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Iptakalim improves cerebral microcirculation in mice after ischemic stroke by inhibiting pericyte contraction
In this study we investigated the impacts of iptakalim on pericytes contraction in stroke. Mice were subjected to cerebral artery occlusion (MCAO), then administered iptakalim (10 mg/kg, ip). We showed that iptakalim administration significantly promoted recovery of cerebral blood flow after cerebral ischemia and reperfusion. Furthermore, we found that iptakalim significantly inhibited pericytes contraction, decreased the number of obstructed capillaries, and improved cerebral microcirculation. Using a collagen gel contraction assay, we demonstrated that cultured pericytes subjected to oxygen-glucose deprivation (OGD) cons...
Source: Acta Pharmacologica Sinica - October 26, 2021 Category: Drugs & Pharmacology Authors: Ruo-Bing Guo Yin-Feng Dong Zhi Yin Zhen-Yu Cai Jin Yang Juan Ji Yu-Qin Sun Xin-Xin Huang Teng-Fei Xue Hong Cheng Xi-Qiao Zhou Xiu-Lan Sun Source Type: research

The role of KATP channels in cerebral ischemic stroke and diabetes.
Abstract ATP-sensitive potassium (KATP) channels are ubiquitously expressed on the plasma membrane of cells in multiple organs, including the heart, pancreas and brain. KATP channels play important roles in controlling and regulating cellular functions in response to metabolic state, which are inhibited by ATP and activated by Mg-ADP, allowing the cell to couple cellular metabolic state (ATP/ADP ratio) to electrical activity of the cell membrane. KATP channels mediate insulin secretion in pancreatic islet beta cells, and controlling vascular tone. Under pathophysiological conditions, KATP channels play cytoprotect...
Source: Acta Pharmacologica Sinica - April 19, 2018 Category: Drugs & Pharmacology Authors: Szeto V, Chen NH, Sun HS, Feng ZP Tags: Acta Pharmacol Sin Source Type: research

Conversion and pharmacokinetics profiles of a novel pro-drug of 3-n-butylphthalide, potassium 2-(1-hydroxypentyl)-benzoate, in rats and dogs.
In this study, we investigated the conversion and pharmacokinetics profiles of dl-PHPB in vitro and in vivo. The conversion of dl-PHPB to dl-NBP was pH- and calcium-dependent, and paraoxonase was identified as a major enzyme for the conversion in rat plasma. The pharmacokinetics, tissue distribution and excretion of dl-PHPB were studied and compared with equal-molar doses of dl-NBP in rats and dogs. The in vivo studies showed that dl-PHPB could be quickly and completely converted to dl-NBP. The plasma concentration-time course of converted dl-NBP after intravenous dl-PHPB administration was nearly the same as that after eq...
Source: Acta Pharmacologica Sinica - September 14, 2017 Category: Drugs & Pharmacology Authors: Li J, Xu SF, Peng Y, Feng N, Wang L, Wang XL Tags: Acta Pharmacol Sin Source Type: research

Potassium 2-(1-hydroxypentyl)-benzoate promotes long-term potentiation in Aβ1-42-injected rats and APP/PS1 transgenic mice.
Conclusion:Chronic administration of dl-PHPB improves learning and memory and promotes LTP in the animal models of Alzheimer's disease, possibly via increasing p-GluN2B expression in the hippocampus. PMID: 24858312 [PubMed - as supplied by publisher]
Source: Acta Pharmacologica Sinica - May 26, 2014 Category: Drugs & Pharmacology Authors: Li PP, Wang WP, Liu ZH, Xu SF, Lu WW, Wang L, Wang XL Tags: Acta Pharmacol Sin Source Type: research