Tripelennamine citrate
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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- CAS No.: 6138-56-3
- Formule: C22H29N3O7
- Masse moléculaire:447.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Références
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Voir tous les produits spécifiques à Isoform Histamine Receptor
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Activité biologique
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H1 Receptor |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Thoroughbred (3 fillies, 4 geldings, 3-6 yr old, 460 kg)[1]
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Dosage:1.10 mg/kg
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Administration:i.v.; single dose 15 minutes preexercise
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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.
Chemical Information
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CAS No. 6138-56-3
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Masse moléculaire 447.48
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Formule C22H29N3O7
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SMILES
CN(C)CCN(CC1=CC=CC=C1)C2=NC=CC=C2.O=C(CC(C(O)=O)(O)CC(O)=O)O
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tripelennamine citrate Related Classifications
HY-17428B Related Classifications
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