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PF-05105679
PF-05105679 is a drug which acts as a potent and selective blocker of the TRPM8 ion channel, which is the main receptor responsible for the sensation of cold. It was developed as a potential analgesic, and blocks the sensation of cold in both animals and human trials. It also lowers core body temperature in small mammals, but does not produce this effect in humans in the normal dosage range. See also * AMG-333 AMG-333 is a drug which acts as a potent and selective blocker of the TRPM8 ion channel, which is the main receptor responsible for the sensation of cold Cold is the presence of low temperature, especially in the atmosphere. In common ... * RQ-00203078 References Quinolines Tertiary amines Benzoic acids Fluoroarenes Amides {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TRPM8
Transient receptor potential cation channel subfamily M (melastatin) member 8 (TRPM8), also known as the cold and menthol receptor 1 (CMR1), is a protein that in humans is encoded by the ''TRPM8'' gene. The TRPM8 channel is the primary molecular transducer of cold somatosensation in humans. In addition, mints can desensitize a region through the activation of TRPM8 receptors (the 'cold'/menthol receptor). Structure The TRPM8 channel is a homotetramer, composed of four identical subunits with a transmembrane domain with six helices (S1–6). The first four, S1–4, act as the voltage sensor and allow binding of menthol, icilin and similar channel agonists. S5 and S6 and a connecting loop, also part of the structure, make up the pore, a non-selective cation channel which consists of a highly conserved hydrophobic region. A range of diverse components are required for the high level of specificity in response to cold and menthol stimuli which eventually lead to ion flow through the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMG-333
AMG-333 is a drug which acts as a potent and selective blocker of the TRPM8 ion channel, which is the main receptor responsible for the sensation of cold Cold is the presence of low temperature, especially in the atmosphere. In common usage, cold is often a subjective perception. A lower bound to temperature is absolute zero, defined as 0.00K on the Kelvin scale, an absolute thermodynamic .... It was developed as a potential treatment for migraine. See also * PF-05105679 * RQ-00203078 References Pyridines Trifluoromethyl ethers Amides Fluoroarenes Carboxylic acids {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RQ-00203078
RQ-00203078 is a drug which acts as a potent and selective blocker of the TRPM8 ion channel, which is the main receptor responsible for the sensation of cold. It was developed as a potential analgesic, and blocks the development of hyperalgesia following exposure to cold temperatures or chronic morphine administration. See also * AMG-333 * PF-05105679 PF-05105679 is a drug which acts as a potent and selective blocker of the TRPM8 ion channel, which is the main receptor responsible for the sensation of cold. It was developed as a potential analgesic, and blocks the sensation of cold in both a ... References Pyridines Trifluoromethyl ethers Trifluoromethyl compounds Carboxylic acids Chloroarenes Sulfamates {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ion Channel
Ion channels are pore-forming membrane proteins that allow ions to pass through the channel pore. Their functions include establishing a resting membrane potential, shaping action potentials and other electrical signals by gating the flow of ions across the cell membrane, controlling the flow of ions across secretory and epithelial cells, and regulating cell volume. Ion channels are present in the membranes of all cells. Ion channels are one of the two classes of ionophoric proteins, the other being ion transporters. The study of ion channels often involves biophysics, electrophysiology, and pharmacology, while using techniques including voltage clamp, patch clamp, immunohistochemistry, X-ray crystallography, fluoroscopy, and RT-PCR. Their classification as molecules is referred to as channelomics. Basic features There are two distinctive features of ion channels that differentiate them from other types of ion transporter proteins: #The rate of ion transport through the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cold
Cold is the presence of low temperature, especially in the atmosphere. In common usage, cold is often a subjective perception. A lower bound to temperature is absolute zero, defined as 0.00K on the Kelvin scale, an absolute thermodynamic temperature scale. This corresponds to on the Celsius scale, on the Fahrenheit scale, and on the Rankine scale. Since temperature relates to the thermal energy held by an object or a sample of matter, which is the kinetic energy of the random motion of the particle constituents of matter, an object will have less thermal energy when it is colder and more when it is hotter. If it were possible to cool a system to absolute zero, all motion of the particles in a sample of matter would cease and they would be at complete rest in the classical sense. The object could be described as having zero thermal energy. Microscopically in the description of quantum mechanics, however, matter still has zero-point energy even at absolute zero, because ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
Core Body Temperature
Normal human body-temperature (normothermia, euthermia) is the typical temperature range found in humans. The normal human body temperature range is typically stated as . Human body temperature varies. It depends on sex, age, time of day, exertion level, health status (such as illness and menstruation), what part of the human body, body the measurement is taken at, state of consciousness (waking, sleeping, sedated), and emotions. Body temperature is kept in the normal range by Thermoregulation in humans, thermoregulation, in which adjustment of temperature is triggered by the central nervous system. Methods of measurement Taking a person's temperature is an initial part of a full clinical examination. There are various types of medical thermometers, as well as sites used for measurement, including: * In the rectum (rectal temperature) * In the mouth (oral temperature) * Under the arm (axillary temperature) * In the ear (tympanic temperature) * On the skin of the forehead ove ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Quinolines
Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N. It is a colorless hygroscopic liquid with a strong odor. Aged samples, especially if exposed to light, become yellow and later brown. Quinoline is only slightly soluble in cold water but dissolves readily in hot water and most organic solvents. Quinoline itself has few applications, but many of its derivatives are useful in diverse applications. A prominent example is quinine, an alkaloid found in plants. Over 200 biologically active quinoline and quinazoline alkaloids are identified. 4-Hydroxy-2-alkylquinolines (HAQs) are involved in antibiotic resistance. Occurrence and isolation Quinoline was first extracted from coal tar in 1834 by German chemist Friedlieb Ferdinand Runge; he called quinoline ''leukol'' ("white oil" in Greek). Coal tar remains the principal source of commercial quinoline. In 1842, French chemist Charles Gerhardt obtained a compound by dry distilling quinine, str ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tertiary Amines
In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines). Important amines include amino acids, biogenic amines, trimethylamine, and aniline; Inorganic derivatives of ammonia are also called amines, such as monochloramine (). The substituent is called an amino group. Compounds with a nitrogen atom attached to a carbonyl group, thus having the structure , are called amides and have different chemical properties from amines. Classification of amines Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzoic Acids
Benzoic acid is a white (or colorless) solid organic compound with the formula , whose structure consists of a benzene ring () with a carboxyl () substituent. It is the simplest aromatic carboxylic acid. The name is derived from gum benzoin, which was for a long time its only source. Benzoic acid occurs naturally in many plants and serves as an intermediate in the biosynthesis of many secondary metabolites. Salts of benzoic acid are used as food preservatives. Benzoic acid is an important precursor for the industrial synthesis of many other organic substances. The salts and esters of benzoic acid are known as benzoates . History Benzoic acid was discovered in the sixteenth century. The dry distillation of gum benzoin was first described by Nostradamus (1556), and then by Alexius Pedemontanus (1560) and Blaise de Vigenère (1596). Justus von Liebig and Friedrich Wöhler determined the composition of benzoic acid. These latter also investigated how hippuric acid is related ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
