63307-63-1

• 常用中文名：[D- MET2 , PRO5 ]-ENKEPHALINAMIDE
• 常用英文名：[D- MET2 , PRO5 ]-ENKEPHALINAMIDE
• CAS号：63307-63-1
• 分子式：C₃₀H₄₀N₆O₆S
• 分子量：612.74000
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 阿片受体
• 发布时间：2017-04-26 19:23:33
• 更新时间：2024-01-12 16:17:52
• (D-Met2,Pro5)-脑啡肽是一种高效的阿片类激动剂,具有抗伤害活性[1][2][3]。

名称

• 英文名: 1-[2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carboxamide
• 英文别名: H-Tyr-D-Met-Gly-Phe-Pro-NH2; L-tyrosyl-D-methionyl-glycyl-L-phenylalanyl-L-proline amide; Tyr-D-Met-Gly-Phe-Pro-NH2

物化性质

• 密度: 1.31g/cm3
• 沸点: 1065ºC at 760 mmHg
• 分子式: C₃₀H₄₀N₆O₆S
• 分子量: 612.74000
• 闪点: 597.9ºC
• 精确质量: 612.27300
• PSA: 233.71000
• LogP: 4.12870
• 折射率: 1.616

生物活性

• 描述: (D-Met2,Pro5)-脑啡肽是一种高效的阿片类激动剂,具有抗伤害活性[1][2][3]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
  研究领域 >> 其他
  信号通路 >> 神经信号通路 >> 阿片受体
• 体内研究: (D-Met2,Pro5)-脑啡肽(静脉注射；0.25和0.5 mg/kg；一次)导致哺乳期大鼠催乳素(PRL)分泌减少[2]。动物模型：Wistar哺乳大鼠[2]剂量：0.25和0.5 mg/kg给药：静脉注射；0.25和0.5mg/kg；结果：连续哺乳大鼠给药15分钟后血浆PRL水平降低。非剥夺哺乳期母亲血浆PRL浓度显著降低。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TW3583000 CHEMICAL NAME : L-Prolinamide, L-tyrosyl-D-methionylglycyl-L-phenylalanyl- CAS REGISTRY NUMBER : 63307-63-1 LAST UPDATED : 199706 DATA ITEMS CITED : 4 MOLECULAR FORMULA : C30-H40-N6-O6-S MOLECULAR WEIGHT : 612.82 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 510 mg/kg TOXIC EFFECTS : Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning REFERENCE : PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 118 mg/kg TOXIC EFFECTS : Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning REFERENCE : PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1700 mg/kg TOXIC EFFECTS : Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning REFERENCE : PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 278 mg/kg TOXIC EFFECTS : Behavioral - rigidity (including catalepsy) Behavioral - antipsychotic Behavioral - alteration of classical conditioning REFERENCE : PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,641,1987

合成路线

66864-05-9 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177

13734-34-4 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177

38017-89-9 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177

70777-31-0 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177

108329-67-5 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177

82558-39-2 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177

74825-83-5 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177

69612-72-2 ~% 63307-63-1

文献：Audigier; Mazarguil; Gout; Cros European Journal of Medicinal Chemistry, 1980 , vol. 15, # 2 p. 173 - 177