TASP0390325

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.

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 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.

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GPCR/G Protein

Vasopressin Receptor

Vasopressin Receptor

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1642187-96-9

554.44

C25H30Cl2FN5O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (180.36 mM; 超声助溶 )

Cl.O=C1C2=CC(OCCCN3CCOCC3)=CN=C2N=C(C=4C=CC(F)=C(Cl)C4)N1CC(=O)NC(C)C

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(-20℃)

With Ice Pack

≥ 2 years