1H,12H-Benzo[i]pyrano[3,4-g]indolizin-12-one,2,3,5,6,8,9,10,13-octahydro-2-methoxy-, (2S,13bS)-

用途

二氢-β-红细胞胺是一种竞争性烟碱受体拮抗剂。二氢-β-促红细胞胺阻断尼古丁的辨别刺激特性。二氢-β-促红细胞胺抑制尼古丁诱导的焦虑作用[1][2]。

名称

[ CAS 号 ]:
23255-54-1

[ 英文名 ]:
1H,12H-Benzo[i]pyrano[3,4-g]indolizin-12-one,2,3,5,6,8,9,10,13-octahydro-2-methoxy-, (2S,13bS)-

[英文别名 ]:

dihydro-beta-erythroidine
1-(2,6,6-trimethyl-1-cyclohexen-1-yl)butan-1-one
.β.-Erythroidine, dihydro-
1-(2,6,6-trimethylcyclohex-1-en-1-yl)butan-1-one
1-Butyryl-2,6,6-trimethyl-cyclohexen

生物活性

[ 描述 ]:

二氢-β-红细胞胺是一种竞争性烟碱受体拮抗剂。二氢-β-促红细胞胺阻断尼古丁的辨别刺激特性。二氢-β-促红细胞胺抑制尼古丁诱导的焦虑作用[1][2]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 神经疾病

[体内研究]

二氢-β-促红细胞胺(0.5、1.6、5.0 mg/kg；皮下注射)可阻断大鼠尼古丁的辨别刺激特性[1]。二氢-β-促红细胞胺(100 ng)对大鼠中缝背核尼古丁的抗焦虑作用有拮抗作用[2]。动物模型：200-250 g雄性带帽李斯特大鼠[1]剂量：0.5、1.6、5.0 mg/kg给药：S.c.结果：在给药后45分钟内,阻止了CTA(条件性味觉厌恶)的发展,并阻断了尼古丁(0.2或0.4 mg/kg SC)的辨别刺激作用。

[参考文献]

[1]. Shoaib M, et al. Antagonism of stimulus properties of nicotine by dihydro-beta-erythroidine (DHbetaE) in rats. Psychopharmacology (Berl). 2000 Apr;149(2):140-6.

[2]. Cheeta S, et al. Antagonism of the anxiolytic effect of nicotine in the dorsal raphe nucleus by dihydro-beta-erythroidine. Pharmacol Biochem Behav. 2001 Dec;70(4):491-6.

物理化学性质

[ 密度 ]:
1.25g/cm3

[ 沸点 ]:
486.6ºC at 760 mmHg

[ 分子式 ]:
C₁₆H₂₁NO₃

[ 分子量 ]:
275.34300

[ 闪点 ]:
248.1ºC

[ 精确质量 ]:
275.15200

[ PSA ]:
38.77000

[ LogP ]:
1.75120

[ 蒸汽压 ]:
1.27E-09mmHg at 25°C

[ 折射率 ]:
1.592

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KF3150000

CHEMICAL NAME :: beta-Erythroidine, dihydro-

CAS REGISTRY NUMBER :: 23255-54-1

BEILSTEIN REFERENCE NO. :: 0036193

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C16-H21-N-O3

MOLECULAR WEIGHT :: 275.38

WISWESSER LINE NOTATION :: T B6656 1A Q AX DVO JN XU XUTJ PO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4500 ug/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 113,212,1955

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 3 mg/kg

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

REFERENCE :: RISSAF Rendiconti Istituto Superiore di Sanita (Italian Edition). (Rome, Italy) V.4-27, 1941-64. Volume(issue)/page/year: 12,158,1949