Home Neuronal Signaling Histamine Receptor antagonist Tripelennamine HCl

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Tripelennamine HCl Histamine Receptor antagonist

Cat.No.S3146

Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
Tripelennamine HCl Histamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 291.82

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Quality Control

Batch: S314601 Water]58 mg/mL]false]DMSO]2 mg/mL]false]Ethanol]1 mg/mL]false Purity: 99.99%
99.99

Chemical Information, Storage & Stability

Molecular Weight 291.82 Formula

C16H21N3.HCl

 Storage (From the date of receipt)
CAS No. 154-69-8 Download SDF Storage of Stock Solutions

Synonyms Pyribenzamine HCl Smiles CN(C)CCN(CC1=CC=CC=C1)C2=CC=CC=N2.Cl

Solubility

In vitro
Batch:

Water : 58 mg/mL

DMSO : 2 mg/mL (6.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
H1 receptor [1]
30 μM
In vitro
Tripelennamine HCl is a substrate for a tertiary amine UDP-glucuronosyltransferases which catalyzes the formation of quaternary ammonium-linked glucuronides. This compound 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. [1] Vibrations of the aminopyridine chromophore in this chemical 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. [2]
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 this compound treatment. This compound 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] This chemical (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. [4]
References

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