RB-3007

	RB-3007 RB-3007 is an orally active analogue of RB-101. It acts as an enkephalinase inhibitor, which is used in scientific research. See also * RB-101 - enkephalinase inhibitor that produces analgesia without respiratory depression * D/DL-Phenylalanine - D-phenylalanine blockage of enkephalin degradation may be responsible for the reputed analgesic effect of DL-Phenylalanine * Racecadotril - an antidiarrheal drug which acts as a peripheral enkephalinase inhibitor * Ecadotril - a neutral endopeptidase inhibitor An endopeptidase inhibitor is a drug that inhibits one or more endopeptidase enzymes. Endopeptidases are one of two types of proteases (enzymes that break down proteins and peptides), the other being exopeptidases. Endopeptidases cleave peptide bond ... References {{reflist Enkephalinase inhibitors Organophosphates ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	RB-101 RB-101 is a drug that acts as an enkephalinase inhibitor, which is used in scientific research. RB-101 is a prodrug which acts by splitting at the disulfide bond once inside the brain, to form two selective enzyme inhibitors and blocking both types of the zinc-metallopeptidase enkephalinase enzymes. This inhibits the breakdown of the endogenous opioid peptides known as enkephalins. These two enzymes, aminopeptidase N (APN) and neutral endopeptidase 24.11 (NEP), are responsible for the breakdown of both kinds of enkephalin naturally found in the body, and so RB-101 causes a buildup of both Met-enkephalin and Leu-enkephalin. These peptides act primarily at the delta opioid receptor, although they also stimulate the mu opioid receptor to some extent through a delta-opioid receptor mediated interaction with another peptide cholecystokinin, and the enzyme-inhibiting effects of RB-101 thus produce indirect stimulation of both of these opioid receptor subtypes. This causes RB-101 to be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Enkephalinase Inhibitor An enkephalinase inhibitor is a type of enzyme inhibitor which inhibits one or more members of the enkephalinase class of enzymes that break down the endogenous enkephalin opioid peptides. Examples include racecadotril, ubenimex (bestatin), RB-101, and D-phenylalanine, as well as the endogenous opioid peptides opiorphin and spinorphin. It also includes RB-3007, Semax and Selank. Analgesic, anticraving, antidepressant, anxiolytic, and antidiarrheal effects are common properties of enkephalinase inhibitors. See also * Enkephalinase * Enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin ... References Analgesics Antidiarrhoeals {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Respiratory Depression Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide (hypercapnia) and respiratory acidosis. Hypoventilation is not synonymous with respiratory arrest, in which breathing ceases entirely and death occurs within minutes due to hypoxia and leads rapidly into complete anoxia, although both are medical emergencies. Hypoventilation can be considered a precursor to hypoxia and its lethality is attributed to hypoxia with carbon dioxide toxicity. Causes Hypoventilation may be caused by: A medical condition such as stroke affecting the brainstem Voluntary breath-holding or underbreathing, for example, hypoventilation training or the Buteyko method. Medication or drugs, typically when taken in accidental or intentional overdose. Opioids and benzodiazepines in particular are known to cause respiratory depress ... [...More Info...] [...Related Items...] OR:* [Wikipedia] [Google] [Baidu]
	Phenylalanine Phenylalanine (symbol Phe or F) is an essential α-amino acid with the formula . It can be viewed as a benzyl group substituted for the methyl group of alanine, or a phenyl group in place of a terminal hydrogen of alanine. This essential amino acid is classified as neutral, and nonpolar because of the inert and hydrophobic nature of the benzyl side chain. The L-isomer is used to biochemically form proteins coded for by DNA. Phenylalanine is a precursor for tyrosine, the monoamine neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline), and the skin pigment melanin. It is encoded by the codons UUU and UUC. Phenylalanine is found naturally in the milk of mammals. It is used in the manufacture of food and drink products and sold as a nutritional supplement for its analgesic and antidepressant effects. It is a direct precursor to the neuromodulator phenethylamine, a commonly used dietary supplement. As an essential amino acid, phenylalanine is n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Enkephalin An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin have been found, one containing leucine ("leu"), and the other containing methionine ("met"). Both are products of the proenkephalin gene. * Met-enkephalin is Tyr-Gly-Gly-Phe-Met. * Leu-enkephalin has Tyr-Gly-Gly-Phe-Leu. Endogenous opioid peptides There are three well-characterized families of opioid peptides produced by the body: enkephalins, B-endorphin, and dynorphins. The met-enkephalin peptide sequence is coded for by the enkephalin gene; the leu-enkephalin peptide sequence is coded for by both the enkephalin gene and the dynorphin gene. The proopiomelanocortin gene (POMC) also contains the met-enkephalin sequence on the N-terminus of beta-endorphin, but the endorphin peptide is not processed into enkephalin. Effects on stress ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
picture info	Analgesic An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
picture info	Racecadotril Racecadotril, also known as acetorphan, is an antidiarrheal medication which acts as a peripheral enkephalinase inhibitor. Unlike other opioid medications used to treat diarrhea, which reduce intestinal motility, racecadotril has an antisecretory effect — it reduces the secretion of water and electrolytes into the intestine. It is available in France (where it was first introduced in ~1990) and other European countries (including Germany, Italy, the United Kingdom, Spain, Portugal, Poland, Finland, Russia and the Czech Republic) as well as most of South America and some South East Asian countries (including China, India and Thailand), but not in the United States. It is sold under the tradename Hidrasec, among others. Thiorphan is the active metabolite of racecadotril, which exerts the bulk of its inhibitory actions on enkephalinases. Medical uses Racecadotril is used for the treatment of acute diarrhea in children and adults and has better tolerability than loperamide, as i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Antidiarrheal An anti-diarrhoeal drug (or anti-diarrheal drug in American English) is any medication which provides symptomatic relief for diarrhoea. Types * Electrolyte solutions, while not true antidiarrhoeals, are used to replace lost fluids and salts in acute cases. * Bulking agents like methylcellulose, guar gum or plant fibre (bran, sterculia, isabgol, etc.) are used for diarrhoea in functional bowel disease and to control ileostomy output. * Absorbents absorb toxic substances that cause infective diarrhoea, methylcellulose is an absorbent. * Anti-inflammatory compounds such as bismuth subsalicylate. * Anticholinergics reduce intestinal movement and are effective against both diarrhoea and accompanying cramping. * Opioids' classical use besides pain relief is as an anti-diarrhoeal drug. Opioids have agonist actions on the intestinal opioid receptors, which when activated cause constipation. Drugs such as morphine or codeine can be used to relieve diarrhoea this way. A notable opioid fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Ecadotril Ecadotril is a neutral endopeptidase inhibitor ((NEP) EC 3.4.24.11) and determined by the presence of peptidase family M13 as a neutral endopeptidase inhibited by phosphoramidon. Ecadotril is the (''S'')-enantiomer of racecadotril. NEP-like enzymes include the endothelin- converting enzymes. The peptidase M13 family believed to activate or inactivate oligopeptide (pro)-hormones such as opioid peptides, neprilysin is another member of this group, in the case of the metallopeptidases and aspartic, the nucleophiles clan or family for example MA, is an activated water molecule. The peptidase domain for members of this family also contains a bacterial member and resembles that of thermolysin the predicted active site residues for members of this family and thermolysin occur in the motif HEXXH. Thermolysin complexed with the inhibitor (''S'')-thiorphan are isomeric thiol-containing inhibitors of endopeptidase EC 24-11 (also called "enkephalinase"). See also * RB-101 * Candoxatril ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Endopeptidase Inhibitor An endopeptidase inhibitor is a drug that inhibits one or more endopeptidase enzymes. Endopeptidases are one of two types of proteases (enzymes that break down proteins and peptides), the other being exopeptidases. Endopeptidases cleave peptide bonds of non-terminal amino acids (that is, they cut proteins/peptides into two chains), whereas exopeptidases break terminal bonds, resulting in the release of a single amino acid or dipeptide from the peptide chain. Examples of endopeptidase inhibitors Some examples of endopeptidase inhibitors include the following: * Neprilysin inhibitors Selective neprilysin inhibitors * Candoxatril - prodrug to candoxatrilat * Candoxatrilat - active metabolite of candoxatril * Dexecadotril (retorphan) - (''R'')-enantiomer of racecadotril; prodrug to (''R'')-thiorphan * Ecadotril (sinorphan) - (''S'')-enantiomer of racecadotril; prodrug to (''S'')-thiorphan * Racecadotril (acetorphan) - racemic form of dexecadotril and ecadotril; prodr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Enkephalinase Inhibitors Enkephalinases are enzymes that degrade endogenous enkephalin opioid peptides. They include: * Aminopeptidase N (APN) * Neutral endopeptidase (NEP) * Dipeptidyl peptidase 3 (DPP3) * Carboxypeptidase A6 (CPA6) * Leucyl/cystinyl aminopeptidase (LNPEP) * Angiotensin-converting enzyme (ACE) See also * Enkephalinase inhibitor * Oxytocinase Oxytocinase is a type of enzyme that metabolizes the endogenous neuropeptide, oxytocin. The most well-characterized oxytocinase is leucyl/cystinyl aminopeptidase, which is also an enkephalinase. Other oxytocinases are also known. During pregnancy, o ... References Hydrolases Human proteins Nociception {{Enzyme-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]