A77636塩酸塩

A77636塩酸塩 価格

A77636塩酸塩 化学特性,用途語,生産方法

• 説明

  A-77636 is a dopamine D₁ receptor agonist (K_i = 40 nM). It induces activity equal to or greater than dopamine in an adenylate cyclase assay of D₁ receptor activity in fish retina and rat caudate putamen (EC₅₀s = 7.4 and 1.1 nM, respectively) but does not show agonist activity at D₂ receptors expressed in MMQ cells when used at concentrations up to 10 μM. A-77636 (10 μM) induces desensitization of dopamine-stimulated cAMP accumulation and downregulation of D₁ receptors, reducing D₁ receptor expression by 79% in C-6 glioma cells expressing monkey D_1A receptors. In a marmoset model of Parkinson''s disease induced by MPTP, A-77636 (3 μmol/kg, s.c.) increases locomotor activity 5.3-fold and reduces disease severity. Subcutaneous administration of A-77636 elicits cortical acetylcholine release at a dose of 1 μmol/kg. It also elicits over a 230% increase in cortical and hippocampal acetylcholine release when administered at a dose of 4 μmol/kg, an effect that is blocked by the D₁ antagonist SCH 23390 .

• 生物活性

  Potent and selective dopamine D 1 -like receptor agonist (pEC 50 values are 8.97 and < 5 for D 1 -like and D 2 -like receptors respectively). Displays anti-Parkinsonian activity following oral administration in vivo .

A77636塩酸塩 生産企業

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A77636塩酸塩 スペクトルデータ(¹HNMR)

145307-34-2, A77636塩酸塩 キーワード