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      Positive inotropic activity induced by a dehydroisoandrosterone derivative in isolated rat heart model

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      https://www.riss.kr/link?id=A104666129

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      다국어 초록 (Multilingual Abstract)

      Experimental studies indicate that some steroidderivatives have inotropic activity; nevertheless, there isscarce information about the effects of the dehydroisoandrosteroneand its derivatives at cardiovascular level. Inaddition, to date the cellular s...

      Experimental studies indicate that some steroidderivatives have inotropic activity; nevertheless, there isscarce information about the effects of the dehydroisoandrosteroneand its derivatives at cardiovascular level. Inaddition, to date the cellular site and mechanism of actionof dehydroisoandrosterone at cardiovascular level is veryconfusing. In order, to clarify those phenomena in this study,a dehydroisoandrosterone derivative was synthesized withthe objective of to evaluate its activity on perfusion pressureand coronary resistance and compare this phenomenon withthe effect exerted by dehydroisoandrosterone. The Langendorfftechnique was used to measure changes on perfusionpressure and coronary resistance in an isolated rat heartmodel in absence or presence of dehydroisoandrosterone andits derivative. Additionally, to characterize the molecularmechanism involved in the inotropic activity induced bydehydroisoandrosterone derivative was evaluated by measuringleft ventricular pressure in absence or presence offollowing compounds; flutamide, prazosin, metoprolol andnifedipine. The results showed that dehydroisoandrosteronederivative significantly increased the perfusion pressure andcoronary resistance in comparison with the control conditionsand dehydroisoandrosterone. Additionally, other dataindicate that dehydroisoandrosterone derivative increase leftventricular pressure in a dose-dependent manner [1 9 10-9–1 9 10-4 mmol]; nevertheless, this phenomenon was significantlyinhibited by nifedipine at a dose of 1 9 10-6mmol. In conclusion, these data suggest that dehydroisoandrosteronederivative induces positive inotropic activitythrough of activation the L-type calcium channel.

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      참고문헌 (Reference)

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      7 Erdmann, E, "The effectiveness of inotropic agents in isolated cardiac preparations from the human heart" 66 : 1-6, 1988

      8 Figueroa-Valverde, L., "Synthesis of a new inotropic steroid derivative and its relationship with log P, p, Rm, Vm, Pc" 23 (23): 1599-1604, 2011

      9 Figueroa-Valverde, L., "Synthesis and evaluation of the cardiovascular effects of two, membrane impermeant, macromolecular complexes of dextran-testosterone" 67 (67): 611-619, 2002

      10 De Munari, S., "Structure-based design and synthesis of novel potent na?, k?-atpase inhibitors derived from a 5a, 14aandrostane scaffold as positive inotropic compounds" 46 (46): 3644-3654, 2003

      1 Hocht, C., "Una aproximacion cinetica y dinamica de metildopa en ratas con coartacion aortica mediante microdialisis" 67 : 769-773, 1999

      2 Lederer, W., "Transient inward current underlying arrhythmogenic effects of cardiotonic steroids in purkinjefibres" 263 : 73-100, 1976

      3 Silverberg, D., "The use of subcutaneous erythropoietin and intravenous iron for the treatment of the anemia of severe, resistant congestive heart failure improves cardiac and renal function and functional cardiac class, and markedly reduces hospitalizations" 35 (35): 1737-1744, 2000

      4 Rannard, S., "The selective reaction of primary amines with carbonyl imidazole containing compounds : Selective amide and carbamate synthesis" 2 : 2117-2120, 2000

      5 Akera, T., "The role of Na?, K?-ATPase in the inotropic action of digitalis" 29 : 187-220, 1977

      6 Clark, A. J, "The mode of action of strophanthidin upon cardiac tissue" 5 (5): 215-234, 1914

      7 Erdmann, E, "The effectiveness of inotropic agents in isolated cardiac preparations from the human heart" 66 : 1-6, 1988

      8 Figueroa-Valverde, L., "Synthesis of a new inotropic steroid derivative and its relationship with log P, p, Rm, Vm, Pc" 23 (23): 1599-1604, 2011

      9 Figueroa-Valverde, L., "Synthesis and evaluation of the cardiovascular effects of two, membrane impermeant, macromolecular complexes of dextran-testosterone" 67 (67): 611-619, 2002

      10 De Munari, S., "Structure-based design and synthesis of novel potent na?, k?-atpase inhibitors derived from a 5a, 14aandrostane scaffold as positive inotropic compounds" 46 (46): 3644-3654, 2003

