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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

用途

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

[ CAS 号 ]:
127408-30-4

[ 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 ]:
Y-27152

[英文别名 ]:

Conantokin-R
Y-27152

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.

物理化学性质

[ 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

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