DPI 201-106

Names

[ 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

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