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Signaling Peptide Receptor
Signaling peptide receptor is a type of receptor (biochemistry), receptor which binds one or more signaling peptides or signaling proteins. An example is the tropomyosin receptor kinase B (TrkB), which is bound and activated by the neurotrophin, neurotrophic protein brain-derived neurotrophic factor (BDNF). Another example is the μ-opioid receptor (MOR), which is bound and activated by the opioid peptide, opioid peptide hormone β-endorphin. Adiponectin receptor AdipoR1 * Agonists ** Peptide *** Adiponectin *** ADP-355 *** ADP-399 ** Non-peptide *** AdipoRon *** (–)-Arctigenin *** Arctiin *** Gramine *** Matairesinol * Antagonists ** Peptide *** ADP-400 AdipoR2 * Agonists ** Peptide *** Adiponectin *** ADP-355 *** ADP-399 ** Non-peptide *** AdipoRon *** Deoxyschizandrin *** Parthenolide *** Syringing (drug), Syringing *** Taxifoliol * Antagonists ** Peptide *** ADP-400 Angiotensin receptor Bradykinin receptor * Agonists ** Bradykinin ** Kallidin * Antagonis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and Signal_transduction, transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses, such as a change in the electrophysiology, electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter, inhibits electrical activity of neurons by binding to GABAA receptor, GABA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand (biochemistry), ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G prote ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gramine
Gramine (also called donaxine) is a naturally occurring indole alkaloid present in several plant species. Gramine may play a defensive role in these plants, since it is toxic to many organisms. Occurrence Gramine has been found in the giant reed, ''Arundo donax'', ''Acer saccharinum'' (Silver Maple), ''Hordeum'', (a grass genus that includes barley) and '' Phalaris'' (another grass genus). Effects and toxicity Gramine is a close analogue of the psychedelic drug dimethyltryptamine (DMT), but its side chain has one less carbon atom in comparison. In contrast to DMT, gramine does not have significant psychedelic-like behavioral effects in animals. The same is true of 5-methoxygramine (5-MeO-gramine), which failed to substitute for DOM in rodent drug discrimination tests. Gramine has been found to act as an agonist of the adiponectin receptor 1 (AdipoR1). The LD50 of gramine is 44.6 mg/ kg iv in mice and 62.9 mg/ kg iv in rats. Numerous studies have been done on the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Calcitonin Gene-related Peptide
Calcitonin gene-related peptide (CGRP) is a neuropeptide that belongs to the calcitonin family. Human CGRP consists of two Protein isoform, isoforms, CGRP alpha (α-CGRP, also known as CGRP I) and CGRP beta (β-CGRP, also known as CGRP II). α-CGRP is a 37-amino acid neuropeptide formed by alternative splicing of the calcitonin/CGRP gene located on chromosome 11. β-CGRP is less studied. In humans, β-CGRP differs from α-CGRP by three amino acids and is encoded in a separate, nearby gene. The CGRP family includes calcitonin (CT), adrenomedullin (AM), and amylin (AMY). Function CGRP is produced in both peripheral and central neurons. It is a potent peptide vasodilator and can function in the transmission of nociception. In the spinal cord, the function and expression of CGRP may differ depending on the location of synthesis. CGRP is derived mainly from the cell bodies of motor neurons when synthesized in the Ventral horn of spinal cord, ventral horn of the spinal cord and may c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amylin
Amylin, or islet amyloid polypeptide (IAPP), is a 37-residue peptide hormone. It is co-secreted with insulin from the pancreatic β-cells in the ratio of approximately 100:1 (insulin:amylin). Amylin plays a role in glycemic regulation by slowing gastric emptying and promoting satiety, thereby preventing post-prandial spikes in blood glucose levels. IAPP is processed from an 89-residue coding sequence. Proislet amyloid polypeptide (proIAPP, proamylin, proislet protein) is produced in the pancreatic beta cells (β-cells) as a 67 amino acid, 7404 Dalton pro-peptide and undergoes post-translational modifications including protease cleavage to produce amylin. Synthesis ProIAPP consists of 67 amino acids, which follow a 22 amino acid signal peptide which is rapidly cleaved after translation of the 89 amino acid coding sequence. The human sequence (from N-terminus to C-terminus) is: (MGILKLQVFLIVLSVALNHLKA) TPIESHQVEKR^ KCNTATCATQRLANFLVHSSNNFGAILSSTNVGSNTYG^ KR^ NAVEVLKREP ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LF22-0542
Safotibant (INN) also known by the research code LF22-0542 is a non-peptide bradykinin B1 antagonist. It displayed binding Ki values of 0.35 and 6.5 nM at cloned human and mouse B1 receptors, respectively, while having no affinity for either human, mouse, or rat B2 receptors at concentrations up to 10 μM. This means that LF22-0542 is at least 4000 times selective for the B1 receptor over the B2 receptor. Systemic administration of LF22-0542 inhibited acute pain induced by acetic acid, formalin, and a hot plate. It also reversed acute inflammatory pain induced by carrageenan, and persistent inflammatory pain induced by CFA. In a neuropathic pain model, LF22-0542 reversed the thermal hyperalgesia Hyperalgesia ( or ; ''hyper'' from Greek ὑπέρ (''huper'') 'over' + ''-algesia'' from Greek ἄλγος (algos) 'pain') is an abnormally increased sensitivity to pain, which may be caused by damage to nociceptors or peripheral nerves and ..., but not the mechanical hyperalgesi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Icatibant
