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Receptors, Drug (3)


Articles on Receptors, Drug

  1. Variations in tissue selectivity amongst insulin secretagogues: a systematic review.

    Diabetes Metab 14(2):130-8 (2012) PMID 21923736

    Insulin secretagogues promote insulin release by binding to sulfonylurea receptors on pancreatic β-cells (SUR1). However, these drugs also bind to receptor isoforms on cardiac myocytes (SUR2A) and vascular smooth muscle (SUR2B). Binding to SUR2A/SUR2B may inhibit ischaemic precondit...
  2. Successful treatment of congenital hyperinsulinism with long-acting release octreotide.

    Eur J Endocrinol 166(2):333-9 (2012) PMID 22048969

    Congenital hyperinsulinism (HI) is a common cause of hypoglycemia in infancy. The medical treatment of diazoxide-unresponsive HI is based on a somatostatin analogue. This study aims at replacing three daily s.c. octreotide (Sandostatin, Novartis) injections by a singl...
  3. Treating diabetes today: a matter of selectivity of sulphonylureas.

    Diabetes Metab (2012) PMID 22118705

    It is well known that sulphonylureas (SUs), commonly used in the treatment of type 2 diabetes mellitus, stimulate insulin secretion by closing ATP-sensitive K(+) (K(ATP) ) channels in pancreatic β-cells by binding to the SU receptor SUR1. SUs are now known also to activate cAMP sens...
  4. Unique properties of the ATP-sensitive K⁺ channel in the mouse ventricular cardiac conduction system.

    Circ Arrhythm Electrophysiol 4(6):926-35 (2011) PMID 21984445

    We recorded K(ATP) channels in isolated CCS myocytes using Cntn2-EGFP reporter mice. The CCS K(ATP) channels were less sensitive to inhibitory cytosolic ATP compared with ventricular channels and more strongly activated by MgADP. They also had a smaller slope conductance. The 2 types of channels had...
  5. [An asymptomatic chronic hypokalaemia].

    Ann Biol Clin (Paris) 69(4):459-64 (2011) PMID 21896412

    We report the case of an asymptomatic patient presenting a severe chronic renal hypokalaemia. Once being sure of no diuretics use, two hypothesis can be mentioned for a normotensive patient presenting an hypokalaemia associated with a metabolic alcalosis: Bartter syndrome or Gitelman syndrome. The h...
  6. Pendrin as a novel target for diuretic therapy.

    Cell Physiol Biochem 28(3):521-6 (2011) PMID 22116366

    The Cl(-)/HCO(3)(-) exchanger pendrin (SLC26A4, PDS) and the thiazide-sensitive NaCl cotransporter NCC (SLC12A3) are expressed on the apical membranes of distal nephron segments and mediate salt absorption, with pendrin working in tandem with the epithelial Na channel (ENaC) and NCC...
  7. Clinical characteristics of recessive and dominant congenital hyperinsulinism due to mutation(s) in the ABCC8/KCNJ11 genes encoding the ATP-...

    J Pediatr Endocrinol Metab 24(11-12):1019-23 (2011) PMID 22308858

    We report the clinical and genetic characteristics of five patients with neonatal HH, three had recessively inherited K(ATP) channel mutations and two with a dominantly acting mutation. As a result of failure to medical therapy, patients with recessive K(ATP) channel mutations underwent a near total...
  8. Lasting 18F-DOPA PET uptake after clinical remission of the focal form of congenital hyperinsulinism.

    Horm Res Paediatr 76(4):286-90 (2011) PMID 21912073

    Positron emission tomography (PET) using (18)F-DOPA is a useful tool for detecting the focal forms of congenital hyperinsulinism. (18)F-DOPA is taken up by aromatic L-amino acid decarboxylase in pancreatic β-cells. However, the role of this enzyme in insulin secretion is unknown....
  9. Diazoxide maintenance of myocyte volume and contractility during stress: Evidence for a non-sarcolemmal K"A"T"P channel location

    J Thorac Cardiovasc Surg 140(5):7 (2010) PMID 20804990

    Animal and human myocytes demonstrate significant swelling and reduced contractility during exposure to stress (metabolic inhibition, hyposmotic stress, or hyperkalemic cardioplegia), and these detrimental consequences may be inhibited by the addition of diazoxide (adenosine triphosp...
  10. Decreased ENaC expression compensates the increased NCC activity following inactivation of the kidney-specific isoform of WNK1 and prevents ...

    Proc Natl Acad Sci U S A 107(42):18109-14 (2010) PMID 20921400 PMCID PMC2964238

    We show here that this isoform is an important regulator of sodium transport. KS-WNK1(-/-) mice display an increased activity of the Na-Cl cotransporter NCC, expressed specifically in the distal convoluted tubule, where it participates in the fine tuning of sodium reabsorption. Moreover, the express...