TASP 0390325 is a potent and orally active, selective V1B receptor antagonist (IC50 = 2.22 nM for rat pituitary receptors). In the range of 10 μM, there was no significant affinity for the other 85 receptors, ion channels and transporters, including V1A and V2. ACTH level was increased by TASP 0390325 in rats. TASP 0390325 is an antidepressant and anti-anxiety compound.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague-Dawley (SD) rats |
| Formulation | suspended in 0.5% methylcellulose 400 |
| Dosages | 0.3 and 1 mg/kg |
| Administration | Oral administration |
| Molecular Weight | 554.44 |
| Formula | C25H29ClFN5O4.HCl |
| CAS Number | 1642187-96-9 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| Big Endothelin-1 (1-38), human
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| (d(CH2)51, Tyr(Me)2, Arg8)-Vasopressin
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Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. |
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