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Misoprostol is used for the prevention of NSAID-induced gastric ulcers.It acts upon gastric parietal cells, inhibiting the secretion of gastric acid by G-protein coupled receptor-mediated inhibition of adenylate cyclase, which leads to decreased intracellular cyclic AMP levels and decreased proton pump activity at the apical surface of the parietal cell.
These new agents can in a reversible and competitive fashion inhibit the final step in the gastric acid secretion with respect to K + binding to the parietal cell gastric H + /K + ATPase. That is, they block the action of the H + /K + ATPase by binding to or near the site of the K + channel. Since the binding is competitive and reversible these ...
A canaliculus is an adaptation found on gastric parietal cells. It is a deep infolding, or little channel, which serves to increase the surface area, e.g. for secretion. The parietal cell membrane is dynamic; the numbers of canaliculi rise and fall according to secretory n
The PPIs are given in an inactive form, which is neutrally charged and readily crosses cell membranes into intracellular compartments (like the parietal cell canaliculus) with acidic environments. In an acid environment, the inactive drug is protonated and rearranges into its active form.
Ball-and-stick model of cimetidine, the prototypical H 2 receptor antagonist. H 2 antagonists, sometimes referred to as H2RAs [1] and also called H 2 blockers, are a class of medications that block the action of histamine at the histamine H 2 receptors of the parietal cells in the stomach.
Prostaglandin EP 3 receptor (EP 3, 53kDa), is a prostaglandin receptor for prostaglandin E 2 (PGE 2) encoded by the human gene PTGER3; [5] it is one of four identified EP receptors, the others being EP 1, EP 2, and EP 4, all of which bind with and mediate cellular responses to PGE 2 and also, but generally with lesser affinity and responsiveness, certain other prostanoids (see Prostaglandin ...
Prostaglandin analogues such as misoprostol are used in treatment of duodenal and gastric ulcers. [2] Misoprostol and other prostaglandin analogues protect the lining of the gastrointestinal tract from harmful stomach acid and are especially indicated for the elderly on continuous doses of NSAIDs.
The hydrogen potassium ATPase is activated indirectly by gastrin that causes ECL cells to release histamine. [11] The histamine binds to H2 receptors on the parietal cell, activating a cAMP-dependent pathway which causes the enzyme to move from the cytoplasmic tubular membranes to deeply folded canaliculi of the stimulated parietal cell. [2]