Bioactivity | 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]. | ||||||||||||
Target | Sodium Channel | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | DPI 201-106 | ||||||||||||
CAS | 97730-95-5 | ||||||||||||
Formula | C29H30N4O2 | ||||||||||||
Molar Mass | 466.57 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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- [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. |