1642187-96-9
1642187-96-9 structure
- Name: TASP0390325
- Chemical Name: TASP 0390325
- CAS Number: 1642187-96-9
- Molecular Formula: C25H30Cl2FN5O4
- Molecular Weight: 554.44
- Catalog: Signaling Pathways GPCR/G Protein Vasopressin Receptor
- Create Date: 2022-03-27 08:12:57
- Modify Date: 2024-01-09 19:30:45
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TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities[1].
| Name | TASP 0390325 |
|---|---|
| Synonyms |
2-(3-Chloro-4-fluorophenyl)-N-(1-methylethyl)-6-[3-(4-morpholinyl)propoxy]-4-oxo-pyrido[2,3-d]pyrimidine-3(4H)-acetamide hydrochloride
2-[2-(3-Chloro-4-fluorophenyl)-6-[3-(4-morpholinyl)propoxy]-4-oxopyrido[2,3-d]pyrimidin-3(4H)-yl]-N-isopropylacetamide hydrochloride (1:1) Pyrido[2,3-d]pyrimidine-3(4H)-acetamide, 2-(3-chloro-4-fluorophenyl)-N-(1-methylethyl)-6-[3-(4-morpholinyl)propoxy]-4-oxo-, hydrochloride (1:1) |
| Description | TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities[1]. |
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| Related Catalog | |
| In Vitro | TASP0390325 shows a high affinity and potent antagonist activity for V1B receptors[1]. TASP0390325 dose-dependently inhibits [3H]-AVP binding to recombinant human V1B receptors with the IC50 value of 2.72 nM[1]. TASP0390325 also inhibits [3H]-AVP binding to rat anterior pituitary membranes, with the IC50 value of 2.22 nM[1]. TASP0390325 potently attenuates the 2.5 nM AVP-induced increase in [Ca2+]i, with IC50 values of and 20.2 nM[1]. Pretreatment with TASP0390325 inhibits the retention of 11C-TASP699 in a dose-dependent manner. Binding of 11C-TASP699 to monkey pituitary slices is specifically localized to the anterior lobe. The radioligand binding is inhibited by TASP0390325 in a concentration-dependent manner. The IC50 value of TASP0390325 is 2.16 nM[2]. |
| In Vivo | TASP0390325 blocks the anterior pituitary V1B receptor in vivo. Oral administration of TASP0390325 antagonized the increase in plasma ACTH levels induced by CRF/dDAVP in rats, indicating that TASP0390325 blocks the anterior pituitary V1B receptor in vivo. TASP0390325 (1 mg/kg) significantly antagonizes CRF/dDAVP-induced plasma ACTH in rats[1]. Oral administration of TASP0390325 also exerts antidepressant effects in two models of depression (a forced swimming test and an olfactory bulbectomy model)[1]. Animal Model: Male Sprague-Dawley (SD) rats (211-246 g)[1] Dosage: 0.3 and 1 mg/kg (TASP0390325 is suspended in 0.5% methylcellulose 400) Administration: Oral administration Result: Antagonized the increase in plasma ACTH levels induced by CRF/dDAVP in rats at a dose of 1 mg/kg. In contrast, 0.3 and 1.0 mg/kg itself did not significantly affect basal ACTH levels. |
| References |
| Molecular Formula | C25H30Cl2FN5O4 |
|---|---|
| Molecular Weight | 554.44 |
| Exact Mass | 553.165894 |