萝芙素盐酸盐

Rauwolscine hydrochloride是高效,选择性的 α2 adrenergic 受体拮抗剂,Ki 值为12 nM。

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

Ki: 12 nM (α2 adrenergic receptor)[1]

[3H] Rauwolscine与α2肾上腺素能受体的结合是可逆的,具有stcreospccific和可饱和的。 [3H] Rauwolscine特异性地标记脑膜中α2肾上腺素能受体的高和低亲和力状态[1]。 [3H] Rauwolscine也表现为5-HT1A受体激动剂,这一结论与早期功能研究相符,表明rauwolscine(以及育亨宾)在5-HT自身受体水平上具有激动作用[2]。当使用[3H] 5-HT作为放射性配体时,确定rauwolscine对人受体具有相对高的亲和力(Ki人= 14.3nM,Ki大鼠= 35.8nM)[3]。饱和度研究表明,[3H] Rauwolscine的亲和力在小鼠,大鼠,兔,狗(2.33-3.03 nM)中相似,除了男性,其显着高于(0.98 nM)[4]。

将新鲜牛额叶皮质与[3H]萝芙辛（82μCi/ mM，稀释）一式三份孵育。通过过滤器在减压下过滤终止孵育，然后用冰冷的Tris-HCl缓冲液冲洗，干燥过夜并加入含有3.0mL 95％Econofluor / 5％Protosol溶液的一次性玻璃小瓶中。通过液体闪烁光谱法对样品计数，效率为32％。 （ - ） - [3H]肾上腺素与牛皮质膜结合在25°C [1]。

[1]. Perry BD, et al. [3H]rauwolscine (alpha-yohimbine): a specific antagonist radioligand for brain alpha 2-adrenergic receptors. Eur J Pharmacol. 1981 Dec 17;76(4):461-4.

[2]. De Vos H, et al. [3H]rauwolscine behaves as an agonist for the 5-HT1A receptors in human frontal cortex membranes. Eur J Pharmacol. 1991 May 25;207(1):1-8.

[3]. Wainscott DB, et al. [3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):17-24.

[4]. Neylon CB, et al. [3H]-rauwolscine binding to alpha 2-adrenoceptors in the mammalian kidney: apparent receptor heterogeneity between species. Br J Pharmacol. 1985 Jun;85(2):349-59.

盐酸异丙肾上腺素 | ICI 118,551盐酸盐 | 盐酸去氧肾上腺素 | 盐酸育亨宾 | 肾上腺素 | 盐酸伊伐布雷定 | 盐酸哌唑嗪 | 盐酸克仑特罗 | 甲磺酸酚妥拉明 | 盐酸胍法辛 | 匹莫齐特 | 盐酸索他洛尔 | 卡维地洛 | 阿替洛尔 | 琥珀酸美托洛尔

MOLECULAR FORMULA :

C21-H26-N2-O3.Cl-H

MOLECULAR WEIGHT :

390.95

WISWESSER LINE NOTATION :

T F6 D5 C666 EM ON&&TTTJ TQ UVO1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

125 mg/kg

TOXIC EFFECTS :

Behavioral - convulsions or effect on seizure threshold

REFERENCE :

LDBU** "Zur Pharmakologie der Yohimbealkaloide, Dissertation," Langer, J., Institute fuer Pharmakologie und Experimentelle Therapie der Universitat Breslau, Poland, 1932 Volume(issue)/page/year: -,-,1932

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

20 mg/kg

TOXIC EFFECTS :

Behavioral - general anesthetic Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea

REFERENCE :

LDBU** "Zur Pharmakologie der Yohimbealkaloide, Dissertation," Langer, J., Institute fuer Pharmakologie und Experimentelle Therapie der Universitat Breslau, Poland, 1932 Volume(issue)/page/year: -,-,1932

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rabbit

DOSE/DURATION :

2 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

LDBU** "Zur Pharmakologie der Yohimbealkaloide, Dissertation," Langer, J., Institute fuer Pharmakologie und Experimentelle Therapie der Universitat Breslau, Poland, 1932 Volume(issue)/page/year: -,-,1932

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - guinea pig

DOSE/DURATION :

162 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

BSPHAV Bulletin des Sciences Pharmacologiques. (Paris, France) V.1-49, 1899-1942. For publisher information, see APFRAD. Volume(issue)/page/year: 47,33,1940

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Parenteral

SPECIES OBSERVED :

Amphibian - frog

DOSE/DURATION :

200 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

BSPHAV Bulletin des Sciences Pharmacologiques. (Paris, France) V.1-49, 1899-1942. For publisher information, see APFRAD. Volume(issue)/page/year: 47,33,1940