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Inverse Agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; they are in fact sometimes called ''blockers'' (examples include alpha blockers, beta blockers, and calcium channel blockers). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists. A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand. An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level. The efficacy of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Inverse Agonist 3
Inverse or invert may refer to: Science and mathematics * Inverse (logic), a type of conditional sentence which is an immediate inference made from another conditional sentence * Additive inverse, the inverse of a number that, when added to the original number, yields zero * Compositional inverse, a function that "reverses" another function * Inverse element * Inverse function, a function that "reverses" another function **Generalized inverse, a matrix that has some properties of the inverse matrix but not necessarily all of them * Multiplicative inverse (reciprocal), a number which when multiplied by a given number yields the multiplicative identity, 1 ** Inverse matrix of an Invertible matrix Other uses * Invert level, the base interior level of a pipe, trench or tunnel * ''Inverse'' (website), an online magazine * An outdated term for an LGBT person; see Sexual inversion (sexology) See also * Inversion (other) * Inverter (other) * Opposite (disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Endogeny (biology)
Endogeny, in biology, refers to the property of originating or developing from within an organism, Tissue (biology), tissue, or Cell (biology), cell. For example, ''endogenous substances'', and ''endogenous processes'' are those that originate within a living system (e.g. an organism or a Cell (biology), cell). For instance, estradiol is an endogenous estrogen hormone produced within the body, whereas ethinylestradiol is an exogenous synthetic estrogen, commonly used in birth control pills. In contrast, ''Exogeny#Biology, exogenous substances'' and ''exogenous'' ''processes'' are those that originate from outside of an organism. References External links *{{Wiktionary-inline, endogeny Biology ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocortin 4 Receptor
The melanocortin 4 receptor (MC4R) is a G protein-coupled receptor involved in regulating energy homeostasis, appetite, and sexual function. It plays a key role in metabolic processes and is predisposes to certain forms of obesity in humans. MC4R is a receptor that is activated by α-melanocyte-stimulating hormone (α-MSH), influencing energy homeostasis and feeding behavior in the central nervous system. In mouse models, MC4R has been shown to regulate feeding behavior, metabolism, reproductive function, and erectile response. Clinical significance The importance of the MC4R in the regulation of human body weight first became apparent in 1998 with the reports from two groups of single families in whom heterozygous frameshift mutations in ''MC4R'' cosegregated with dominantly inherited severe early-onset obesity. In 2009, two very large genome-wide association studies of body mass index (BMI) confirmed the association of common variants about 150 kilobases downstream of the ''M ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melanocortin Receptors
Melanocortin receptors are members of the rhodopsin family of 7-transmembrane G protein-coupled receptors. There are five known members of the melanocortin receptor system each with differing specificities for melanocortins: * . MC1R is associated with pigmentation genetics. * . MC2R is also known as the ACTH receptor or corticotropin receptor because it is specific for ACTH alone. * . MC3R is associated with childhood growth, accrual of lean mass and onset of puberty. * . Defects in MC4R are a cause of autosomal dominant obesity, accounting for 6% of all cases of early-onset obesity. * . MC5R These receptors are inhibited by endogenous inverse agonists agouti signalling peptide and agouti-related peptide, and activated by synthetic (i.e. afamelanotide) and endogenous agonist melanocyte-stimulating hormones. Selective ligands Several selective ligands for the melanocortin receptors are known, and some synthetic compounds have been investigated as potential tanning, anti-obes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agouti Signalling Peptide
Agouti-signaling protein is a protein that in humans is encoded by the ASIP gene. It is responsible for the distribution of melanin pigment in mammals. Agouti interacts with the melanocortin 1 receptor to determine whether the melanocyte (pigment cell) produces phaeomelanin (a red to yellow pigment), or eumelanin (a brown to black pigment). This interaction is responsible for making distinct light and dark bands in the hairs of animals such as the agouti, which the gene is named after. In other species such as horses, agouti signalling is responsible for determining which parts of the body will be red or black. Mice with wildtype agouti will be grey-brown, with each hair being partly yellow and partly black. Loss of function mutations in mice and other species cause black fur coloration, while mutations causing expression throughout the whole body in mice cause yellow fur and obesity. The agouti-signaling protein (ASIP) is a competitive antagonist with alpha-Melanocyte-stimulati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agouti-related Peptide
