Lupitidine

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Lupitidine
Lupitidine.svg
Clinical data
ATC code
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CAS Number
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Chemical and physical data
Formula C21H27N5O2S
Molar mass 413.54 g·mol−1
3D model (JSmol)

Lupitidine (INN; lupitidine hydrochloride (USAN); development code SKF-93479) is a long-acting H2 receptor antagonist [1] developed by Smith, Kline & French and described as an antiulcerogenic that was never marketed. [2] It was shown to inhibit nocturnal gastric acid secretion [3] and, in experiments on rodents, produced diffuse neuroendocrine cell hyperplasia and an increase in multifocal glandular hyperplasia due to hypergastrinemia resulting from the pharmacological suppression of gastric acid secretion. [4]

Related Research Articles

Secretin Hormone involved in stomach, pancreas and liver secretions

Secretin is a hormone that regulates water homeostasis throughout the body and influences the environment of the duodenum by regulating secretions in the stomach, pancreas, and liver. It is a peptide hormone produced in the S cells of the duodenum, which are located in the intestinal glands. In humans, the secretin peptide is encoded by the SCT gene.

H<sub>2</sub> antagonist Drugs that selectively bind to but do not activate histamine h2 receptors.

H2 antagonists, sometimes referred to as H2RAs and also called H2 blockers, are a class of medications that block the action of histamine at the histamine H2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid. H2 antagonists can be used in the treatment of dyspepsia, peptic ulcers and gastroesophageal reflux disease. They have been surpassed by proton pump inhibitors (PPIs); the PPI omeprazole was found to be more effective at both healing and alleviating symptoms of ulcers and reflux oesophagitis than the H2 blockers ranitidine and cimetidine.

Zollinger–Ellison syndrome Condition in which tumours stimulate excessive gastric acid production

Zollinger–Ellison syndrome is a disease in which tumors cause the stomach to produce too much acid, resulting in peptic ulcers. Symptoms include abdominal pain and diarrhea.

Histamine chemical compound

Histamine is an organic nitrogenous compound involved in local immune responses, as well as regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. Histamine is involved in the inflammatory response and has a central role as a mediator of itching. As part of an immune response to foreign pathogens, histamine is produced by basophils and by mast cells found in nearby connective tissues. Histamine increases the permeability of the capillaries to white blood cells and some proteins, to allow them to engage pathogens in the infected tissues. It consists of an imidazole ring attached to an ethylamine chain; under physiological conditions, the amino group of the side-chain is protonated.

Gastrin mammalian protein found in Homo sapiens

Gastrin is a peptide hormone that stimulates secretion of gastric acid (HCl) by the parietal cells of the stomach and aids in gastric motility. It is released by G cells in the pyloric antrum of the stomach, duodenum, and the pancreas.

Famotidine Chemical compound (medication)

Famotidine, sold under the brand name Pepcid among others, is a medication that decreases stomach acid production. It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. It is taken by mouth or by injection into a vein. It begins working within an hour.

Ghrelin peptide hormone involved in appetite regulation

Ghrelin is a circulating hormone produced by enteroendocrine cells of the gastrointestinal tract, especially the stomach, and is often called a "hunger hormone" because it increases food intake. Blood levels of ghrelin are highest before meals when hungry, returning to lower levels after mealtimes. Ghrelin may help prepare for food intake by increasing gastric motility and gastric acid secretion.

Achlorhydria medical state where the production of hydrochloric acid in gastric secretions of the stomach and other digestive organs is absent or low

Achlorhydria, also known as hypochlorhydria, refers to states where the production of hydrochloric acid in gastric secretions of the stomach and other digestive organs is absent or low, respectively. It is associated with various other medical problems.

Cimetidine introduction

Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid production. It is mainly used in the treatment of heartburn and peptic ulcers.

