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SDZ SER-082
SER-082, or SDZ SER-082, is a binding selectivity, selective serotonin 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C receptor receptor antagonist, antagonist or weak partial agonist with an ergoline-like chemical structure, structure which is used in scientific research. It shows similar affinity (pharmacology), affinity for the serotonin 5-HT2B and 5-HT2C receptors and has ~40-fold higher affinity for the serotonin 5-HT2C receptor over the closely related serotonin 5-HT2A receptor, 5-HT2A receptor. Usages It has been used in animal studies into the behavioural effects of the different 5-HT2 subtypes, and how they influence the effects of other drugs such as cocaine. The drug has been found to have no effect on anxiety in multiple paradigms in rodents. In contrast to other serotonin 5-HT2C receptor antagonists, SER-082 does not produce hyperlocomotion in rodents, and instead can produce hypolocomotion at high doses that is independent of the serotonin 5-HT2C receptor. It ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
In chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants and .The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. \begin \ce;& \quad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyperlocomotion
Locomotor activity is a measure of animal behavior which is employed in scientific research. Hyperlocomotion, also known as locomotor hyperactivity, hyperactivity, or increased locomotor activity, is an effect of certain drugs in animals in which locomotor activity (locomotion) is increased. It is induced by certain drugs like psychostimulants and NMDA receptor antagonists and is reversed by certain other drugs like antipsychotics and certain antidepressants. Stimulation of locomotor activity is thought to be mediated by increased signaling in the nucleus accumbens, a major brain area involved in behavioral activation and motivated behavior. Hypolocomotion, also known as locomotor hypoactivity, hypoactivity, and decreased locomotor activity, is an effect of certain drugs in animals in which locomotor activity is decreased. It is a characteristic effect of many sedative agents and general anesthetics. Antipsychotics, which are dopamine receptor antagonists, and many serotonerg ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2B Antagonists
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and vas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lysergine
Lysergine, also known as 9,10-didehydro-6,8β-dimethylergoline, is an ergot alkaloid and serotonin receptor agonist of the ergoline family. It is a minor constituent of ergot. Pharmacology Lysergine shows selectivity for activation of the serotonin 5-HT2A receptor over several other closely related serotonin receptors (54-fold over the 5-HT2B receptor, 38-fold over the 5-HT2C receptor, and 127-fold over the 5-HT1A receptor). The drug is a partial agonist of the 5-HT2A receptor with moderate intrinsic activity (Emax = 57%). An analogue of lysergine, (+)-13-fluorolysergol, is an even more selective agonist of the 5-HT2A receptor than lysergine (EC50 for 5-HT2B and 5-HT2C of >10,000nM). However, this compound has relatively weak maximal efficacy in activating the receptor (Emax = 17%). See also * Descarboxylysergic acid * Lysergic acid * Ergine * Lysergol * SDZ SER-082 SER-082, or SDZ SER-082, is a binding selectivity, selective serotonin 5-HT2B receptor, 5-HT2B and 5 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WAY-100635
WAY-100635 is a piperazine drug and research chemical widely used in scientific studies. It was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor. It is sometimes referred to as a silent antagonist at the former receptor. It is closely related to WAY-100135. In light of its dopaminergic activity, conclusions drawn from studies that employ WAY-100635 as a selective 5-HT1A antagonist may need to be re-evaluated. Human PET studies In human PET studies WAY-100635 shows high binding in the cerebral cortex, hippocampus, raphe nucleus and amygdaloid nucleus, while lower in thalamus and basal ganglia. One study described a single case with relatively high binding in the cerebellum. In relating its binding to subject variables one Swedish study found WAY-100635 binding in raphe brain region correlating with self-transcendence and spiritual acceptance personality traits. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1A Receptor
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarization and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, Septum pellucidum, septum, amygdala, and Raphe nuclei, raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-MeO-DMT
5-MeO-DMT (5-methoxy-''N'',''N''-dimethyltryptamine), also known as ''O''-methylbufotenin or mebufotenin (), is a naturally occurring psychedelic of the tryptamine family. It is found in a wide variety of plant species, and is also secreted by the glands of at least one toad species, the Colorado River toad. It may occur naturally in humans as well. Like its close relatives dimethyltryptamine (DMT) and bufotenin (5-HO-DMT), it has been used as an entheogen in South America. Slang terms include ''five-methoxy'', ''the power'', ''bufo'', and ''toad venom''. The drug has been described as the most powerful psychedelic and, by journalist Michael Pollan, as the "Mount Everest of psychedelics". Adverse effects of 5-MeO-DMT include sickness, vomiting, headache, chest pressure, fatigue, anxiety, fear, terror, confusion, paranoia, crying, loss of awareness and motor control, and reactivations. The drug acts as a non-selective serotonin receptor agonist, including of the sero ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substituted Tryptamine
