TASP0390325 是一种高亲和力的、具有口服活性的精氨酸加压素受体 1B(V1B受体)拮抗剂,具有抗抑郁和抗焦虑活性。
生物活性 | TASP0390325 is a high affinity and orally activeargininevasopressin receptor1B(V1B receptor) antagonist with antidepressant and anxiolytic activities[1]. |
体外研究 (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 IC50value of 2.72 nM[1]. TASP0390325 also inhibits [3H]-AVP binding to rat anterior pituitary membranes, with the IC50value of 2.22 nM[1]. TASP0390325 potently attenuates the 2.5 nM AVP-induced increase in [Ca2+]i, with IC50values of and 20.2 nM[1]. Pretreatment with TASP0390325 inhibits the retention of11C-TASP699 in a dose-dependent manner. Binding of11C-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 IC50value of TASP0390325 is 2.16 nM[2].
|
体内研究 (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. |
|
分子量 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |