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Casokefamide
Casokefamide (INN), also known as β-casomorphin 4027 (β-CM-4027) and D-Ala2,4,Tyr5.html" ;"title="small>D-Ala2,4,Tyr5">small>D-Ala2,4,Tyr5β-casomorphin-5-amide, is a peripherally-specific, synthetic opioid pentapeptide with the amino acid sequence Tyr-D-Ala-Phe-D-Ala-Tyr-NH2. Derived from the β-casomorphin sequence, it was designed with the intention of improving resistance to digestive enzymes so that it could be used as an antidiarrheal medicine. Unlike other casomorphins, which are generally selective μ-opioid receptor agonists, casokefamide binds to both the μ- and δ-opioid receptors. In a clinical study, casokefamide was found to be effective via the oral route for the treatment of chronic diarrhea, and did not produce any side effects. However, further clinical development was not pursued and it was never marketed. See also * Morphiceptin * Frakefamide Frakefamide (INN) is a synthetic, fluorinated linear tetrapeptide with the amino acid sequence Tyr-D-Ala-(' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Frakefamide
Frakefamide (INN) is a synthetic, fluorinated linear tetrapeptide with the amino acid sequence Tyr-D-Ala-(''p''-F)Phe-Phe-NH2 which acts as a peripherally-specific, selective μ-opioid receptor agonist. Despite its inability to penetrate the blood-brain-barrier and enter the central nervous system, frakefamide has potent analgesic effects and, unlike centrally-acting opioids like morphine, does not produce respiratory depression, indicating that its antinociceptive effects are mediated by peripheral μ-opioid receptors. It was under development for the treatment of pain by AstraZeneca and Shire but was shelved after phase II clinical trials. See also * Casokefamide Casokefamide (INN), also known as β-casomorphin 4027 (β-CM-4027) and D-Ala2,4,Tyr5.html" ;"title="small>D-Ala2,4,Tyr5">small>D-Ala2,4,Tyr5β-casomorphin-5-amide, is a peripherally-specific, synthetic opioid pentapeptide with the amino acid se ... * Metkefamide References {{Opioidergics Analgesics ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Morphiceptin
Morphiceptin is a tetrapeptide (Tyr-Pro-Phe-Pro-NH2) that is a selective μ-opioid receptor agonist. It is derived from β-casomorphin and has over 1,000 times selectivity for μ- over δ-opioid receptors. When injected intracerebroventricularly (into the ventricular system of the brain), morphiceptin had an analgesic ED50 of 1.7 nmol per animal. The analgesic effects of morphiceptin were reversed by naloxone, meaning that the analgesic effect is mediated by the μ-opioid receptor. Morphiceptin is the (1S,2S,3S,4S)-form whereas deproceptin is the (1S,2S,3S,4R)-form 4799-23-5 See also * Casokefamide Casokefamide ( INN), also known as β-casomorphin 4027 (β-CM-4027) and D-Ala2,4,Tyr5.html" ;"title="small>D-Ala2,4,Tyr5">small>D-Ala2,4,Tyr5β-casomorphin-5-amide, is a peripherally-specific, synthetic opioid pentapeptide with the amino acid s ... References {{Opioidergics Analgesics Opioid peptides Tetrapeptides ... [...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 |
Opioid Peptides
Opioid peptides are peptides that bind to opioid receptors in the brain; opiates and opioids mimic the effect of these peptides. Such peptides may be produced by the body itself, for example endorphins. The effects of these peptides vary, but they all resemble those of opiates. Brain opioid peptide systems are known to play an important role in motivation, emotion, attachment behaviour, the response to stress and pain, control of food intake, and the rewarding effects of alcohol and nicotine. Opioid-like peptides may also be absorbed from partially digested food (casomorphins, exorphins, and rubiscolins). The opioid food peptides have lengths of typically 4–8 amino acids. The body's own opioids are generally much longer. Opioid peptides are released by post-translational proteolytic cleavage of precursor proteins. The precursors consist of the following components: a signal sequence that precedes a conserved region of about 50 residues; a variable-length region; and the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidiarrhoeals
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] |
Side Effect
In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequences of the use of a drug. Developing drugs is a complicated process, because no two people are exactly the same, so even drugs that have virtually no side effects, might be difficult for some people. Also, it is difficult to make a drug that targets one part of the body but that does not affect other parts, the fact that increases the risk of side effects in the untargeted parts. Occasionally, drugs are prescribed or procedures performed specifically for their side effects; in that case, said side effect ceases to be a side effect and is now an intended effect. For instance, X-rays were historically (and are currently) used as an imaging technique; the discovery of their oncolytic capability led to their employ in radiotherapy (ablation o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diarrhea
Diarrhea, also spelled diarrhoea, is the condition of having at least three loose, liquid, or watery bowel movements each day. It often lasts for a few days and can result in dehydration due to fluid loss. Signs of dehydration often begin with loss of the normal stretchiness of the skin and irritable behaviour. This can progress to decreased urination, loss of skin color, a fast heart rate, and a decrease in responsiveness as it becomes more severe. Loose but non-watery stools in babies who are exclusively breastfed, however, are normal. The most common cause is an infection of the intestines due to either a virus, bacterium, or parasite—a condition also known as gastroenteritis. These infections are often acquired from food or water that has been contaminated by feces, or directly from another person who is infected. The three types of diarrhea are: short duration watery diarrhea, short duration bloody diarrhea, and persistent diarrhea (lasting more than two weeks, w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Study
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
δ-opioid Receptor
The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous ligands. The regions of the brain where the δ-opioid receptor is largely expressed vary from species model to species model. In humans, the δ-opioid receptor is most heavily expressed in the basal ganglia and neocortical regions of the brain. Function The endogenous system of opioid receptors is well known for its analgesic potential; however, the exact role of δ-opioid receptor activation in pain modulation is largely up for debate. This also depends on the model at hand since receptor activity is known to change from species to species. Activation of delta receptors produces analgesia, perhaps as significant potentiators of μ-opioid receptor agonists. However, it seems like delta agonism provides heavy potentiation to any mu agonism. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
μ-opioid Receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical μ-opioid receptor agonist is morphine, the primary psychoactive alkaloid in opium. It is an inhibitory G-protein coupled receptor that activates the Gi alpha subunit, inhibiting adenylate cyclase activity, lowering cAMP levels. Structure The structure of the μ-opioid receptor has been determined with the antagonist β-FNA, the agonist BU72, and in a complex with DAMGO and Gi protein. Splice variants Three variants of the μ-opioid receptor are well characterized, though RT-PCR has identified up to 10 total splice variants in humans. Location They can exist either presynaptically or postsynaptically depending upon cell types. The μ-opioid receptors exist mostly presynaptically in the periaqueductal gray region, and in the superfi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peripheral
A peripheral or peripheral device is an auxiliary device used to put information into and get information out of a computer. The term ''peripheral device'' refers to all hardware components that are attached to a computer and are controlled by the computer system, but they are not the core components of the computer, such as the CPU or power supply unit. In other words, peripherals can also be defined as devices that can be easily removed and plugged into a computer system. Several categories of peripheral devices may be identified, based on their relationship with the computer: *An ''input device'' sends data or instructions to the computer, such as a mouse, keyboard, graphics tablet, image scanner, barcode reader, game controller, light pen, light gun, microphone and webcam; *An ''output device'' provides output data from the computer, such as a computer monitor, projector, printer, headphones and computer speaker; *An ''input/output device'' performs both input and output fun ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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