产品
编 号：F310447
分子式：C19H22ClNO2
分子量：331.84
分子式：C19H22ClNO2
分子量：331.84
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CAS No: 30007-39-7
产品详情
生物活性：
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively.
体外研究：
BE2254 inhibits (-)-noradrenaline-mediated increases in gluconeogenesis with K,sub>B of 0.74 nM.The alpha-1 selective antagonist [125I]BE2254 is used to specifically label a single class of binding sites with a dissociation constant of 131.0 pM and a maximal binding capacity of 17.6 fmol/mg of protein. Catecholamines compete for [125I]BE2254 binding stereospecifically and with the characteristic alpha adrenergic potency series of (-)-epinephrine greater than (-)-norepinephrine much greater than (-)-isoproterenol. The alpha-1 selective antagonist prazosin (Kd=2.4 nM) is much more potent in competing for [125I]BE2254 binding than is the alpha-2 selective antagonist yohimbine (Kd=2900 nM).
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively.
体外研究：
BE2254 inhibits (-)-noradrenaline-mediated increases in gluconeogenesis with K,sub>B of 0.74 nM.The alpha-1 selective antagonist [125I]BE2254 is used to specifically label a single class of binding sites with a dissociation constant of 131.0 pM and a maximal binding capacity of 17.6 fmol/mg of protein. Catecholamines compete for [125I]BE2254 binding stereospecifically and with the characteristic alpha adrenergic potency series of (-)-epinephrine greater than (-)-norepinephrine much greater than (-)-isoproterenol. The alpha-1 selective antagonist prazosin (Kd=2.4 nM) is much more potent in competing for [125I]BE2254 binding than is the alpha-2 selective antagonist yohimbine (Kd=2900 nM).
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