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Betazole
Betazole (also known as ametazole) is a histamine H2 receptor agonist. Betazole hydrochloride is known as gastramine and histalog. It has been used as a gastric stimulant to test for maximal production of gastric secretion activity. The test can be used in diagnosis of diseases such as Zollinger-Ellison syndrome where there is excess acid production, in this case driven by over production of gastrin. The volume of acid secretion is measured following administration of betazole, diagnosis being secretion greater than 60% of the maximal acid secretion following betazole stimulation. This procedure can lead to complications and should be avoided in subjects with coronary artery disease. It is also used in diagnosis of gastritis in association with a test for secretin activity. Betazole is used as a stimulant in preference to histamine because of its specificity for the H2 receptor and its advantage of not generating the undesirable side effects that histamine would induce. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Histamine H2 Receptor
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. Function Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3 and H4. The histamine receptor H2 belongs to the rhodopsin-like family of G protein-coupled receptors. It is an integral membrane protein and stimulates gastric acid secretion. It also regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation. Histamine may play a role in penile erection. Tissue distribution Histamine H2 receptors are expressed in the following tissues: ;Peripheral tissues *Gastric parietal cells (oxyn ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Betaxolol
Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and angina. Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta2 receptors) as timolol may. Betaxolol also shows greater affinity for beta1 receptors than metoprolol. In addition to its effect on the heart, betaxolol reduces the pressure within the eye (intraocular pressure). This effect is thought to be caused by reducing the production of the liquid (which is called the aqueous humor) within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma. It was patented in 1975 and approved for medical use in 1983. Medical uses Hypertension Betaxolol is most commonly ingested orally alone or with other medica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
Gastric Secretion
The stomach is a muscular, hollow organ in the gastrointestinal tract of humans and many other animals, including several invertebrates. The stomach has a dilated structure and functions as a vital organ in the digestive system. The stomach is involved in the gastric phase of digestion, following chewing. It performs a chemical breakdown by means of enzymes and hydrochloric acid. In humans and many other animals, the stomach is located between the oesophagus and the small intestine. The stomach secretes digestive enzymes and gastric acid to aid in food digestion. The pyloric sphincter controls the passage of partially digested food (chyme) from the stomach into the duodenum, where peristalsis takes over to move this through the rest of intestines. Structure In the human digestive system, the stomach lies between the oesophagus and the duodenum (the first part of the small intestine). It is in the left upper quadrant of the abdominal cavity. The top of the stomach lies against ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gastrin
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. Gastrin binds to cholecystokinin B receptors to stimulate the release of histamines in enterochromaffin-like cells, and it induces the insertion of K+/H+ ATPase pumps into the apical membrane of parietal cells (which in turn increases H+ release into the stomach cavity). Its release is stimulated by peptides in the Lumen (anatomy), lumen of the stomach. Physiology Genetics In humans, the ''GAS'' gene is located on the long arm of the seventeenth chromosome (17q21). Synthesis Gastrin is a linear peptide hormone produced by G cells of the duodenum and in the pyloric antrum of the stomach. It is secreted into the bloodstream. The encoded polypeptide is preprogastrin, which is cleaved by enzymes in posttranslational modification to produce progastr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Coronary Artery Disease
Coronary artery disease (CAD), also called coronary heart disease (CHD), ischemic heart disease (IHD), myocardial ischemia, or simply heart disease, involves the reduction of blood flow to the heart muscle due to build-up of atherosclerotic plaque An atheroma, or atheromatous plaque, is an abnormal and reversible accumulation of material in the inner layer of an arterial wall. The material consists of mostly macrophage cells, or debris, containing lipids, calcium and a variable amount ... in the arteries of the heart. It is the most common of the cardiovascular diseases. Types include stable angina, unstable angina, myocardial infarction, and sudden cardiac death. A common symptom is chest pain or discomfort which may travel into the shoulder, arm, back, neck, or jaw. Occasionally it may feel like heartburn. Usually symptoms occur with exercise or emotional Stress (psychological), stress, last less than a few minutes, and improve with rest. Shortness of breath may also o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gastritis
Gastritis is inflammation of the lining of the stomach. It may occur as a short episode or may be of a long duration. There may be no symptoms but, when symptoms are present, the most common is upper abdominal pain (see dyspepsia). Other possible symptoms include nausea and vomiting, bloating, loss of appetite and heartburn. Complications may include stomach bleeding, stomach ulcers, and stomach tumors. When due to autoimmune problems, low red blood cells due to not enough vitamin B12 may occur, a condition known as pernicious anemia. Common causes include infection with '' Helicobacter pylori'' and use of nonsteroidal anti-inflammatory drugs ( NSAIDs). Less common causes include alcohol, smoking, cocaine, severe illness, autoimmune problems, radiation therapy and Crohn's disease. Endoscopy, a type of X-ray known as an upper gastrointestinal series, blood tests, and stool tests may help with diagnosis. The symptoms of gastritis may be a presentation of a myocardial infarcti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Secretin
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. Secretin helps regulate the pH of the duodenum by (1) inhibiting the secretion of gastric acid from the parietal cells of the stomach and (2) stimulating the production of bicarbonate from the ductal cells of the pancreas. It also stimulates the secretion of bicarbonate and water by cholangiocytes in the bile duct, protecting it from bile acids by controlling the pH and promoting the flow in the duct. Meanwhile, in concert with secretin's actions, the other main hormone simultaneously issued by the duodenum, cholecystokinin (CCK), is stimulating the gallbladder to contract, delivering its stored bile. Prosecretin is a precursor to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nizatidine
Nizatidine is a histamine H2 receptor antagonist that inhibits stomach acid production, and is commonly used in the treatment of peptic ulcer disease and gastroesophageal reflux disease. It was patented in 1980 and approved for medical use in 1988. It was developed by Eli Lilly. Brand names include Tazac and Axid. Medical use Nizatidine is used to treat duodenal ulcers, gastric ulcers, and gastroesophageal reflux disease (GERD/GORD), and to prevent stress ulcers. Adverse effects Side effects are uncommon, usually minor, and include diarrhea, constipation, fatigue, drowsiness, headache, and muscle aches. History and development Nizatidine was developed by Eli Lilly, and was first marketed in 1988. It is considered to be equipotent with ranitidine and differs by the substitution of a thiazole ring in place of the furan ring in ranitidine. In September 2000, Eli Lilly announced they would sell the sales and marketing rights for Axid to Reliant Pharmaceuticals. Subsequently, Re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amines
In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines). Important amines include amino acids, biogenic amines, trimethylamine, and aniline; Inorganic derivatives of ammonia are also called amines, such as monochloramine (). The substituent is called an amino group. Compounds with a nitrogen atom attached to a carbonyl group, thus having the structure , are called amides and have different chemical properties from amines. Classification of amines Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
