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TASP0390325
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TASP0390325图片
CAS NO:1642187-96-9
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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

554.44

Formula

C25H30Cl2FN5O4

CAS 号

1642187-96-9

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.