LOPERAMIDE AND CALMODULIN - The Lancet
LOPERAMIDE AND CALMODULIN. JanetE. Merritt ∙ BarryL. Brown ∙ Stephen Tomlinson. a Department of Human Metabolism and Clinical Biochemistry, University of Sheffield Medical School, Sheffield S10 2RX, United Kingdom. b and University Clinical Sciences Centre, Northern General Hospital, Sheffield, United Kingdom.
We investigated whether the synthetic opiate loperamide-HCI is able to regulate specific transport systems for sodium and chloride in brush border membrane vesicles (BBMVs) from human ileum and whether such activities are mediated by calcium/ calmodulin.
Calmodulin-mediated effects of loperamide on chloride …
We investigated whether the synthetic opiate loperamide-HCl is able to regulate specific transport systems for sodium and chloride in brush border membrane vesicles (BBMVs) from human ileum and whether such activities are mediated by calcium/ calmodulin. In BBMVs we studied antiport, antiport, cotransport, and the Cl− conductive pathway.
Potential roles of P-gp and calcium channels in loperamide and ...
2003年11月15日 · The aim of this paper was to examine both loperamide and diphenoxylate transport into and through Caco-2 cell monolayers, a cell line known to express endogenously high levels of P-gp, in order to determine the extent that P-gp efflux may be keeping these opiates out of the sensitive organs and to compare the rates of efflux determined here ...
Loperamide: novel effects on capacitative calcium influx
Loperamide at micromolar concentrations has now been shown to have a remarkable stimulatory effect on the capacitative calcium influx that is triggered in many cells by depletion of the inositol-trisphosphate-sensitive stores of calcium in the endoplasmic reticulum.
Loperamide: A positive modulator for store-operated calcium …
1997年12月12日 · Loperamide is the first compound known to augment levels of intracellular calcium when SOC channels are activated. The effect appears to be general as it is observed in a variety of cell types. Loperamide also alters the sensitivity of SOC channels to various inhibitors.
Mechanisms of action of loperamide - PubMed
The mechanism of action of loperamide on fluid and electrolyte transport is examined with reference to opiate agonism, calcium-channel blocking, calmodulin inhibition, and paracellular permeability. The colon appears to be the main site of action of …
Loperamide, an antidiarrheal agent, induces apoptosis and DNA …
Blocking the µ-opioid receptor of the gastrointestinal tract and antagonizing calmodulin are the two main molecular mechanisms for the antidiarrheal effect of loperamide (34–37). In previous years, loperamide was also found to possess anti-neoplastic activity in a variety of tumors in vitro , including liver, breast, lung and canine cancers ...
Calmodulin-mediated effects of loperamide on chloride transport …
1988年7月1日 · We investigated whether the synthetic opiate loperamide-HCl is able to regulate specific transport systems for sodium and chloride in brush border membrane vesicles (BBMVs) from human ileum and whether such activities are mediated by calcium/ calmodulin.
Calmodulin-mediated effects of loperamide on chloride transport by ...
1988年7月1日 · Increasing the Ca t+/calmodulin activity of loperamide-pretreated BBMVs with 2 /AM calcium plus 5 /AM calmodulin led to a significant inhibition of Cl-/OH- antiport and Na+/Cl- cotransport by 40% 't 5% (p < 0.005). Unlike traditional opiates, the synthetic antidiarrheal drug loperamide can bind to calmodulin and inhibit its activity (1).