ArticleBritish journal of pharmacology1992
Imidazoline antagonists of alpha 2-adrenoceptors increase insulin release in vitro by inhibiting ATP-sensitive K+ channels in pancreatic beta-cells.
Article in British journal of pharmacology, 1992. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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21 citing papers in PubMed, 101 citations in OpenAlex.
- Pharmacological stimulation and inhibition of insulin secretion in mouse islets lacking ATP-sensitive K+ channels.British journal of pharmacology · 2010Article
- alpha2A-adrenoceptor antagonism increases insulin secretion and synergistically augments the insulinotropic effect of glibenclamide in mice.British journal of pharmacology · 2008Article
- Article
- Induction of pancreatic duct cells of neonatal rats into insulin-producing cells with fetal bovine serum: a natural protocol and its use for patch clamp experiments.World journal of gastroenterology · 2005Article
- The imidazoline NNC77-0020 affects glucose-dependent insulin, glucagon and somatostatin secretion in mouse pancreatic islets.Naunyn-Schmiedeberg's archives of pharmacology · 2003Article
- Identification of the monomeric G-protein, Rhes, as an efaroxan-regulated protein in the pancreatic beta-cell.British journal of pharmacology · 2002Article
- Cibenzoline, an ATP-sensitive K(+) channel blocker, binds to the K(+)-binding site from the cytoplasmic side of gastric H(+),K(+)-ATPase.British journal of pharmacology · 2001Article
- Biological significance of agmatine, an endogenous ligand at imidazoline binding sites.British journal of pharmacology · 2001Review
- In vitro mechanism of action on insulin release of S-22068, a new putative antidiabetic compound.British journal of pharmacology · 1999Article
- Protection by imidazol(ine) drugs and agmatine of glutamate-induced neurotoxicity in cultured cerebellar granule cells through blockade of NMDA receptor.British journal of pharmacology · 1999Article
- Multiple effector pathways regulate the insulin secretory response to the imidazoline RX871024 in isolated rat pancreatic islets.British journal of pharmacology · 1999Article
- Direct glucocorticoid inhibition of insulin secretion. An in vitro study of dexamethasone effects in mouse islets.The Journal of clinical investigation · 1997Article
- Elevation of cytosolic calcium by imidazolines in mouse islets of Langerhans: implications for stimulus-response coupling of insulin release.British journal of pharmacology · 1996Article
- The novel cardioprotective agent BMS-180448 activates a potassium conductance in cardiac and vascular smooth muscle.Naunyn-Schmiedeberg's archives of pharmacology · 1996Article
- Comparison of the cromakalim antagonism and bradycardic actions of a series of novel alinidine analogues in the rat.Naunyn-Schmiedeberg's archives of pharmacology · 1994Article
- The imidazoline site involved in control of insulin secretion: characteristics that distinguish it from I1- and I2-sites.British journal of pharmacology · 1994Article
- In vivo properties of SB 200646A, a 5-HT2C/2B receptor antagonist.British journal of pharmacology · 1994Article
- Antagonism of levcromakalim by imidazoline- and guanidine-derivatives in rat portal vein: involvement of the delayed rectifier.British journal of pharmacology · 1993Article
- Attenuation by phentolamine of hypoxia and levcromakalim-induced abbreviation of the cardiac action potential.British journal of pharmacology · 1993Article
- Antagonism of the stimulatory effects of efaroxan and glibenclamide in rat pancreatic islets by the imidazoline, RX801080.British journal of pharmacology · 1993Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Islets from normal mice were used to study the mechanisms by which imidazoline antagonists of alpha 2-adrenoceptors increase insulin release in vitro. 2. Alinidine, antazoline, phentolamine and tolazoline inhibited 86Rb efflux from islets perifused with a medium containing 3 mM glucose, i.e. under conditions where many adenosine 5'-triphosphate (ATP)-sensitive K+ channels are open in the beta-cell membrane. They also reduced the acceleration of 86Rb efflux caused by diazoxide, an opener of ATP-sensitive K+ channels. 3. ATP-sensitive and voltage-sensitive K+ currents were measured in single beta-cells by the whole-cell mode of the patch-clamp technique. Antazoline more markedly inhibited the ATP-sensitive than the voltage-sensitive current, an effect previously observed with phentolamine. Alinidine and tolazoline partially decreased the ATP-sensitive K+ current. 4. The four imidazolines reversed the inhibition of insulin release caused by diazoxide (through opening of ATP-sensitive K+ channels) or by clonidine (through activation of alpha 2-adrenoceptors) in a concentration-dependent manner. Only the former effect correlated with the ability of each drug to increase control insulin release stimulated by 15 mM glucose alone. 5. It is concluded that the ability of imidazoline antagonists of alpha 2-adrenoceptors to increase insulin release in vitro can be ascribed to their blockade of ATP-sensitive K+ channels in beta-cells rather than to their interaction with the adrenoceptor.
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