97730-95-5

97730-95-5 structure

Name: DPI 201-106
Chemical Name: 4-[3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropoxy]-1H-indole-2-carbonitrile
CAS Number: 97730-95-5
Molecular Formula: C₂₉H₃₀N₄O₂
Molecular Weight: 466.57400
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
Create Date: 2016-04-24 19:20:10
Modify Date: 2024-01-08 17:58:22
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].

Name	4-[3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropoxy]-1H-indole-2-carbonitrile
Synonyms	Dpi 201-106

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.

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

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

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