產(chǎn)品目錄

規(guī)格	50mg 200mg
CAS	21102-95-4
別名
化學名	8-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-8-azaspiro[4.5]decane-7,9-dione;dihydrochloride
分子式	C22H31N3O3.2HCl
分子量	458.42
溶解度	DMF: 10 mg/ml,DMSO: 25 mg/ml,Ethanol: 0.2 mg/ml,PBS (pH 7.2): 0.5 mg/ml
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：

BMY 7378 is a α2C and α1D adrenergic receptors inhibitor (pKi= 6.54 and 8.2, respectively) and a mixed agonist and antagonist for 5-HT1A receptors.

Adrenergic α1 and α2 receptors are G protein-coupled receptors that are located in CNS and periphery. It plays a role in regulating neurotransmission, smooth muscle contraction and thermogegualtion. 5-HT receptor is a G-protein coupled receptor for 5-hydroxytryptamine (serotonin) that found in nerve systems. It also functions as receptor for various alkaloids and psychoactive substances.

BMY 7378 blocks the inhibition on forskolin-stimulated adenylate cyclase activity in rat hippocampus induced by the 5-HT1A agonist, 8-OHh-DPAT. [1] In rat spinal cord, BMY 7378 is a weak partial agonist at the hippocampal 5-HT1A receptors. [2] BMY 7378 is also the first α1D adrenergic receptors subtype selective ligand that has high affinity and had a clear pharmacological distinction between the α1B and α1D adrenergic receptors subtypes. [3] In ligand-binding assay, BMY 7378 displays a 10-fold selectivity for α2C adrenergic receptors over other α2 adrenergic receptors. [4]

BMY 7378 not only shows 5-HT1A antagonist activity in the rat behavioral experiments, but also exerts a marked decrease of 5-HT release in ventral hippocampus of the anaesthetized rat in a dose-dependent manner (0.01-1.0 mg/kg s.c.) [5]

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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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