127408-30-4

• 常用中文名：N-(苄氧基)-n-((3s,4r)-6-氰基-3-羟基-2,2-二甲基苯并二氢吡喃-4-基)乙酰胺
• 常用英文名：Y-27152
• CAS号：127408-30-4
• 分子式：C₂₁H₂₂N₂O₄
• 分子量：366.41
• 相关类别： 信号通路 跨膜转运 钾通道
• 发布时间：2019-01-12 18:29:13
• 更新时间：2024-01-22 08:23:03
• Y-27152 是KATP (Kir6)通道开放剂Y-26763的前体药物,是长效的K+ 通道开放剂,在高血压大鼠和狗在清醒状态下发挥降压作用的同时,具有更低的心动过速作用。

名称

• 中文名: N-(苄氧基)-n-((3s,4r)-6-氰基-3-羟基-2,2-二甲基苯并二氢吡喃-4-基)乙酰胺
• 英文名: N-[(3S,4R)-6-Cyano-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl]-N-(phenylmethoxy)acetamide
• 英文别名: Conantokin-R; Y-27152

物化性质

• 密度: 1.28g/cm3
• 沸点: 513.4ºC at 760mmHg
• 分子式: C₂₁H₂₂N₂O₄
• 分子量: 366.41
• 闪点: 264.3ºC
• 精确质量: 366.15800
• PSA: 82.79000
• LogP: 3.11158
• 蒸汽压: 2.29E-11mmHg at 25°C
• 折射率: 1.617

生物活性

• 描述: Y-27152 是KATP (Kir6)通道开放剂Y-26763的前体药物,是长效的K+ 通道开放剂,在高血压大鼠和狗在清醒状态下发挥降压作用的同时,具有更低的心动过速作用。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 靶点:

  K+ channel[1].

• 参考文献:

  [1]. Nakajima T, et al. Y-27152, a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state. J Pharmacol Exp Ther. 1992 May;261(2):730-6.

  [2]. Fukunari A, et al. Y-26763 protects the canine heart from a stunning injury through opening of the KATP channels. Eur J Pharmacol. 1997 Apr 4;323(2-3):197-204.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : AB5956333 CHEMICAL NAME : Acetamide, N-(6-cyano-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-be nzopyran-4-yl)- N-(phenylmethoxy)-, (3S-trans)- CAS REGISTRY NUMBER : 127408-30-4 LAST UPDATED : 199603 DATA ITEMS CITED : 5 MOLECULAR FORMULA : C21-H22-N2-O4 MOLECULAR WEIGHT : 366.45 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 : >2 gm/kg TOXIC EFFECTS : Cardiac - other changes Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - other changes REFERENCE : CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,372,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Cardiac - other changes Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - other changes REFERENCE : CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,372,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 10 mg/kg TOXIC EFFECTS : Cardiac - other changes Vascular - BP lowering not characterized in autonomic section Lungs, Thorax, or Respiration - other changes REFERENCE : CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,372,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 910 mg/kg/13W-I TOXIC EFFECTS : Cardiac - changes in heart weight Vascular - BP lowering not characterized in autonomic section Endocrine - changes in thymus weight REFERENCE : CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,372,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 27300 ug/kg/13W-I TOXIC EFFECTS : Cardiac - changes in heart weight Vascular - BP lowering not characterized in autonomic section REFERENCE : CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 9,372,1991