1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. 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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Tripelennamine citrate

Tripelennamine citrate Chemical Structure

CAS No. : 6138-56-3

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Description

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[1][2][3].

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.
Molecular Weight

447.48

Formula

C22H29N3O7

CAS No.
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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Initial Source
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Room temperature in continental US; may vary elsewhere.

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

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Tripelennamine citrate
Cat. No.:
HY-17428B
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