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TAS2R14 Agonist 28.1
TAS2R14 agonist 28.1 (sometimes referred to simply as 28.1) is an experimental drug that acts as a potent and selective agonist of the bitter taste receptor TAS2R14. It was developed by modification of flufenamic acid, a pharmaceutical known for its bitter taste which produces bitterness via activation of TAS2R14, but is around six times more potent. TAS2R14 is also expressed in the lungs and causes bronchodilatation, so TAS2R14 agonists such as 28.1 may be useful in the treatment of asthma and other lung diseases. See also * Amarogentin * Oligoporin D Oligoporin D is a natural product isolated from the "bitter bracket" mushroom '' Amaropostia stiptica''. It was found to be one of the most potent agonists yet discovered for the bitter taste The gustatory system or sense of taste is the sen ... References Experimental drugs Pyrimidines Tetrazoles Anilines Trifluoromethyl compounds {{respiratory-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bitter Taste
The gustatory system or sense of taste is the sensory system that is partially responsible for the perception of taste. Taste is the perception stimulated when a substance in the mouth reacts chemically with taste receptor cells located on taste buds in the oral cavity, mostly on the tongue. Taste, along with the sense of smell and trigeminal nerve stimulation (registering texture, pain, and temperature), determines flavors of food and other substances. Humans have taste receptors on taste buds and other areas, including the upper surface of the tongue and the epiglottis. The gustatory cortex is responsible for the perception of taste. The tongue is covered with thousands of small bumps called papillae, which are visible to the naked eye. Within each papilla are hundreds of taste buds. The exceptions to this is the filiform papillae that do not contain taste buds. There are between 2000 and 5000Boron, W.F., E.L. Boulpaep. 2003. Medical Physiology. 1st ed. Elsevier Science U ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TAS2R14
Taste receptor type 2 member 14 is a protein that in humans is encoded by the ''TAS2R14'' gene. Taste receptors for bitter substances (T2Rs/TAS2Rs) belong to the family of G-protein coupled receptors and are related to class A-like GPCRs. There are 25 known T2Rs in humans responsible for bitter taste perception. Bitter taste receptor hTAS2R14 is one of the human bitter taste receptors, recognizing an enormous variety of structurally different molecules, including natural and synthetic bitter compounds. Gene TAS2R14 gene (Taste receptor type 2 member 14) is a Protein Coding gene. This gene maps to the taste receptor gene cluster on chromosome 12p13. An important paralog of this gene is TAS2R13. SNPs Taste receptors harbor many polymorphisms, and several SNPs have a profound impact on the gene function and expression. Data obtained fro1000 genomes project Site-directed mutagenesis The following residues have been subjected to site-directed mutagenesis. Signal transd ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bronchodilatation
Bronchodilatation, or bronchodilation, is a reduction in airway resistance caused by the relaxation of airway smooth muscle. It is the opposite of bronchoconstriction. Medically, bronchodilatation is used in the treatment of certain respiratory disorders, where it can reduce respiratory symptoms and/or improve lung function. Pharmacologically, bronchodilatation is achieved via bronchodilator A bronchodilator or broncholytic (although the latter occasionally includes secretory inhibition as well) is a substance that dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lun ...s. References Respiration {{respiratory-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Asthma
Asthma is a common long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wheezing, coughing, chest tightness, and shortness of breath. A sudden worsening of asthma symptoms sometimes called an 'asthma attack' or an 'asthma exacerbation' can occur when allergens, pollen, dust, or other particles, are inhaled into the lungs, causing the bronchioles to constrict and produce mucus, which then restricts oxygen flow to the alveoli. These may occur a few times a day or a few times per week. Depending on the person, asthma symptoms may become worse at night or with exercise. Asthma is thought to be caused by a combination of genetic and environmental factors. Environmental factors include exposure to air pollution and allergens. Other potential triggers include medications such as aspirin and beta blockers. Diag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amarogentin
Amarogentin is a chemical compound found in gentian (''Gentiana lutea'') or in ''Swertia chirata''. Gentian root has a long history of use as a herbal bitter in the treatment of digestive disorders and is an ingredient of many proprietary medicines. The bitter principles of gentian root are secoiridoid glycosides amarogentin and gentiopicrin. The former is one of the most bitter (taste), bitter natural compounds known and is used as a scientific basis for measuring bitterness. In humans, it activates the bitter taste receptor TAS2R50. The biphenylcarboxylic acid moiety is biosynthesized by a polyketide-type pathway, with three units of acetyl-CoA and one unit of 3-Hydroxybenzoyl-CoA, 3-hydroxybenzoyl-CoA, this being formed from an early shikimate pathway intermediate and not via cinnamic or benzoic acid. It also shows an antileishmanial activity in animal models being an inhibitor of topoisomerase I. See also * Denatonium * TAS2R14 agonist 28.1 * Oligoporin D References {{ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oligoporin D
Oligoporin D is a natural product isolated from the "bitter bracket" mushroom '' Amaropostia stiptica''. It was found to be one of the most potent agonists yet discovered for the bitter taste The gustatory system or sense of taste is the sensory system that is partially responsible for the perception of taste. Taste is the perception stimulated when a substance in the mouth reacts chemically with taste receptor cells located on tas ... receptor TAS2R46, and consequently one of the most bitter substances known. References Natural products Steroids {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrimidines
Pyrimidine (; ) is an aromatic, heterocyclic, organic compound similar to pyridine (). One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has nitrogen atoms at positions 1 and 3 in the ring. The other diazines are pyrazine (nitrogen atoms at the 1 and 4 positions) and pyridazine (nitrogen atoms at the 1 and 2 positions). In nucleic acids, three types of nucleobases are pyrimidine derivatives: cytosine (C), thymine (T), and uracil (U). Occurrence and history The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. It is also found in many synthetic compounds such as barbiturates and the HIV drug zidovudine. Although pyrimidine derivatives such as alloxan were known in the early 19th century, a laboratory synthesis of a pyrimidine was not carried out until 1879, when Grimaux reported the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetrazoles
A tetrazole is a synthetic organic heterocyclic compound, consisting of a 5-member ring of four nitrogen atoms and one carbon atom. The name tetrazole also refers to the parent compound - a whitish crystalline powder with the formula CH2N4, of which three isomers exist. Structure and bonding Three isomers of the parent tetrazole exist, differing in the position of the double bonds: 1''H''-, 2''H''-, and 5''H''-tetrazole. The 1''H''- and 2''H''- isomers are tautomers, with the equilibrium lying on the side of 1''H''-tetrazole in the solid phase. In the gas phase, 2''H''-tetrazole dominates. These isomers can be regarded as aromatic, with 6 π-electrons, while the 5''H''-isomer is nonaromatic. Phosphorus analogs do not have the same electronic nature, with 1''H''-tetraphosphole having a more pyramidal geometry of the phosphorus at position 1. Instead, it is the anionic tetraphospholides that are aromatic. Strongly inductively electron-withdrawing functional groups attached ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