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      12 Templeton, J., "Progesterone derivatives that bind to the digitalis receptor : synthesis of 14 beta-hydroxyprogesterone : A novel steroid with positive inotropic activity" 30 (30): 1502-1505, 1987

      13 Medvedeva, A., "Preparation of 3-(trimethylsilanyl)propynoic acid N-(hydroxyalkyl) amides" 143-149, 2001

      14 Levin, D, "Potential toxicological concerns associated with carboxylic acid chlorination and other reactions" 1 : 182-, 1997

      15 Bengtsson, C., "Plasma levels and effects of metoprolol on blood pressure and heart rate in hypertensive patients after an acute dose and between two doses during long-term treatment" 17 : 400-408, 1975

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      21 Pierard, L., "Haemodynamic alterations during ischaemia induced by dobutamine stress testing" 10 (10): 783-790, 1989

      22 Wier, W., "Excitation-contraction coupling in cardiac Purkinje fibers effects of cardiotonic steroids on the intracellular [Ca2?] transient, membrane potential, and contraction" 83 (83): 395-415, 1984

      23 Maixten, J., "Efficacy and safety of the novel Na?, K?-ATPase inhibitor 20R 14bamino 3b-rhamnosyl 5b-pregnan 20b-ol in a dog model of heart failure" 42 (42): 1301-1305, 1992

      24 Endoh, M., "Effects of new inotropic agents on cyclic nucleotide metabolism and calcium transients in canine ventricular muscle" 73 : 117-133, 1986

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      26 Smith, T. W, "Digitalis toxicity : Epidemiology and clinical use of serum concentration measurements" 58 : 470-476, 1975

      27 Figueroa-Valverde, L., "Design and synthesis of two brucine derivatives and evaluation of its antibacterial activity against Escherichia coli and Salmonella typhi" 24 (24): 2173-2176, 2012

      28 Hutchison, S., "Dehydroepiandrosterone sulfate induces acute vasodilation of porcine coronary arteries in vitro and in vivo" 46 (46): 325-332, 2005

      29 Charalampopoulos, I., "Dehydroepiandrosterone sulfate and allopregnanolone directly stimulate catecholamine production via induction of tyrosine hydroxylase and secretion by affecting actin polymerization" 146 (146): 3309-3318, 2005

      30 Tan, J., "Dehydroepiandrosterone activates mutant androgen receptors expressed in the androgen-dependent human prostate cancer xenograft CWR22 and LNCaP cells" 11 (11): 450-459, 1997

      31 Hauser, R., "Conversion of nitriles to amides and acids by means of boron fluoride" 20 : 1448-1453, 1955

      32 Braunwald, E., "Congestive heart failure: Fifty years of progress" 102 : 14-23, 2000

      33 Henry, P. D, "Comparative pharmacology of calcium antagonists : nifedipine, verapamil and diltiazem" 46 : 1047-1058, 1980

      34 Feldman, A, "Classification of positive inotropic agents" 22 (22): 1223-1227, 1993

      35 Simard, J., "Characteristics of interaction of the antiandrogen flutamide with the androgen receptor in various target tissues" 44 : 261-270, 1986

      36 Figueroa-Valverde, L., "Changes induced by estradiol-ethylenediamine derivative on perfusion pressure and coronary resistance in isolated rat heart : L-type calcium channel" 155 (155): 27-32, 2011

      37 Figueroa Valverde, L., "Biological activity of progesterone-dihydropyridimidine derivative on perfusion pressure and coronary resistance in isolated rat heart" 4 : 170-177, 2010

      38 Graham, R., "Alpha blocking action of the antihypertensive agent, prazosin" 201 : 747-752, 1977

      39 Ceballos, G., "Acute and nongenomic effects of testosterone on isolated and perfused rat heart" 33 : 691-697, 1999

      40 Figueroa, L., "Actividad inducida por androsterona y hemisuccinato de androsterona sobre la presion de perfusion y la resistencia vascular" 29 (29): 625-634, 2009

      41 Pignier, C., "A novel steroid-like compound F90927 exerting positive-inotropic effects in cardiac muscle" 147 (147): 772-782, 2006

      42 Gobbini, M., "17 alpha-O-(aminoalkyl)oxime derivatives of 3 beta, 14 beta-dihydroxy-5 beta-androstane and 3 betahydroxy-14-oxoseco-D-5 beta-androstane as inhibitors of Na(?), K(?)-ATPase at the digitalis receptor" 44 (44): 3821-3830, 2001

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      기준연도 WOS-KCI 통합IF(2년) KCIF(2년) KCIF(3년)
      2016 1.96 0.2 1.44
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