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DOM-CR
DOM-CR, or DOM/CR, an acronym of "DOM-conformationally restrained", is a tetrahydroisoquinoline (THIQ) and cyclized phenethylamine related to the psychedelics DOM and 2C-D. It is a cyclized THIQ analogue of DOM and 2C-D. DOM-CR shows more than 20-fold reduced affinity for the serotonin 5-HT2A receptor compared to DOM (Ki = 2,150nM vs. 100nM, respectively). In contrast to DOM, DOM-CR does not substitute for DOM in rodent drug discrimination tests, suggesting that it lacks psychedelic effects. Similarly, DOM-CR does not substitute for dextroamphetamine or MDMA, suggesting that it likewise lacks stimulant or entactogenic effects. However, DOM-CR does substitute for TDIQ (MDTHIQ), a selective α2-adrenergic receptor ligand. At high doses, DOM-CR produces behavioral disruption in drug discrimination tests. In contrast to DOM and amphetamine, DOM-CR does not produce hyperlocomotion in rodents. DOM-CR was first described in the scientific literature by Richard Glennon and colleag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substituted Tetrahydroisoquinoline
A substituted tetrahydroisoquinoline is a tetrahydroisoquinoline with one or more chemical substituents. Many simple tetrahydroisoquinoline alkaloids related to mescaline are known and occur naturally in cactus species such as peyote (''Lophophora williamsii'') and ''Pachycereus pringlei'' among many others. Simple tetrahydroisoquinolines may be thought of as cyclized phenethylamines. As an example, anhalinine may be thought of as a cyclic compound, cyclized structural analog, analogue of mescaline. The simple tetrahydroisoquinolines are analogous in concept to the substituted β-carboline, β-carbolines and harmala alkaloids, which can be considered cyclized analogues of substituted tryptamine, tryptamines. Some of the simple tetrahydroisoquinolines, for instance pellotine, are known to be pharmacology, pharmacologically active, although none are known to have hallucinogenic activity. Known activities of simple tetrahydroisoquinolines include sedative and hypnotic effects, monoam ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclized 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 compounds of phenethylamine which can be formed by replacing, or 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 ring that is joined to an amino (NH) group via a two-carbon sidechain. Hence, any substituted phenethylamine can be classified according to the substitution of hydrogen (H) atoms on phenethylamine's phenyl ring, sidechain, or amino group with a specific group of atoms. Several classes of substances can be considered phenylethylamine derivatives such as Substituted amphetamines, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetrahydroisoquinoline
Tetrahydroisoquinoline (TIQ or THIQ), also known as AMPH-CR, is an organic compound with the chemical formula C9H11N. Classified as a secondary amine, it is derived from isoquinoline by hydrogenation. It is a colorless viscous liquid that is miscible with most organic solvents. The tetrahydroisoquinoline skeleton is encountered in a number of bioactive compounds and drugs. Pharmacology THIQ is a conformationally restrained (CR) or cyclized analogue of β-phenethylamine and amphetamine and is also known as AMPH-CR. In contrast to amphetamine however, THIQ fails to substitute for dextroamphetamine in rodent drug discrimination tests, suggesting that it lacks stimulant effects. Similar findings have been made for other tetrahydroisoquinoline analogues of psychoactive phenethylamines, for instance DOM-CR. In any case, THIQ does substitute for TDIQ (MDTIQ), a selective α2-adrenergic receptor ligand, indicating that it is not pharmacologically inactive. Reactions As a secon ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TDIQ
TDIQ, also known as MDTHIQ or MDA-CR, is a tetrahydroisoquinoline drug used in scientific research, which has anxiolytic and anorectic effects in animals. It has an unusual effects profile in animals, with the effects generalising to cocaine and partially to MDMA and ephedrine, but the effects did not generalise to amphetamine and TDIQ does not have any stimulant effects. It is thought these effects are mediated via a partial agonist action at Alpha-2 adrenergic receptors, and TDIQ has been suggested as a possible drug for the treatment of cocaine dependence. See also * Substituted tetrahydroisoquinoline * AMPH-CR and DOM-CR * MDAI * MDAT * Norsalsolinol * Tetrahydroisoquinoline Tetrahydroisoquinoline (TIQ or THIQ), also known as AMPH-CR, is an organic compound with the chemical formula C9H11N. Classified as a secondary amine, it is derived from isoquinoline by hydrogenation. It is a colorless viscous liquid that is mis ... * C10H11NO2 References Alpha-2 adrenergic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT6 Receptor
The 5HT6 receptor is a subtype of 5HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gs and mediates excitatory neurotransmission. ''HTR6'' denotes the human gene encoding for the receptor. Distribution The 5HT6 receptor is expressed almost exclusively in the brain. It is distributed in various areas including, but not limited to, the olfactory tubercle, cerebral cortex ( frontal and entorhinal regions), nucleus accumbens, striatum, caudate nucleus, hippocampus, and the molecular layer of the cerebellum. Based on its abundance in extrapyramidal, limbic, and cortical regions it can be suggested that the 5HT6 receptor plays a role in functions like motor control, emotionality, cognition, and memory. Function Blockade of central 5HT6 receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas, whereas activation enh ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1D Receptor
