennamine can be used in the treatment of asthma, hay fever, rhinitus and urticaria.in vitro: Arterial and mixed venous blood-gas and pH measurements were made at rest before and after saline or drug administration and during incremental exercise leading to maximal exertion at 14 m/s on 3.5% uphill grade for 120 s. Galloping at this workload elicited maximal heart rate and induced exercise-induced pulmonary hemorrhage in all horses in both treatments, thereby indicating that capillary stress failure-related pulmonary injury had occurred [1].in vivo: The data obtained (median and range in brackets) in camels and horses, respectively, were as follows: the terminal elimination half-lives were 2.39 (1.91-6.54) and 2.08 (1.31-5.65) h, total body clearances were 0.97 (0.82-1.42) and 0.84 (0.64-1.17)L/h/kg. The volumes of distribution at steady state were 2.87 (1.59-6.67) and 1.69 (1.18-3.50) L/kg, the volumes of the central compartment of the two compartment pharmacokinetic model were 1.75 (0.68-2.27) and 1.06 (0.91-2.20) L/kg [2]. After intramuscular administration of 50 or 100 mg tripelennamine, mean plasma concentrations at 30 minutes were 105 and 194 ng/ml, respectively, and mean plasma t1/2 values were 2.9 and 4.4 hours, respectively [3].
References:
[1]. Manohar M, Goetz TE, Humphrey S, H1-receptor antagonist, tripelennamine, does not affect arterial hypoxemia in exercising Thoroughbreds. J Appl Physiol. 2002 Apr;92(4):1515-23.
[2]. Wasfi IA, Abdel Hadi AA, Elghazali M, Comparative disposition of tripelennamine in horses and camels after intravenous administration. J Vet Pharmacol Ther. 2000 Jun;23(3):145-52.
[3]. Yeh SY, Todd GD, Johnson RE, The pharmacokinetics of pentazocine and tripelennamine. Clin Pharmacol Ther. 1986 Jun;39(6):669-76.
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