Tripelennamine hydrochloride
Based on 1 Customer Validation
Tripelennamine hydrochloride is a histamine H1-receptor antagonist. Tripelennamine hydrochloride effectively reverses histamine-induced bronchoconstriction, increased transpulmonary pressure, elevated pulmonary vascular resistance and reduced dynamic compliance. Tripelennamine hydrochloride does not significantly affect arterial hypoxemia, hemoglobin desaturation and hypercapnia in horses undergoing short-term high-intensity exercise. Tripelennamine hydrochloride exhibits local and central analgesic activity. Tripelennamine hydrochloride can be used in studies related to emphysema, urticaria and acute laminitis.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 154-69-8
- Formula: C16H22ClN3
- Molecular Weight:291.82
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
Tripelennamine (1.0 μg/mL) hydrochloride 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.
| Species | Dose | Route | T1/2α | T1/2β | AUC | CLt | Vss | MRT |
|---|---|---|---|---|---|---|---|---|
| Horse[2] | 0.5 mg/kg | i.v. | 0.42 h | 2.08 h | 597.5 ng·h/mL | 0.84 L/h/kg | 1.69 L/kg | 2.25 h |
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. 154-69-8
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Appearance Solid
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Molecular Weight 291.82
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Formula C16H22ClN3
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Color White to off-white
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SMILES
CN(C)CCN(CC1=CC=CC=C1)C2=NC=CC=C2.[H]Cl
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 100 mg/mL (342.68 mM; Need ultrasonic)
DMSO : 25 mg/mL (85.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.57 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (114.21 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (292 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Manohar M, et al. H1-receptor antagonist, tripelennamine, does not affect arterial hypoxemia in exercising Thoroughbreds. J Appl Physiol (1985). 2002;92(4):1515-1523. [Content Brief]
[2]. Wasfi IA, et al. Comparative disposition of tripelennamine in horses and camels after intravenous administration. J Vet Pharmacol Ther. 2000;23(3):145-152. [Content Brief]
[3]. Yeh SY, et al. The pharmacokinetics of pentazocine and tripelennamine. Clin Pharmacol Ther. 1986 Jun;39(6):669-76. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.4268 mL | 17.1338 mL | 34.2677 mL | 85.6692 mL |
| 5 mM | 0.6854 mL | 3.4268 mL | 6.8535 mL | 17.1338 mL | |
| 10 mM | 0.3427 mL | 1.7134 mL | 3.4268 mL | 8.5669 mL | |
| 15 mM | 0.2285 mL | 1.1423 mL | 2.2845 mL | 5.7113 mL | |
| 20 mM | 0.1713 mL | 0.8567 mL | 1.7134 mL | 4.2835 mL | |
| 25 mM | 0.1371 mL | 0.6854 mL | 1.3707 mL | 3.4268 mL | |
| 30 mM | 0.1142 mL | 0.5711 mL | 1.1423 mL | 2.8556 mL | |
| 40 mM | 0.0857 mL | 0.4283 mL | 0.8567 mL | 2.1417 mL | |
| 50 mM | 0.0685 mL | 0.3427 mL | 0.6854 mL | 1.7134 mL | |
| 60 mM | 0.0571 mL | 0.2856 mL | 0.5711 mL | 1.4278 mL | |
| 80 mM | 0.0428 mL | 0.2142 mL | 0.4283 mL | 1.0709 mL | |
| H2O | 100 mM | 0.0343 mL | 0.1713 mL | 0.3427 mL | 0.8567 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Tripelennamine hydrochloride Related Classifications
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