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Y-27152

Names

[ CAS No. ]:
127408-30-4

[ Name ]:
Y-27152

[Synonym ]:
Conantokin-R
Y-27152

Biological Activity

[Description]:

Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

K+ channel[1].


[References]

[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.

Chemical & Physical Properties

[ Density]:
1.28g/cm3

[ Boiling Point ]:
513.4ºC at 760mmHg

[ Molecular Formula ]:
C21H22N2O4

[ Molecular Weight ]:
366.41

[ Flash Point ]:
264.3ºC

[ Exact Mass ]:
366.15800

[ PSA ]:
82.79000

[ LogP ]:
3.11158

[ Vapour Pressure ]:
2.29E-11mmHg at 25°C

[ Index of Refraction ]:
1.617

Toxicological Information

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

Related Compounds

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