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Cholecystokinin Antagonist
A cholecystokinin receptor antagonist is a specific type of receptor antagonist which blocks the receptor sites for the peptide hormone cholecystokinin (CCK). Classification There are two subtypes of this receptor known at present, defined as CCKA and CCKB (also called CCK-1 and CCK-2, respectively). The CCKA receptor is mainly expressed in the small intestine, and is involved in the regulation of enzyme secretion by the pancreas, secretion of gastric acid in the stomach, intestinal motility and signaling of satiety (fullness). The CCKB receptor is expressed mainly in the central nervous system, and has functions relating to anxiety and the perception of pain. Antagonists for the CCK receptors can thus have multiple functions in both the gut and brain. Research The best known CCK receptor antagonist is the non-selective antagonist proglumide, which blocks both CCKA and CCKB receptors, and was originally developed for the treatment of stomach ulcers. This action derived fr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves ." '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, beta b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peptide
Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty amino acids are called oligopeptides, and include dipeptides, tripeptides, and tetrapeptides. Peptides fall under the broad chemical classes of biological polymers and oligomers, alongside nucleic acids, oligosaccharides, polysaccharides, and others. Proteins consist of one or more polypeptides arranged in a biologically functional way, often bound to ligands such as coenzymes and cofactors, to another protein or other macromolecule such as DNA or RNA, or to complex macromolecular assemblies. Amino acids that have been incorporated into peptides are termed residues. A water molecule is released during formation of each amide bond.. All peptides except cyclic peptides have an N-terminal (amine group) and C-terminal (carboxyl g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hormone
A hormone (from the Ancient Greek, Greek participle , "setting in motion") is a class of cell signaling, signaling molecules in multicellular organisms that are sent to distant organs or tissues by complex biological processes to regulate physiology and behavior. Hormones are required for the normal development of animals, plants and fungi. Due to the broad definition of a hormone (as a signaling molecule that exerts its effects far from its site of production), numerous kinds of molecules can be classified as hormones. Among the substances that can be considered hormones, are eicosanoids (e.g. prostaglandins and thromboxanes), steroids (e.g. Estrogen, oestrogen and brassinosteroid), amino acid derivatives (e.g. epinephrine and auxin), protein or peptides (e.g. insulin and CLE peptides), and gases (e.g. ethylene and nitric oxide). Hormones are used to communicate between organ (anatomy), organs and Tissue (biology), tissues. In vertebrates, hormones are responsible for regulating ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cholecystokinin
Cholecystokinin (CCK or CCK-PZ; from Greek ''chole'', "bile"; ''cysto'', "sac"; ''kinin'', "move"; hence, ''move the bile-sac (gallbladder)'') is a peptide hormone of the gastrointestinal system responsible for stimulating the digestion of fat and protein. Cholecystokinin, formerly called pancreozymin, is synthesized and secreted by enteroendocrine cells in the duodenum, the first segment of the small intestine. Its presence causes the release of pancreatic juice from the pancreas and bile from the gallbladder. History Evidence that the small intestine controls the release of bile was uncovered as early as 1856, when French physiologist Claude Bernard showed that when dilute acetic acid was applied to the orifice of the bile duct, the duct released bile into the duodenum. In 1903, the French physiologist showed that this reflex was not mediated by the nervous system. In 1904, the French physiologist Charles Fleig showed that the discharge of bile was mediated by a substance t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cholecystokinin A Receptor
The Cholecystokinin A receptor is a human protein, also known as CCKAR or CCK1, with CCK1 now being the IUPHAR-recommended name. Function This gene encodes a G-protein coupled receptor that binds sulfated members of the cholecystokinin (CCK) family of peptide hormones. This receptor is a major physiologic mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach. In the central and peripheral nervous system this receptor regulates satiety and the release of beta-endorphin and dopamine. The extracellular, N-terminal, protein domain, domain of this protein adopts a protein tertiary structure, tertiary structure consisting of a few Helix, helical turn (biochemistry), turns and a disulfide bond, disulfide-cross linked loop. It is required for interaction of the cholecystokinin A receptor with its corresponding Hormone, hormonal ligand (biochemistry), ligand. Selective Ligands Agonists * Cholecystokinin * CCK-4 * SR-146,131 * A-71623 - ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cholecystokinin B Receptor
The cholecystokinin B receptor also known as CCKBR or CCK2 is a protein that in humans is encoded by the ''CCKBR'' gene. This gene encodes a G protein-coupled receptor for gastrin and cholecystokinin (CCK), regulatory peptides of the brain and gastrointestinal tract. This protein is a type B gastrin receptor, which has a high affinity for both sulfated and nonsulfated CCK analogs and is found principally in the central nervous system and the gastrointestinal tract. A misspliced transcript variant including an intron has been observed in cells from colorectal and pancreatic tumors. CNS effects Cholecystokinin, CCK receptors significantly influence neurotransmission in the brain, regulating anxiety, feeding, and locomotion. CCK-B expression may correlate parallel to anxiety and depression phenotypes in humans. CCK-B receptors possess a complex regulation of dopamine activity in the brain. CCK-B activation appears to possess a general inhibitory action on dopamine activity in the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Proglumide