5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding it. 5-HT1D acts on the central nervous system, and affects locomotion and anxiety. It also induces vasoconstriction in the brain. Tissue distribution 5HT1D receptors are found at low levels in the basal ganglia (globus pallidus, substantia nigra, caudate putamen), the hippocampus, and in the cortex. Structure 5HT1D receptor is a G protein linked receptor that activates an intracellular messenger cascade to produce an inhibitory response by decreasing cellular levels of cAMP. The 5HT1D is a 7-TM receptor. A large intercellular loop between TM-5 and TM-6 is believed to be associated with coupling to a second messenger. Agonists might bind in a manner that utilizes an aspartate residue in TM-3 and residues in the TM-4, TM-5 and TM-6. A human clone containing an intronless open reading frame was found to encode 377 amino acids of the 5HT1D receptor. The ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmacological Activity
In pharmacology, biological activity or pharmacological activity describes the beneficial or adverse effects of a drug on living matter. When a drug is a complex chemical mixture, this activity is exerted by the substance's active ingredient or pharmacophore but can be modified by the other constituents. Among the various properties of chemical compounds, pharmacological/biological activity plays a crucial role since it suggests uses of the compounds in the medical applications. However, chemical compounds may show some adverse and toxic effects which may prevent their use in medical practice. Biological activity is usually measured by a bioassay and the activity is generally dosage-dependent, which is investigated via dose-response curves. Further, it is common to have effects ranging from beneficial to adverse for one substance when going from low to high doses. Activity depends critically on fulfillment of the ADME criteria. To be an effective drug, a compound not only must ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2 Receptor
The 5-HT2 receptors are a subfamily of 5-HT receptors that bind the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). The 5-HT2 subfamily consists of three G protein-coupled receptor G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related ...s (GPCRs) which are coupled to Gq/G11 and mediate excitatory neurotransmission, including 5-HT2A, 5-HT2B, and 5-HT2C. For more information, please see the respective main articles of the individual subtypes: * 5-HT2A receptor * 5-HT2B receptor * 5-HT2C receptor See also * 5-HT1 receptor * 5-HT3 receptor * 5-HT4 receptor * 5-HT5 receptor * 5-HT6 receptor * 5-HT7 receptor * 5-HT2 antagonists References {{Serotonergics Serotonin receptors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monoamine Transporter
Monoamine transporters (MATs) are proteins that function as integral Cell membrane, plasma-membrane Neurotransmitter transporter, transporters to regulate concentrations of extracellular monoamine neurotransmitters. The three major classes are serotonin transporters (SERTs), dopamine transporters (DATs), and norepinephrine transporters (NETs) and are responsible for the reuptake of their associated amine neurotransmitters (serotonin, dopamine, and norepinephrine). MATs are located just outside the synaptic cleft (peri-synaptically), transporting monoamine transmitter overflow from the synaptic cleft back to the cytoplasm of the pre-synaptic neuron. MAT regulation generally occurs through protein phosphorylation and post-translational modification. Due to their significance in neuronal signaling, MATs are commonly associated with drugs used to Psychiatric medication, treat mental disorders as well as recreational drugs. Compounds targeting MATs range from medications such as the wi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Conformational Restriction
In chemistry, rotamers are chemical species that differ from one another primarily due to rotations about one or more single bonds. Various arrangements of atoms in a molecule that differ by rotation about single bonds can also be referred to as conformations. Conformers/rotamers differ little in their energies, so they are almost never separable in a practical sense. Rotations about single bonds are subject to small energy barriers. When the time scale for interconversion is long enough for isolation of individual rotamers (usually arbitrarily defined as a half-life of interconversion of 1000 seconds or longer), the species are termed atropisomers (''see:'' atropisomerism). The ring-flip of substituted cyclohexanes constitutes a common form of conformers. The study of the energetics of bond rotation is referred to as conformational analysis. In some cases, conformational analysis can be used to predict and explain product selectivity, mechanisms, and rates of reactions. Conform ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
