|1-(3,4-二甲氧基苯乙基)-4-(3-苯基丙基)哌嗪|CsnPharm

CAS No.: 165377-43-5

Synonyms: SA4503;AGY 94806;UNII-9J7A4144BX

SA4503 is an agonist of opioid sigma1 receptor (σ1R) with IC50 of 17.4 nM.

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400-920-2911

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描述SA4503 is a potent and selective agonist for the sigma 1 receptor subtype in the brain. SA4503 showed a high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM), while it had about 100-fold less affinity for the sigma 2 receptor subtype labeled by [3H]1,3-di(2-tolyl)guanidine ([3H]DTG) in the presence of 200 nM (+)-pentazocine. SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems^[3]. Treatment with SA4503 (0.1-1 μM) dose-dependently inhibited hypertrophy in cultured cardiomyocytes induced by angiotensin II (Ang II). Chronic SA4503 administration also significantly attenuates myocardial hypertrophy and restores ATP production in transverse aortic constriction mice^[4]. SA4503 administration rescued PO (pressure overload)-induced σ1R decreases in aortic smooth muscle and endothelial cells. SA4503 treatment also rescued PO-induced impairments in ACh- and clonidine-induced vasodilation without affecting PE- and ET-1-induced vasoconstriction^[5]. The administration of SA4503 significantly alters the activity of spontaneously active midbrain DA (dopamine) neurons, particularly those in the VTA (ventral tegmental area) following repeated administration^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00551109	Depressive Disorder, Major	Phase 2	Completed	-	Finland ... more >> Helsinki, Finland Jyväskylä, Finland Kuopio, Finland Tampere, Finland Turku, Finland Collapse <<
NCT00639249	Ischemic Stroke	Phase 2	Completed	-	United Kingdom ... more >> Southern General Hospital Glasgow, United Kingdom Collapse <<

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