產(chǎn)品目錄

規(guī)格	500 μg 1mg 5mg
CAS	16562-13-3
別名	Stepholidine;(-)-Stepholidine;L-SPD
化學(xué)名	3,9-dimethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[3,2-a]isoquinoline-2,10-diol
分子式	C19H21NO4
分子量	327.37
溶解度	1.1mg/mL in ethanol, 5mg/mL in DMSO, or in DMF
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

(–)-Stepholidine is a dopamine receptor antagonist and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A.[1],[2],[3] (–)-Stepholidine binds to dopamine D1, D2, D3, D4, and D5 receptors (Kis = 5.1, 11.6, 24, 1,450, and 5.8 nM, respectively) as well as 5-HT1A, 5-HT2B, α2C-adrenergic receptors (α2C-ARs), and sigma-2 (σ2) receptors in a radioligand binding assay (Kis = 143, 226, 215, and 53 nM, respectively).[1] It inhibits dopamine-induced cAMP accumulation in HEK293 cells expressing dopamine D1, D2, and D5 receptors with IC50 values of 20.5, 128, and 27 nM, respectively. (–)-Stepholidine inhibits forskolin-induced cAMP production in CHO cells expressing rat 5-HT1A receptors (EC50 = 1.2 μM).[2] In vivo, (–)-stepholidine (1 mg/kg, i.v.) increases dopamine neuron firing rates, the number of spikes in bursts, and the amplitude of slow oscillations by 20, 155, and 126%, respectively, in the rat ventral tegmental area (VTA), effects that can be blocked by the 5-HT1A antagonist WAY-100635. [3] Pretreatment with (–)-stepholidine inhibits amphetamine- and phencyclidine-induced locomotor activity in rats (ED50s = 2.4 and 6.5 mg/kg, respectively).[4]

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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