Substituted tryptamines, or simply tryptamines, also known as serotonin analogues (i.e., 5-hydroxytryptamine analogues), are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino group, amino (NH2) group via an ethyl (−CH2–CH2−) side chain, sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms. Well-known tryptamines include serotonin, an important neurotransmitter, and melatonin, a hormone involved in regulating the sleep-wake cycle. Tryptamine alkaloids are found in fungi, plants and animals; and sometimes used by humans for the neurological or psychotropic effects of the substance. Prominent examples of tryptamine alkaloids include psilocybin (from "psilocybin mushrooms") and dimethyltryptamine, DMT. In South America, dimethyltryptamine is obtained f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOI (drug)
2,5-Dimethoxy-4-iodoamphetamine (DOI) is a psychedelic drug of the amphetamine and 4-substituted-2,5-dimethoxyamphetamine (DOx) families. It is relatively little-used as a recreational drug but is frequently used in scientific research in the study of psychedelics and serotonin receptors. DOI acts as a potent serotonin 5-HT2 receptor agonist, including of the serotonin 5-HT2A and 5-HT2C receptors. The compound has a stereocenter, and ''R''-(−)-DOI is the more active stereoisomer. 125I">sup>125I''R''-(−)-DOI is used as a radioligand and indicator of the presence of serotonin 5-HT2A receptors in studies. DOI's effects have been compared to LSD, although there are differences that experienced users can distinguish. Besides the longer duration of DOI compared to LSD, the trip tends to be more energetic than an LSD trip, with more body load and a different subjective visual experience. The after effects include residual stimulation and difficulty sleeping, which, depen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substituted Phenethylamine
Substituted phenethylamines (or simply phenethylamines) are a chemical class of organic compounds that are based upon the phenethylamine structure; the class is composed of all the derivative (chemistry), derivative compounds of phenethylamine which can be formed by replacing, or substitution reaction, substituting, one or more hydrogen atoms in the phenethylamine core structure with substituents. Phenylethylamines are also generally found to be central nervous system stimulants with many also being entactogens/empathogens, and hallucinogens. Structural classification The structural formula of any substituted phenethylamine contains a phenyl group, phenyl ring that is joined to an amino group, amino (NH) group via a two-carbon substituent, sidechain. Hence, any substituted phenethylamine can be classified according to the substitution of hydrogen atom, hydrogen (H) atoms on phenethylamine's phenyl ring, sidechain, or amino group with a moiety (chemistry), specific group of at ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonergic Psychedelic
Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic hallucinogens or serotonergic hallucinogens, the term ''psychedelic'' is sometimes used more broadly to include various other types of hallucinogens as well, such as those which are atypical or adjacent to psychedelia like salvia and MDMA, respectively. Classic psychedelics generally cause specific psychological, visual, and auditory changes, and oftentimes a substantially altered state of consciousness. They have had the largest influence on science and culture, and include mescaline, LSD, psilocybin, and DMT. There are a large number of both naturally occurring and synthetic serotonergic psychedelics. Most psychedelic drugs fall into one of the three families of chemical compounds: tryptamines, phenethylamines, or lysergamides. They pro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypolocomotion
Locomotor activity is a measure of animal behavior which is employed in scientific research. Hyperlocomotion, also known as locomotor hyperactivity, hyperactivity, or increased locomotor activity, is an effect of certain drugs in animals in which locomotor activity (locomotion) is increased. It is induced by certain drugs like psychostimulants and NMDA receptor antagonists and is reversed by certain other drugs like antipsychotics and certain antidepressants. Stimulation of locomotor activity is thought to be mediated by increased signaling in the nucleus accumbens, a major brain area involved in behavioral activation and motivation, motivated behavior. Hypolocomotion, also known as locomotor hypoactivity, hypoactivity, and decreased locomotor activity, is an effect of certain drugs in animals in which locomotor activity is decreased. It is a characteristic effect of many sedative agents and general anesthetics. Antipsychotics, which are dopamine receptor antagonists, and many s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
