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DPI 201-106

Names

[ CAS No. ]:
97730-95-5

[ Name ]:
DPI 201-106

[Synonym ]:
Dpi 201-106

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]:

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

[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]

[1]. G Scholtysik, et al. DPI 201-106, a novel cardioactive agent. Combination of cAMP-independent positive inotropic, negative chronotropic, action potential prolonging and coronary dilatory properties. Naunyn Schmiedebergs Arch Pharmacol.1985 May;329(3):316-25.

[2]. G Scholtysik, et al. Interaction of DPI 201-106 with cardiac glycosides. J Cardiovasc Pharmacol. 1989 Feb;13(2):342-7.

[3]. M Mevissen, et al. Identification of a cardiac sodium channel insensitive to synthetic modulators. J Cardiovasc Pharmacol Ther. 2001 Apr;6(2):201-12.

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

Related Compounds