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Midaglizole hydrochloride

CAS No. : 79689-25-1

MCE 国际站：Midaglizole hydrochloride

产品活性：Midaglizole hydrochloride (DG5128) 是有效的 α2-肾上腺素受体拮抗剂。Midaglizole hydrochloride (DG5128) 对 α2-肾上腺素能受体的亲和力 (pK_i= 6.28) 比 α1-肾上腺素能受体高 7.4 倍。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Adrenergic Receptor

In Vitro: Midaglizole (DG-5128) at concentrations up to 10 μM inhibits [³H]clonidine binding more effectively than it doed [³H]prazosin binding in rat cerebral cortex membranes. The mode of inhibition is homogeneous and consistent with the law of simple mass action. The EC₅₀ values for stimulation of insulin release from rat islets and the MIN6 β-cell line induced by Midaglizole are 200 nM and 24 μM, respectively. The IC₅₀ values for K_ATP current inhibition induced by Midaglizole are 3.8 μM and 4.4 uM for Kir6.2 and Kir6.2/SUR1 , respectively.

In Vivo: Midaglizole (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats.

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