product name Tripelennamine HCl
Description: Tripelennamine is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM. Tripelennamine is a substrate for a tertiary amine UDP-glucuronosyltransferases which catalyzes the formation of quaternary ammonium-linked glucuronides. Tripelennamine inhibits the glucuronidation of 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine (PhIP) by a mixture of competitive and noncompetitive inhibition in both human and rabbit liver microsomes.
References: Chem Res Toxicol. 1993 Nov-Dec;6(6):846-51; J Appl Physiol (1985). 2002 Apr;92(4):1515-23.
291.82
Formula
C16H21N3.HCl
CAS No.
154-69-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 2 mg/mL (6.9 mM)
Water: 58 mg/mL (198.75 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
Pyribenzamine HCl
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427774
| In Vitro |
In vitro activity: Tripelennamine is a substrate for a tertiary amine UDP-glucuronosyltransferases which catalyzes the formation of quaternary ammonium-linked glucuronides. Tripelennamine inhibits the glucuronidation of 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine (PhIP) by a mixture of competitive and noncompetitive inhibition in both human and rabbit liver microsomes. Vibrations of the aminopyridine chromophore in Tripelennamine at neutral pH, where the aminoalkyl chain is protonated, are modified when compared to the vibrational pattern recorded for a fully neutral molecule in alkaline solution. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Tripelennamine HCl (i.v.) causes central nervous system (CNS) excitement in standing horses, and the horses became very alert, agitated, and uncomfortable, as indicated by their raising the head and tightening the neck muscles, excessive rapid movements of eyes and ears, biting, snorting, briskly swishing the tail, and stomping and pawing with front feet. Accordingly, hemoglobin concentration of standing horses increase significantly after Tripelennamine HCl treatment. Tripelennamine HCl (i.v.) significantly increases mixed venous blood O2 tension and hemoglobin-O2 saturation in standing horse, as well as arterial and mixed-venous blood O2 contents, but the arterial-to-mixed-venous O2 content gradient of standing horses is not significantly affected. [3] Tripelennamine HCl (0.5 mg/kg i.v.) administrated both in horses and camels results in the terminal elimination half-lives of 2.39 and 2.08 hours, total body clearances of 0.97 and 0.84 L/h/kg. The volumes of distribution at steady state are 2.87 and 1.69 L/kg, the volumes of the central compartment of the two compartment pharmacokinetic model are 1.75 and 1.06 L/kg . |
| Animal model | |
| Formulation & Dosage | |
| References | Chem Res Toxicol. 1993 Nov-Dec;6(6):846-51; J Appl Physiol (1985). 2002 Apr;92(4):1515-23. |
