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Capsazepine
Capsazepine is a synthetic antagonist of capsaicin. It is used as a biochemical tool in the study of TRPV ion channels. Pharmacology Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel. Capsazepine is therefore considered to be a TRPV1 antagonist. The TRPV1 channel functions as a pain and temperature sensor in mammalians. Capsazepine blocks the activation of TRPV1 channels by other chemicals, but not by other painful stimuli such as heat. Depending on the pharmacological assay, the IC50 is in the nanomolar to low micromolar range. In addition to its effects on TRPV1 channels, it was also shown to activate the noxious chemical sensor TRPA1 channel, inhibit the cold activated TRPM8 channel, voltage-activated calcium channels and nicotinic acetylcholine receptors. It mainly serves as a tool to study the TRPV1 ion channel. Development Capsazepine was discovered by a research group wo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Discovery And Development Of TRPV1 Antagonists
Relief from chronic pain remains a recognized unmet medical need. Consequently, the search for new analgesic agents is being intensively studied by the pharmaceutical industry. The TRPV1 receptor is an ion channel that has been implicated in mediation of many types of pain and therefore studied most extensively. The first competitive antagonist, capsazepine, was first described in 1990; since then, development of novel TRPV1 antagonists has come a long way. This effort has led to the identification of several TRPV1 antagonists that have entered clinical trials as analgesic agents. Should these new chemical entities relieve symptoms of chronic pain, then this class of compounds may offer one of the first novel mechanisms for the treatment of pain in many years. History Capsaicin, the active ingredient in chili pepper was first isolated over a century ago. In 1919 the exact chemical structure of capsaicin was determined and the complete synthesis of the compound was achieved a decade ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Capsaicin
Capsaicin (8-methyl-''N''-vanillyl-6-nonenamide) ( or ) is an active component of chili peppers, which are plants belonging to the genus ''Capsicum''. It is a chemical irritant for mammals, including humans, and produces a sensation of burning in any tissue with which it comes into contact. Capsaicin and several related alkaloids are called capsaicinoids and are produced as secondary metabolites by chili peppers, probably as deterrents against certain mammals and fungi.What Made Chili Peppers So Spicy? Talk of the Nation, 15 August 2008. Pure capsaicin is a , colorless, highly |
Capsaicinoids
Capsaicin (8-methyl-''N''-vanillyl-6-nonenamide) ( or ) is an active component of chili peppers, which are plants belonging to the genus ''Capsicum''. It is a chemical irritant for mammals, including humans, and produces a sensation of burning in any tissue with which it comes into contact. Capsaicin and several related alkaloids are called capsaicinoids and are produced as secondary metabolites by chili peppers, probably as deterrents against certain mammals and fungi.What Made Chili Peppers So Spicy? Talk of the Nation, 15 August 2008. Pure capsaicin is a , colorless, highly |
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, |
Benzazepines
Benzazepines are heterocyclic chemical compounds consisting of a benzene ring fused to an azepine ring. Examples include: File:Benazepril structure.svg, Benazepril File:Fenoldopam.svg, Fenoldopam File:GSK-189,254.svg, GSK-189,254 File:Ivabradine 2.svg, Ivabradine File:Semagacestat structure.svg, Semagacestat File:Varenicline.svg, Varenicline See also * Benzodiazepine Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ... * Dibenzazepine References {{Heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Catechols
Catechol ( or ), also known as pyrocatechol or 1,2-dihydroxybenzene, is a toxic organic compound with the molecular formula . It is the ''ortho'' isomer of the three isomeric benzenediols. This colorless compound occurs naturally in trace amounts. It was first discovered by destructive distillation of the plant extract catechin. About 20,000 tonnes of catechol are now synthetically produced annually as a commodity organic chemical, mainly as a precursor to pesticides, flavors, and fragrances. Catechol occurs as feathery white crystals that are very rapidly soluble in water. Isolation and synthesis Catechol was first isolated in 1839 by Edgar Hugo Emil Reinsch (1809–1884) by distilling it from the solid tannic preparation catechin, which is the residuum of catechu, the boiled or concentrated juice of ''Mimosa catechu'' (''Acacia catechu''). Upon heating catechin above its decomposition point, a substance that Reinsch first named ''Brenz-Katechusäure'' (burned catechu acid) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JWH-133
JWH-133 (Dimethylbutyl-deoxy-Delta-8-THC) is a potent selective CB2 receptor agonist with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors. It was discovered by and named after, John W. Huffman. It's important to note that JWH-133 has been confused with other analogs of Delta-8-THC in professionally published peer-reviewed literature. Including being confused with Dimethylpentyl-Delta-8-THC as well as Dimethylbutyl-Delta-8-THC. Including confusing the chemical name with Dimethylbutyl-Delta-8-THC itself. Including confusing it with the Delta-9 isomer Including using the structural image of Dimethylbutyl-Delta-8-THC instead of Dimethylbutyl-deoxy-Delta-8-THC. It's important to note that 3-(1',1'-Dimethylbutyl)-1-deoxy-delta-8-THC is a selective CB2 agonist, binding 677nM at Cb1 and 3.4nM at CB2 while 3-(1',1'-Dimethylbutyl)-delta-8-THC itself binds 65nM at CB1. Structurally the only difference between JWH-133 and dimethylbutyl-D8-THC is that JWH-133 lacks ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Herkinorin
