中文名 | 5-METHYL-2-(1-PIPERAZINYL)BENZENESULFONIC ACID MONOHYDRATE |
英文名 | 5-METHYL-2-(1-PIPERAZINYL)BENZENESULFONIC ACID MONOHYDRATE |
别名 | 化合物 T14857 |
英文别名 | Caldaret Benzenesulfonic acid, 5-methyl-2-(1-piperazinyl)- 5-METHYL-2-(1-PIPERAZINYL)BENZENESULFONIC ACID MONOHYDRATE |
CAS | 133804-44-1 |
化学式 | C11H16N2O3S |
分子量 | 256.32 |
密度 | 1.302±0.06 g/cm3(Predicted) |
酸度系数 | -1.76±0.42(Predicted) |
存储条件 | Room Temprature |
体外研究 | Caldaret (MCC-135) is demonstrated to restore Ca 2+ -ATPase activity of the sarcoplasmic reticulum (SR) isolated from the myocardium acutely exposed to ischemia and reperfusion in vitro. |
体内研究 | Caldaret, an intracellular Ca 2+ handling modulator, limits infarct size of reperfused canine heart. The cardioprotective effect of Caldaret, a novel intracellular Ca 2+ handling modulator that acts through reverse-mode Na + /Ca 2+ exchanger inhibition and potential sarcoplasmic reticulum (SR) Ca 2+ uptake enhancement, against reperfusion injury is investigated. Intravenously infused Caldaret (3 or 30 microg/kg per hour) for 30 min at left circumflex (LCX)-reperfusion markedly reduces infarct size (by 51.3% or 71.9%, respectively). The amelioration of intracellular Ca 2+ handling dysfunction achieved by Caldaret leads to cardioprotective effects against reperfusion injury following prolonged ischemia. Caldaret (MCC-135) is a new potent compound with beneficial effects in heart failure. In diabetic rats, Caldaret decreases TR80 significantly without significant effect on developed tension (DT). Caldaret has minimal effects on SR Ca 2+ uptake in normal rats, that is observed as increased SR Ca 2+ uptake at uptake time of 20 and 30 s at the highest concentration of 10 μM. In diabetic rats, Caldaret increases SR Ca 2+ uptake all over the range of uptake time. Both initial rate of SR Ca 2+ uptake and the amount of Ca 2+ accumulated in the SR with longer uptake time are increased by Caldaret. |
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