For research use only. Not for therapeutic Use.
TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities[1].
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].
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].
| Catalog Number | I011284 |
| CAS Number | 1642187-96-9 |
| Synonyms | 2-[2-(3-chloro-4-fluorophenyl)-6-(3-morpholin-4-ylpropoxy)-4-oxopyrido[2,3-d]pyrimidin-3-yl]-N-propan-2-ylacetamide;hydrochloride |
| Molecular Formula | C25H30Cl2FN5O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H29ClFN5O4.ClH/c1-16(2)29-22(33)15-32-24(17-4-5-21(27)20(26)12-17)30-23-19(25(32)34)13-18(14-28-23)36-9-3-6-31-7-10-35-11-8-31;/h4-5,12-14,16H,3,6-11,15H2,1-2H3,(H,29,33);1H |
| InChIKey | NUIXGNLBPARAII-UHFFFAOYSA-N |
| SMILES | CC(C)NC(=O)CN1C(=NC2=C(C1=O)C=C(C=N2)OCCCN3CCOCC3)C4=CC(=C(C=C4)F)Cl.Cl |
| Reference | [1]. M Iijima, et al. Antidepressant and anxiolytic profiles of newly synthesized arginine vasopressin V1B receptor antagonists: TASP0233278 and TASP0390325. Br J Pharmacol. 2014 Jul;171(14):3511-25. [2]. Kazumi Koga, et al. High-Contrast PET Imaging of Vasopressin V 1B Receptors with a Novel Radioligand, 11C-TASP699. J Nucl Med. 2017 Oct;58(10):1652-1658. |
