Tripelennamine citrate

Cat. No.: HY-17428B: Fiche technique Instruction de manipulation
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Tripelennamine citrate is a histamine H1-receptor antagonist. Tripelennamine citrate effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine citrate does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine citrate exhibits local and central analgesic activity. Tripelennamine citrate can be used in studies related to emphysema, urticaria and acute laminitis.

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Tripelennamine citrate Chemical Structure

CAS No. : 6138-56-3

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Other In-stock Forms of Tripelennamine citrate:

Tripelennamine hydrochloride

Other Forms of Tripelennamine citrate:

Tripelennamine hydrochloride In-stock
Tripelennamine Obtenir un devis

Recommandations en vedette

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform Histamine Receptor:

Voir toutes les isoformes

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Activité biologique
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Références
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Description

IC₅₀ & Target

H₁ Receptor

In Vitro

Tripelennamine (1.0 μg/mL) citrate exhibits 83.4% protein binding in healthy Arabian camel serum and 73.6% protein binding in healthy horse serum, with no significant difference between the two species^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Single administration of tripelennamine citrate (1.10 mg/kg; i.v.; 15 min prior to exercise) does not significantly alleviate exercise-induced arterial hypoxemia in exercise-trained thoroughbred horses during high-intensity exercise^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Thoroughbred (3 fillies, 4 geldings, 3-6 yr old, 460 kg)^[1]
Dosage:	1.10 mg/kg
Administration:	i.v.; single dose 15 minutes preexercise
Result:	Caused central nervous system excitement, significant tachycardia, systemic and pulmonary hypertension, and raised hemoglobin concentration from 12.7 g/dl to 17.7 g/dl. Increased mixed venous blood O₂ tension and hemoglobin-O₂ saturation, and increased arterial and mixed venous blood O₂ content with no change in arterial-to-mixed venous O₂ content gradient. Increased core temperature during exercise to 41.2°C at 120 seconds of galloping (vs. 40.7°C in controls). Showed no statistically significant differences from controls in exercise-induced arterial hypoxemia (arterial O₂ tension at 120 seconds of galloping: 71.3 Torr vs. 71.3 Torr), arterial hemoglobin-O₂ saturation (80.6% vs. 83.8%), arterial CO₂ tension (60.1 Torr vs. 56.2 Torr), arterial pH (7.040 vs. 7.090), arterial and mixed venous blood O₂ content, arterial-to-mixed venous O₂ content gradient (22.8 mL O₂/dl blood vs. 23.2 mL O₂/dl blood), or O₂ extraction (92.2% vs. 91.5%). Resulted in exercise-induced pulmonary hemorrhage in all treated horses, matching control rates.

Masse moléculaire

447.48

Formule

C₂₂H₂₉N₃O₇

CAS No.

6138-56-3

SMILES

CN(C)CCN(CC1=CC=CC=C1)C2=NC=CC=C2.O=C(CC(C(O)=O)(O)CC(O)=O)O

Structure Classification

Initial Source

Endogenous metabolite

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Manohar M, et al. H1-receptor antagonist, tripelennamine, does not affect arterial hypoxemia in exercising Thoroughbreds. J Appl Physiol. 2002 Apr;92(4):1515-23. [Content Brief]

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

[3]. Yeh SY, et al. The pharmacokinetics of pentazocine and tripelennamine. Clin Pharmacol Ther. 1986 Jun;39(6):669-76. [Content Brief]