Proglumide, sold under the brand name Milid, is a drug that inhibits gastrointestinal motility Motility is the ability of an organism to move independently using metabolism, metabolic energy. This biological concept encompasses movement at various levels, from whole organisms to cells and subcellular components. Motility is observed in ... and reduces gastric secretions. It acts as a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. It was used mainly in the treatment of stomach ulcers, although it has now been largely replaced by newer drugs for this application. An interesting side effect of proglumide is that it enhances the analgesia produced by opioid drugs, and can prevent or even reverse the development of tolerance to opioid drugs. This can make it a useful adjuvant treatment to use alongside opioid drugs in the treatment of chronic pain conditions such as cancer, where opioid analgesics may be required for long periods and developm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzotript
Benzotript (), also known as ''N''-(''p''-chlorobenzoyl)-L-tryptophan, is a muscle relaxant that inhibits gastric secretion and was never marketed. It is a tryptamine derivative and the ''N''-(4-chlorobenzoyl) analogue of the amino acid tryptophan. Similarly to proglumide (''N''2-benzoyl-''N'',''N''-dipropyl-α-glutamine), the drug acts as a competitive Competition is a rivalry where two or more parties strive for a common goal which cannot be shared: where one's gain is the other's loss (an example of which is a zero-sum game). Competition can arise between entities such as organisms, indi ... and non-selective cholecystokinin receptor antagonist. Other more potent tryptophan derivatives have also been developed as cholecystokinin (CCK) antagonists. References 4-Chlorophenyl compounds Abandoned drugs Amino acids Cholecystokinin antagonists Muscle relaxants N-Acyltryptamines {{Gastrointestinal-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lorglumide
Lorglumide (CR-1409) is a drug which inhibits gastrointestinal motility and reduces gastric secretions, acting as a cholecystokinin antagonist, with fairly high selectivity for the CCKA subtype. It has been suggested as a potential treatment for a variety of gastrointestinal problems including stomach ulcers, irritable bowel syndrome, dyspepsia, constipation and pancreatitis, as well as some forms of cancer Cancer is a group of diseases involving Cell growth#Disorders, abnormal cell growth with the potential to Invasion (cancer), invade or Metastasis, spread to other parts of the body. These contrast with benign tumors, which do not spread. Po ..., but animal and human testing has produced inconsistent results and no clear therapeutic role has been established, although it is widely used in scientific research. References {{Drugs for peptic ulcer and GORD Cholecystokinin antagonists Chloroarenes Benzamides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Devazepide
Devazepide (L-364,718, MK-329) is benzodiazepine drug, but with quite different actions from most benzodiazepines, lacking affinity for GABAA receptors and instead acting as an CCKA receptor antagonist. It increases appetite and accelerates gastric emptying, and has been suggested as a potential treatment for a variety of gastrointestinal problems including dyspepsia, gastroparesis and gastric reflux. It is also widely used in scientific research into the CCKA receptor. Synthesis Devazepide is synthesised in a similar manner to other benzodiazepines. See also *Benzodiazepine *Cholecystokinin antagonist A cholecystokinin receptor antagonist is a specific type of receptor antagonist which blocks the receptor sites for the peptide hormone cholecystokinin (CCK). Classification There are two subtypes of this receptor known at present, defined as ... References {{Benzodiazepines Benzodiazepines Cholecystokinin antagonists Indoles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiety
Anxiety is an emotion characterised by an unpleasant state of inner wikt:turmoil, turmoil and includes feelings of dread over Anticipation, anticipated events. Anxiety is different from fear in that fear is defined as the emotional response to a present threat, whereas anxiety is the anticipation of a future one. It is often accompanied by nervous behavior such as pacing back and forth, Somatic anxiety, somatic complaints, and Rumination (psychology), rumination. Anxiety is a feeling of uneasiness and worry, usually generalized and unfocused as an overreaction to a situation that is only subjectively seen as menacing. It is often accompanied by muscular tension, restlessness, Fatigue (medical), fatigue, inability to catch one's breath, tightness in the abdominal region, nausea, and problems in concentration. Anxiety is closely related to fear, which is a response to a real or perceived immediate threat (fight-or-flight response); anxiety involves the expectation of a future t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Panic Attack
Panic attacks are sudden periods of intense fear and Comfort, discomfort that may include palpitations, otherwise defined as a Tachycardia, rapid, Arrhythmia, irregular Heart rate, heartbeat, Hyperhidrosis, sweating, chest pain or discomfort, shortness of breath, Tremor, trembling, dizziness, Hypoesthesia, numbness, confusion, or a sense of impending doom or loss of control. Typically, these symptoms are the worst within ten minutes of onset and can last for roughly 30 minutes, though they can vary anywhere from seconds to hours. While they can be extremely distressing, panic attacks themselves are not physically dangerous. The ''Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition'' (DSM-5) defines them as "an abrupt surge of intense fear or intense discomfort that reaches a peak within minutes and during which time four or more of the following symptoms occur." These symptoms include, but are not limited to, the ones mentioned above. Panic attacks function as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