Herkinorin is an opioid analgesic that is an analog (chemistry), analogue of the natural product salvinorin A. It was discovered in 2005 during structure-activity relationship studies into neoclerodane diterpenes, the family of chemical compounds of which salvinorin A is a member. Unlike salvinorin A, which is a selective κ-opioid receptor agonist with no significant μ-opioid receptor affinity, herkinorin is predominantly a μ-opioid receptor agonist. Compared to salvinorin A, herkinorin has 47× lower Ligand_(biochemistry)#Receptor/ligand_binding_affinity, affinity for κ-opioid receptors (''K''i ＝ 90 nM vs ''K''i ＝ 1.9 nM), and at least 25× higher affinity for μ-opioid receptors (''K''i ＝ 12 nM vs ''K''i > 1000 nM), where it acts as a full agonist (IC50 ＝ 0.5 μM, Emax ＝ 130% vs DAMGO). Herkinorin is a semi-synthetic compound, made from salvinorin B, which is most conveniently made from salvinorin A by deacetylation, since, while both salvinorin A and salvinorin B ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Menthol
Menthol is an organic compound, more specifically a monoterpenoid, made synthetically or obtained from the oils of corn mint, peppermint, or other mints. It is a waxy, clear or white crystalline substance, which is solid at room temperature and melts slightly above. The main form of menthol occurring in nature is (−)-menthol, which is assigned the (1''R'',2''S'',5''R'') configuration. Menthol has local anesthetic and counterirritant qualities, and it is widely used to relieve minor throat irritation. Menthol also acts as a weak κ-opioid receptor agonist. Structure Natural menthol exists as one pure stereoisomer, nearly always the (1''R'',2''S'',5''R'') form (bottom left corner of the diagram below). The eight possible stereoisomers are: : In the natural compound, the isopropyl group is in the ''trans'' orientation to both the methyl and hydroxyl groups. Thus, it can be drawn in any of the ways shown: : The (+)- and (−)-enantiomers of menthol are the most stable among ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Photoswitch
A photoswitch is a type of molecule that can change its structural geometry and chemical properties upon irradiation with electromagnetic radiation. Although often used interchangeably with the term molecular machine, a switch does not perform work upon a change in its shape whereas a machine does. However, photochromic compounds are the necessary building blocks for light driven molecular motors and machines. Upon irradiation with light, photoisomerization about double bonds in the molecule can lead to changes in the cis- or trans- configuration. These photochromic molecules are being considered for a range of applications. Chemical structures and properties A photochromic compound can change its configuration or structure upon irradiation with light. Several examples of photochromic compounds include: azobenzene, spiropyran, merocyanine, diarylethene, spirooxazine, fulgide, hydrazone, nobormadiene, thioindigo, acrylamide-azobenzene-quaternary ammonia, donor-acceptor Stenhouse ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azobenzene
Azobenzene is a photoswitchable chemical compound composed of two phenyl rings linked by a N=N double bond. It is the simplest example of an aryl azo compound. The term 'azobenzene' or simply 'azo' is often used to refer to a wide class of similar compounds. These azo compounds are considered as derivatives of diazene (diimide), and are sometimes referred to as 'diazenes'. The diazenes absorb light strongly and are common dyes. Structure and synthesis ''trans''-Azobenzene is planar. The N-N distance is 1.189 Å. ''cis''-Azobenzene is nonplanar with a C-N=N-C dihedral angle of 173.5°. The N-N distance is 1.251 Å. Azobenzene was first described by Eilhard Mitscherlich in 1834. Yellowish-red crystalline flakes of azobenzene were obtained in 1856. Its original preparation is similar to the modern one. According to the 1856 method, nitrobenzene is reduced by iron filings in the presence of acetic acid. In the modern synthesis, zinc is the reductant in the presence of a base. I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Novartis
Novartis AG is a Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and Cambridge, Massachusetts, United States (global research).name="novartis.com">https://www.novartis.com/research-development/research-locations It is one of the largest pharmaceutical companies in the world. Novartis manufactures the drugs clozapine (Clozaril), diclofenac (Voltaren; sold to GlaxoSmithKline in 2015 deal), carbamazepine (Tegretol), valsartan (Diovan), imatinib mesylate (Gleevec/Glivec), cyclosporine (Neoral/Sandimmune), letrozole (Femara), methylphenidate (Ritalin; production ceased 2020), terbinafine (Lamisil), deferasirox (Exjade), and others. In March 1996, the companies Ciba-Geigy and Sandoz merged to form Novartis; the pharmaceutical and agrochemical divisions of both companies formed Novartis as an independent entity. Other Ciba-Geigy and Sandoz businesses were sold, or, like Ciba Specialty Chemicals, spun off as independent companies. The Sandoz brand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
