DPI 201-106
Names
Biological Activity
[Description]:
DPI 201-106 (SDZ 201106) is a cardiotonic agent with a synergistic sarcolemmal and intracellular mechanism of action. DPI 201-106 shows cardioselective modulation of voltage-gated sodium channels (VGSCs) resulting in a positive inotropic effect[1][2][3].
[Related Catalog]:
[Target]
Sodium Channel[3]
[In Vitro]
DPI 201-106 increases the Ca2+-sensitivity of skinned fibres from porcine trabecula septomarginalis with an EC50 of 0.2 nM[2]. DPI 201-106 produces concentration-dependent positive inotropic effects in guinea-pig and rat left atria, kitten, rabbit and guinea-pig papillary muscles and Langendorff perfused hearts of rabbits between 0.1 and 3 μM[2].
[In Vivo]
In anesthetized dogs, left ventricular dP/dtmax is increased by DPI 201-106 0.2 mg/kg i.v.In digoxin-pretreated anesthetized cats, DPI 201-106 is infused up to an accumulated dose of 12.22 mg/kg i.v. [3].
[References]
Chemical & Physical Properties
[ Density]:
1.29g/cm3
[ Boiling Point ]:
702.6ºC at 760mmHg
[ Molecular Formula ]:
C29H30N4O2
[ Molecular Weight ]:
466.57400
[ Flash Point ]:
378.7ºC
[ Exact Mass ]:
466.23700
[ PSA ]:
75.52000
[ LogP ]:
4.06228
[ Index of Refraction ]:
1.692
Toxicological Information
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- NL5993340
- CHEMICAL NAME :
- 1H-Indole-2-carbonitrile, 4-(3-(4-(diphenylmethyl)-1-piperazinyl)-2-hydroxyprop oxy-, (+-)-
- CAS REGISTRY NUMBER :
- 97730-95-5
- LAST UPDATED :
- 199512
- DATA ITEMS CITED :
- 4
- MOLECULAR FORMULA :
- C29-H30-N4-O2
- MOLECULAR WEIGHT :
- 466.63
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >3 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 40 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >5600 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 47 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- NCDREP New Cardiovascular Drugs. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) 1985- Volume(issue)/page/year: 5,173,1987