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TASP0390325

CAS No. : 1642187-96-9

MCE 站：TASP0390325

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：Vasopressin Receptor

In Vitro: 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.

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.
Oral administration of TASP0390325 also exerts antidepressant effects in two models of depression (a forced swimming test ａnd an olfactory bulbectomy model).

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