Disease relevance of Bimoclomol

• Our findings indicate that Bimoclomol could have a beneficial effect on some dyskinesias, and on drug-induced vertical head movements [1].
• Rats were pretreated with bimoclomol at 3, 6 or 18 h or with 42 degrees thermal stress 24 h before ischemia [2].
• These findings suggest that bimoclomol may have future therapeutic use in diabetic retinopathy [3].
• Oral bimoclomol elevates heat shock protein 70 and reduces myocardial infarct size in rats [2].
• Bimoclomol (BRLP-42) is a novel antiischemic compound acting against peripheral vascular complications of diabetes mellitus (neuropathy, retinopathy, and nephropathy) [4].

High impact information on Bimoclomol

• We show here that the presence of BM does not influence protein denaturation in the cells [5].
• 2. Effects of bimoclomol on action potential configuration was studied in isolated canine ventricular myocytes [6].
• Biphasic effect of bimoclomol on calcium handling in mammalian ventricular myocardium [6].
• 5. In conclusion, the positive inotropic action of bimoclomol is likely due to the activation of the sarcoplasmic reticulum calcium release channel in mammalian ventricular myocardium [6].
• Bimoclomol had a biphasic effect on contractility: both peak left ventricular pressure and the rate of force development significantly increased at a concentration of 10 nM or higher [6].

Chemical compound and disease context of Bimoclomol

• The effect of Bimoclomol (BRLP-42), a drug under clinical development for the treatment of diabetic complications, on experimental peripheral neuropathy was examined in rats made diabetic by injection of streptozotocin [7].

Biological context of Bimoclomol

• In conclusion, bimoclomol improved cell survival in rat neonatal cardiomyocytes, in part, by increasing the levels of HSP70 [8].
• These findings indicate that bimoclomol may be of value in targeting HSF-1 so as to induce up-regulation of protective Hsp-s in a non-stressful manner and for therapeutic benefit [9].
• Enantioselective plasma protein binding of bimoclomol [10].
• [Ca2+]i transients, measured under voltage clamp control, were increased in amplitude and had accelerated decay kinetics in the presence of the compound, in addition to reduction of diastolic [Ca2+]i. Bimoclomol significantly decreased the force of contraction in right ventricular trabeculae [11].
• Enhancement of wound healing by bimoclomol was observed after thermal injury as well as following ultraviolet (UV) irradiation [12].

Anatomical context of Bimoclomol

• 4. Bimoclomol (10 microM - 1 mM) had no significant effect on the rate of calcium uptake into sarcoplasmic reticulum vesicles of the dog, indicating that in vivo calcium reuptake might not substantially be affected by the drug [6].

Associations of Bimoclomol with other chemical compounds

• In the spontaneously hypertensive rats chronic pretreatment with bimoclomol restored sensitivity of aortic rings to acetylcholine; this effect was accompanied by accumulation of HSP-70 in the tissues [12].

Gene context of Bimoclomol

• Moreover, bimoclomol binds to HSF-1 and induces a prolonged binding of HSF-1 to the respective DNA elements [9].
• This study was designed to investigate the effects of subchronic bimoclomol treatment on endothelial function and expression of 72 kD heat shock protein (HSP-72) in spontaneously hypertensive rats [13].

Analytical, diagnostic and therapeutic context of Bimoclomol

• Infarct size was significantly decreased 6 h after oral administration of bimoclomol and 24 h after thermal stress [2].
• Thus, bimoclomol can increase HSP70 and reduce infarct size in a rat model of ischemia and reperfusion [2].
• Concentration-dependent effects of bimoclomol, a novel heat shock protein (HSP) coinducer, were studied on the parameters of action potential and transmembrane ionic currents in enzymatically dispersed canine ventricular cardiomyocytes using conventional microelectrode and whole cell voltage clamp techniques [14].
• The effects of the novel HSP-coinducer bimoclomol was studied on action potentials, ionic currents and [Ca2+]i transients in isolated canine ventricular myocytes using conventional microelectrode techniques and whole cell voltage clamp combined with fluorescent [Ca2+]i measurements [11].
• The binding of bimoclomol enantiomers to human plasma, its components, as well as to plasma from monkey, dog, rat, and mouse was investigated by ultrafiltration and equilibrium dialysis [10].

References