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盐酸HEAT(BE2254)

盐酸HEAT(BE2254)用途

HEAT(BE2254)盐酸盐是一种选择性α1肾上腺素能受体拮抗剂。苯乙胺衍生物盐酸热显示α1a、α1b和α1c的PKI分别为9、9.1和8.57[1][2]。

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盐酸HEAT(BE2254)名称

[ CAS 号 ]:
30007-39-7

[ 中文名 ]:
HETA-盐酸盐

[ 英文名 ]:
HEAT hydrochloride

[英文别名 ]:

HEAT
HEAT hydrochloride
BE-2254 hydrochloride

盐酸HEAT(BE2254)生物活性

[ 描述 ]:

HEAT(BE2254)盐酸盐是一种选择性α1肾上腺素能受体拮抗剂。苯乙胺衍生物盐酸热显示α1a、α1b和α1c的PKI分别为9、9.1和8.57[1][2]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 神经疾病

[体外研究]

BE2254抑制(-)-去甲肾上腺素介导的糖异生增加,K,sub>B为0.74 nM[2]。α-1选择性拮抗剂[125I]BE2254用于特异性标记一类结合位点,其解离常数为131.0μm,最大结合容量为17.6 fmol/mg蛋白质。儿茶酚胺竞争[125I]BE2254立体特异性结合,并具有(-)-肾上腺素大于(-)-去甲肾上腺素远大于(-)-异丙肾上腺素的特征性α肾上腺素能效力系列。α-1选择性拮抗剂哌唑嗪(Kd=2.4nm)在竞争[125I]BE2254结合方面比α-2选择性拮抗剂育亨宾(Kd=2900nm)[3]更有效。

[参考文献]

[1]. Chiu G, et al. Design and synthesis of an alpha1a-adrenergic receptor subtype-selective antagonist from BE2254. Chem Biol Drug Des. 2006;67(6):437-439.

[2]. McPherson GA, et al. A study of alpha 1-adrenoceptors in rat renal cortex: comparison of [3H]-prazosin binding with the alpha 1-adrenoceptor modulating gluconeogenesis under physiological conditions. Br J Pharmacol. 1982;77(1):177-184.

[3]. Tsujimoto G, et al. Alpha adrenergic receptors in the rabbit bladder base smooth muscle: alpha-1 adrenergic receptors mediate contractile responses. J Pharmacol Exp Ther. 1986;236(2):384-389.

盐酸HEAT(BE2254)物理化学性质

[ 沸点 ]:
492.8ºC at 760mmHg

[ 分子式 ]:
C₁₉H₂₂ClNO₂

[ 分子量 ]:
331.83600

[ 闪点 ]:
251.9ºC

[ 精确质量 ]:
331.13400

[ PSA ]:
49.33000

[ LogP ]:
4.16250

盐酸HEAT(BE2254)毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QK4750000

CHEMICAL NAME :: 1(2H)-Naphthalenone, 3,4-dihydro-2-(((2-p-hydroxyphenyl)ethylamino)methyl) -, hydrochloride

CAS REGISTRY NUMBER :: 30007-39-7

LAST UPDATED :: 199706

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C19-H21-N-O2.Cl-H

MOLECULAR WEIGHT :: 331.87

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 650 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 22500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 730 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 33 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 7,231,1982