Agouti-related protein (AgRP), also called agouti-related peptide, is a neuropeptide produced in the brain by the AgRP/NPY neuron. It is synthesized in neuropeptide Y (NPY)-containing cell bodies located in the ventromedial part of the arcuate nucleus in the hypothalamus. AgRP is co-expressed with NPY and acts to increase appetite and decrease metabolism and energy expenditure. It is one of the most potent and long-lasting of appetite stimulators. In humans, the agouti-related peptide is encoded by the ''AGRP'' gene. Structure AgRP is a paracrine signaling molecule made of 112 amino acids (the gene product of 132 amino acids is processed by removal of the N-terminal 20-residue signal peptide domain). It was independently identified by two teams in 1997 based on its sequence similarity with agouti signalling peptide (ASIP), a protein synthesized in the skin controlling coat colour. AgRP is approximately 25% identical to ASIP. The murine homologue of AgRP consists of 111 amin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiogenic
An anxiogenic or panicogenic substance is one that causes anxiety. This effect is in contrast to anxiolytic agents, which inhibits anxiety. Together these categories of psychoactive compounds may be referred to as anxiotropic compounds. Experimental Studies Anxiogenic effects can be measured by, for example, the hole-board test in rats and mice. A number of agents are used to provoke anxiety (anxiogens) or panic (panicogens) in experimental models. Mechanisms of Action Anxiogenic substances typically work through affecting levels of neurotransmitters such as dopamine, epinephrine, gamma-aminobutyric acid (GABA), norepinephrine (NE), and serotonin in the central nervous system (CNS). Some substances may alter functioning in the HPA axis, the neuroendocrine system that mediates responses to stress, where dysfunction has been linked to anxiety and panic disorders. Some substances, such as caffeine and sodium lactate, are largely reported to have anxiogenic effects only if they ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convulsive
A convulsion is a medical condition where the body muscles contract and relax rapidly and repeatedly, resulting in uncontrolled shaking. Because epileptic seizures typically include convulsions, the term ''convulsion'' is often used as a synonym for ''seizure''. However, not all epileptic seizures result in convulsions, and not all convulsions are caused by epileptic seizures. Non-epileptic convulsions have no relation with epilepsy, and are caused by non-epileptic seizures. Convulsions can be caused by epilepsy, infections (including a severe form of listeriosis which is caused by eating food contaminated by Listeria monocytogenes), brain trauma, or other medical conditions. They can also occur from an electric shock or improperly enriched air for scuba diving. The word ''fit'' is sometimes used to mean a convulsion or epileptic seizure. Signs and symptoms A person having a convulsion may experience several different symptoms, such as a brief blackout, confusion, drooling, los ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ro15-4513
Ro15-4513 is a weak partial inverse agonist of the benzodiazepine class of drugs, developed by Hoffmann–La Roche in the 1980s. It acts as an inverse agonist (which acts in a similar way as a competitive antagonist). The drug has been explored as possible antidote to the sedative and cognitively impairing effects of ethanol. Ro15-4513 is structurally related to the benzodiazepine antidote flumazenil. Uses Original development as alcohol antidote The main interest in Ro15-4513 was as an antidote to alcohol (ethanol). Flumazenil effectively blocks the effects of benzodiazepine agonists such as alprazolam and diazepam, and so is used for treating overdoses of these drugs, but is ineffective in blocking alcohol actions. Ro15-4513 was somewhat less effective than flumazenil at blocking the effects of benzodiazepines, but was able to effectively block the effects of ethanol. This meant that in contrast to flumazenil, which is ineffective at treating alcohol overdoses, Ro15-4513 showe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agitation (action)
An agitator is a device or mechanism to put something into motion by shaking or stirring. There are several types of agitation machines, including washing machine agitators (which rotate back and forth) and magnetic agitators (which contain a magnetic bar rotating in a magnetic field). Agitators can come in many sizes and varieties, depending on the application. In general, agitators usually consist of an impeller and a shaft. An impeller is a rotor located within a tube or conduit attached to the shaft. It helps enhance the pressure in order for the flow of a fluid be done. Modern industrial agitators incorporate process control to maintain better control over the mixing process. Washing machine agitator In a top load washing machine the agitator projects from the bottom of the wash basket and creates the wash action by rotating back and forth, rolling garments from the top of the load, down to the bottom, then back up again. There are several types of agitators with the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Relaxant
A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: neuromuscular blockers and spasmolytics. Neuromuscular blockers act by interfering with transmission at the neuromuscular end plate and have no central nervous system (CNS) activity. They are often used during surgical procedures and in intensive care and emergency medicine to cause temporary paralysis. Spasmolytics, also known as "centrally acting" muscle relaxant, are used to alleviate musculoskeletal pain and spasms and to reduce spasticity in a variety of neurological conditions. While both neuromuscular blockers and spasmolytics are often grouped together as muscle relaxant, [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