Enterochromaffin-like cell

Enterochromaffin-like cells or ECL cells are a type of neuroendocrine cell found in the gastric glands of the gastric mucosa beneath the epithelium, in particular in the vicinity of parietal cells, that aid in the production of gastric acid via the release of histamine. They are also considered a type of enteroendocrine cell.

Motilin chemical compound

Motilin is a 22-amino acid polypeptide hormone in the motilin family that, in humans, is encoded by the MLN gene.

Histamine H<sub>2</sub> receptor mammalian protein found in Homo sapiens

H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of protein kinase A. PKA functions to phosphorylate certain proteins, affecting their activity. The drug betazole is an example of a histamine H2 receptor agonist.

Roxatidine acetate is a specific and competitive histamine H2 receptor antagonist drug that is used to treat gastric ulcers, Zollinger–Ellison syndrome, erosive esophagitis, gastro-oesophageal reflux disease, and gastritis.

The endocannabinoid system (ECS) is a biological system composed of endocannabinoids, which are endogenous lipid-based retrograde neurotransmitters that bind to cannabinoid receptors (CBRs), and cannabinoid receptor proteins that are expressed throughout the vertebrate central nervous system and peripheral nervous system. The endocannabinoid system remains under preliminary research, but may be involved in regulating physiological and cognitive processes, including fertility, pregnancy, pre- and postnatal development, various activity of immune system, appetite, pain-sensation, mood, and memory, and in mediating the pharmacological effects of cannabis.

Gastric hydrogen potassium ATPase, also known as H+/K+ ATPase, is an enzyme which functions to acidify the stomach. It is a member of the P-type ATPases, also known as E1-E2 ATPases due to its two states.

Antihistamine Drug that binds to but does not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists

Antihistamines are drugs which treat allergic rhinitis and other allergies. Typically people take antihistamines as an inexpensive, generic, over-the-counter drug that can provide relief from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use.

Cholecystokinin A receptor protein-coding gene in the species Homo sapiens

The Cholecystokinin A receptor is a human protein, also known as CCKAR or CCK1, with CCK1 now being the IUPHAR-recommended name.

GPR35 protein-coding gene in the species Homo sapiens

G protein-coupled receptor 35 also known as GPR35 is a G protein-coupled receptor which in humans is encoded by the GPR35 gene. Heightened expression of GPR35 is found in immune and gastrointestinal tissues, including the crypts of Lieberkühn.

A cholecystokinin antagonist is a specific type of receptor antagonist which blocks the receptor sites for the peptide hormone cholecystokinin (CCK).

Proton pump inhibitors (PPIs) block the gastric hydrogen potassium ATPase (H+/K+ ATPase) and inhibit gastric acid secretion. These drugs have emerged as the treatment of choice for acid-related diseases, including gastroesophageal reflux disease (GERD) and peptic ulcer disease. PPIs also can bind to other types of proton pumps such as those that occur in cancer cells and are finding applications in the reduction of cancer cell acid efflux and reduction of chemotherapy drug resistance.

References

  1. Franzén L, Ghassemifar R, Malcherek P (July 1991). "Experimental mast cell activation improves connective tissue repair in the perforated rat mesentery". Agents and Actions. 33 (3–4): 371–7. doi:10.1007/bf01986588. PMID   1683107. S2CID   23827166.
  2. Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 745–. ISBN   978-1-4757-2085-3.
  3. Dammann HG, Müller P, Simon B (January 1982). "Inhibition of nocturnal acid secretion by H2-receptor-antagonist SKF 93479". Lancet. 1 (8265): 224. doi:10.1016/S0140-6736(82)90788-7. PMID   6119582. S2CID   5525326.
  4. Betton GR, Dormer CS, Wells T, Pert P, Price CA, Buckley P (1 February 1988). "Gastric ECL-cell hyperplasia and carcinoids in rodents following chronic administration of H2-antagonists SK&F 93479 and oxmetidine and omeprazole". Toxicologic Pathology. 16 (2): 288–98. doi: 10.1177/019262338801600222 . PMID   2903544.