Icatibant, sold under the brand name Firazyr, is a medication for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults with C1-esterase-inhibitor deficiency. It is not effective in angioedema caused by medication from the ACE inhibitor class. It is a peptidomimetic consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. Mechanism of action Bradykinin is a peptide-based hormone that is formed locally in tissues, very often in response to a trauma. It increases vessel permeability, dilates blood vessels and causes smooth muscle cells to contract. Bradykinin plays an important role as the mediator of pain. Surplus bradykinin is responsible for the typical symptoms of inflammation, such as swelling, redness, overheating and pain. These symptoms are mediated by activation of bradykinin B2 receptors. Icatibant acts as a bradykinin inhibitor by blocking the binding of native bradykinin to the bradykini ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kallidin
Kallidin belongs to the family kinins, which are the peptide hormones. Kallidin is a decapeptide whose sequence is H-Lys-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH. It can be converted to bradykinin by the aminopeptidase enzyme. Effects of Kinins Kallidin is a bioactive kinin peptide formed in response to injury from kininogen precursors through the action of kallikreins. Like all kinins, kallidin, the deca-peptide, plays an important role in several body pathologies. Kinins can regulate the blood pressure by increasing the level of vasopressor substances. They can also bind to the B1 and B2 cell surface receptors, which are G-protein coupled receptors. The mediation of the B1 receptors by des-Arg kinins as agonists can be expressed in several medical issues, such as cancer and trauma. By binding to the B2 receptors, kinins, endogenous agonists, can regulate the vasodilatation and bronchioconstriction. Chemical Mechanisms Since kinins are peptides, they can be cleaved by the p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bradykinin
Bradykinin (BK) (from Greek ''brady-'' 'slow' + ''-kinin'', ''kīn(eîn)'' 'to move') is a peptide that promotes inflammation. It causes arterioles to dilate (enlarge) via the release of prostacyclin, nitric oxide, and endothelium-derived hyperpolarizing factor and makes veins constrict, via prostaglandin F2, thereby leading to leakage into capillary beds, due to the increased pressure in the capillaries. Bradykinin consists of nine amino acids, and is a physiologically and pharmacologically active peptide of the kinin group of proteins. A class of drugs called angiotensin-converting-enzyme inhibitors (ACE inhibitors) increase bradykinin levels by inhibiting its degradation, thereby increasing its blood pressure lowering effect. ACE inhibitors are FDA approved for the treatment of hypertension and heart failure. Structure Bradykinin, sometimes referred to as BK, is a 9–amino acid Translation (genetics), peptide chain. The amino acid sequence of bradykinin is: arginine, Arg-pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Taxifoliol
Taxifolin (5,7,3',4'-flavan-on-ol), also known as dihydroquercetin, belongs to the subclass flavanonols in the flavonoids, which in turn is a class of polyphenols. It is extracted from plants such as Siberian larch and milk thistle. Stereocenters Taxifolin has two stereocenters on the C-ring, as opposed to quercetin which has none. For example, (+)-taxifolin has (2''R'',3''R'')-configuration, making it one out of four stereoisomers that comprise two pairs of enantiomers. Natural occurrences Taxifolin is found in non-glutinous rice boiled with adzuki bean (adzuki-meshi). It can be found in conifers like the Siberian larch, ''Larix sibirica'', in Russia, in ''Pinus roxburghii'', in ''Cedrus deodara'' and in the Chinese yew, '' Taxus chinensis var. mairei''. It is also found in the silymarin extract from the milk thistle seeds. Taxifolin is present in vinegars aged in cherry wood. Taxifolin, and flavonoids in general, can be found in many beverages and products. Specifical ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Syringing (drug)
A syringe is a simple reciprocating pump consisting of a plunger (though in modern syringes, it is actually a piston) that fits tightly within a cylindrical tube called a barrel. The plunger can be linearly pulled and pushed along the inside of the tube, allowing the syringe to take in and expel liquid or gas through a discharge orifice at the front (open) end of the tube. The open end of the syringe may be fitted with a hypodermic needle, a nozzle or tubing to direct the flow into and out of the barrel. Syringes are frequently used in clinical medicine to administer injections, infuse intravenous therapy into the bloodstream, apply compounds such as glue or lubricant, and draw/measure liquids. There are also prefilled syringes (disposable syringes marketed with liquid inside). The word "syringe" is derived from the Greek σῦριγξ (''syrinx'', meaning "Pan flute", "tube"). Medical syringes Medical syringes include disposable and safety syringes, injection pens, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Parthenolide
Parthenolide is a sesquiterpene lactone of the germacranolide class which occurs naturally in the plant feverfew ('' Tanacetum parthenium''), after which it is named, and in the closely related tansy (''Tanacetum vulgare''). It is found in highest concentration in the flowers and fruit. Parthenolide's molecular structure depiction is often incorrect regarding the stereochemistry of the epoxide, although X-ray single crystal structures are available. Lack of solubility in water and bioavailability In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. H ... limits the potential of parthenolide as a drug. References {{HDAC inhibitors Adiponectin receptor agonists Epoxides Histone deacetylase inhibitors Sesquiterpene lactones ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
