Imazodan (CI‐914)

Steffen, Robert P.; Weishaar, Ronald E.; Evans, Dale B.; Kaplan, Harvey

doi:10.1111/j.1527-3466.1986.tb00489.x

Cited by 6 publications

(15 citation statements)

References 16 publications

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“…Amrinone produced a comparable reduction in forelimb perfusion pressure, but at 10 times the dose [81]. In comparing the balance between inotropic and vasodilator activity for imazodan and amrinone, Steffen et al [79] reported that the ratio of the two activities was 1.02 for imazodan and 0.23 for amrinone, and suggested that imazodan produces a more balanced mix ofinotropic to vasodilator activity than amrinone.…”

Section: In-vivo Studiesmentioning

confidence: 99%

“…When administered in vivo, imazodan exerts both a direct positive inotropic effect on the heart and a direct relaxant effect on the peripheral vasculature [79]. The latter response likely represents inhibition of vascular muscle PDE III by imazodan, since increases in cyclic AMP in smooth muscle result in vasodilation [80].…”

Section: In-vivo Studiesmentioning

confidence: 99%

“…Although imazodan produced no consistent shifts in blood flow to several peripheral vascular beds, e.g., liver, duodenum, and brain, imazodan produced a marked increase in renal blood flow when infused over a range of 1 to 30 pg/kg/min [79]. In addition to peripheral blood flow, the effect of imazodan on myocardial blood flow was also evaluated.…”

Section: In-vivo Studiesmentioning

confidence: 99%

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New mechanisms for positive inotropic agents: Focus on the discovery and development of imazodan

Weishaar¹,

Kobylarz-Singer²,

Klinkefus³

1989

Cardiovasc Drug Ther

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Intense efforts during the last decade to identify a useful positive inotropic agent to replace digitalis for the treatment of congestive heart failure have led to the discovery of several dozen potential substitutes, of which a number are currently undergoing clinical trials. In addition to producing a variety of new therapeutic entities, research in this area has also yielded valuable new information regarding the fundamental events that regulate calcium homeostasis and contractile function in the cardiac cell. For example, several of these new inotropic agents, including the calcium-channel stimulator BAY-k 8644, the sodium-channel stimulator DPI-201-186, and the sodium-calcium exchange inhibitor dichlorobenzamil, have provided considerable insight into the role of sodium and calcium in regulating contractility and the molecular events that mediate potential-dependent ion channels. Likewise, the discovery and development of agents like imazodan, amrinone, enoximone, and other selective type III phosphodiesterase inhibitors have provided new information regarding multiple molecular forms of cyclic nucleotide phosphodiesterase, compartmentation of cyclic AMP, and the importance of soluble vs. membrane-bound phosphodiesterases.

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Section: In-vivo Studiesmentioning

confidence: 99%

Section: In-vivo Studiesmentioning

confidence: 99%

Section: In-vivo Studiesmentioning

confidence: 99%

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New mechanisms for positive inotropic agents: Focus on the discovery and development of imazodan

Weishaar¹,

Kobylarz-Singer²,

Klinkefus³

1989

Cardiovasc Drug Ther

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“…IR (KBr) cm The compounds (7)(8)(9)(10)(11)(12)(13) were identified on the basis of the difference in the melting points and R f values with respect to their reactants. These compounds were not subjected for their spectral analysis as their ACE inhibitory activity results .i.e.…”

Section: -Benzoyl-4-(4-bromobenzylidene)-6-phenyl-45-dihydropyridazmentioning

confidence: 99%

“…There are many cardioactive pyridazinone derivatives, which are either in clinical use or have been tested in clinical trials, for example, imazodan 7,8 , CI-930 8,9 , pimobendan 8,10 , indolidan 8,11 , levosimendan 8,12 , SK&F-93741 8,13 , Y-590 8,14 , Meribendan 15 , NSP-804 16 , NSP-805 16 , bemoradan 17,18 , senazodan 19 , amipizone 8,18 , prinoxodan 20 , SKF 95654 21 , siguazodan 22 and KF 15232 22 . Some of these pyridazinone derivatives were found not suitable for further development because of their side effects and low potency.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antihypertensive Activity of Some Novel Pyridazinones

Imran¹,

Nayeem²

2016

Orient. J. Chem

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Four pyridazinones (2-5) were synthesized by the reaction of 3-benzoylpropionic acid with the corresponding hydrazines. These pyridazinones were further derivatized with appropriate aromatic aldehydes in the presence of piperidine to obtain the desired compounds (6-13). The chemical structures of the synthesized pyridazinones were elucidated on the basis of their spectral analysis (IR, 1 H-NMR, and 13 C-NMR). Molecular docking studies were carried out to identify the most active antihypertensive pyridazinone compound by using the crystal structure of human Angiotensin Converting Enzyme (ACE), the enzyme implicated in the pathogenesis of hypertension. The compound (6) was identified as the most active inhibitor of the Angiotensin Converting Enzyme (ACE). This compound was further assessed for its ACE inhibitory activity using Dojindo ACE Kit-WST test kit. The enzymatic ACE inhibitory activity revealed that the compound (6) had IC 50 value of 5.78 µg/ mL, wherein the standard drug Lisinopril had IC 50 value of 0.85 µg/mL. It has been concluded that incorporation of free amino groups and free carboxylic acid groups in the structure of the synthesized pyridazinone (6-13) may provide more active and potent ACE inhibitors.

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