产品
编 号：F197782
分子式：C25H30Cl2FN5O4
分子量：554.44
分子式：C25H30Cl2FN5O4
分子量：554.44
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1642187-96-9
产品详情
生物活性：
TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.
体内研究：
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.Oral administration of TASP0390325 also exerts antidepressant effects in two models of depression (a forced swimming test and an olfactory bulbectomy model).Animal Model:Male Sprague-Dawley (SD) rats (211-246 g)
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.
体外研究：
TASP0390325 shows a high affinity and potent antagonist activity for V1B receptors. TASP0390325 dose-dependently inhibits [3H]-AVP binding to recombinant human V1B receptors with the IC50 value of 2.72 nM. TASP0390325 also inhibits [3H]-AVP binding to rat anterior pituitary membranes, with the IC50 value of 2.22 nM. TASP0390325 potently attenuates the 2.5 nM AVP-induced increase in [Ca2+]i, with IC50 values of and 20.2 nM.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.
TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.
体内研究：
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.Oral administration of TASP0390325 also exerts antidepressant effects in two models of depression (a forced swimming test and an olfactory bulbectomy model).Animal Model:Male Sprague-Dawley (SD) rats (211-246 g)
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.
体外研究：
TASP0390325 shows a high affinity and potent antagonist activity for V1B receptors. TASP0390325 dose-dependently inhibits [3H]-AVP binding to recombinant human V1B receptors with the IC50 value of 2.72 nM. TASP0390325 also inhibits [3H]-AVP binding to rat anterior pituitary membranes, with the IC50 value of 2.22 nM. TASP0390325 potently attenuates the 2.5 nM AVP-induced increase in [Ca2+]i, with IC50 values of and 20.2 nM.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.
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