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CYB-210010
CYB210010, also known as 2C-T-TFM or 2C-T-36 and as 2,5-dimethoxy-4-(trifluoromethylsulfanyl)phenethylamine, is a lesser-known psychedelic drug of the phenethylamine family related to compounds such as 2C-T and 2C-T-21. Alexander Shulgin attempted to synthesise this compound in the 1990s, and mentions it in his book PiHKAL under the entry for 2C-T-21, but was unsuccessful in producing a key intermediate and never assigned it a 2C-T number. This compound was ultimately first synthesised by Geoffrey Varty and colleagues at Irish biopharmaceutical company Cybin in 2023. It has a Ki of 0.35nM at the serotonin 5-HT2A receptor, and an of 4.1nM at the serotonin 5-HT2A receptor and 7.3nM at the serotonin 5-HT2C receptor, compared to 88nM at the serotonin 5-HT2B receptor. It is a potent, selective, long acting, and orally active agonist for the serotonin 5-HT2A and 5-HT2C receptors and produces psychedelic-like responding in several different animal species. The interactions ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2C-T
2C-T, or 2C-T-1, also known as 4-methylthio-2,5-dimethoxyphenethylamine, is a psychedelic and hallucinogenic drug of the 2C family. It is used by some as an entheogen. It has structural and pharmacodynamic properties similar to the drugs mescaline and 2C-T-2. Effects In ''TiHKAL'', Alexander Shulgin lists a dose range of 60 to 100mg and a duration of 3 to 5hours for 2C-T. It produces psychedelic and MDMA-like effects. Interactions Pharmacology 2C-T shows affinity for the serotonin 5-HT2 receptors and is known to act as an agonist of the serotonin 5-HT2A and 5-HT2B receptors. The mechanism that produces 2C-T's hallucinogenic and entheogenic effects has not been specifically established, however it is most likely to result from serotonin 5-HT2A receptor activation in the brain, a mechanism of action shared by all of the hallucinogenic tryptamines and phenethylamines for which the mechanism of action is known. 2C-T shows no affinity for the monoamine transporters. Chemistry 2 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
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] |
5-HT2C Receptor
The 5-HT2C receptor is a subtype of the 5-HT2 receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Like all 5-HT2 receptors, it is a G protein-coupled receptor (GPCR) that is coupled to Gq/G11 and mediates excitatory neurotransmission. ''HTR2C'' denotes the human gene encoding for the receptor, that in humans is located on the X chromosome. As males have one copy of the gene and females have one of the two copies of the gene repressed, polymorphisms at this receptor can affect the two sexes to differing extent. Structure At the cell surface the receptor exists as a homodimer. The crystal structure has been known since 2018. Distribution 5-HT2C receptors are located mainly in the choroid plexus, and in rats is also found in many other brain regions in high concentrations, including parts of the hippocampus, anterior olfactory nucleus, substantia nigra, several brainstem nuclei, amygdala, subthalamic nucleus and lateral habenula. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYB004
CYB004, or CYB-004, also known as deuterated dimethyltryptamine (dDMT), is a serotonergic psychedelic related to dimethyltryptamine (DMT) which is under development for the treatment of generalized anxiety disorder. It is administered by inhalation or intravenous injection. It is a tryptamine derivative and is a deuterated analogue and form of DMT. The pharmacodynamic profile of CYB004, including its interactions with serotonin receptors and its effects in animals, is similar to that of DMT. As with DMT, CYB004 is a potent agonist of the serotonin 5-HT2A receptor and produces psychedelic-like effects in animals. However, CYB004, due to its deuteration, is more resistant to metabolism than DMT and shows a longer elimination half-life (by 2.5- to 2.9-fold) and slower clearance (by 38 to 55%) in animals. The brain to plasma ratio of CYB004 was also increased (by 30%) relative to DMT, indicating slightly greater central permeability as well. As of August 2024, CYB004 is in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYB003
CYB003, or CYB-003, also known as deuterated psilocybin analogue, is a serotonergic psychedelic related to psilocybin which is under development for the treatment of major depressive disorder, alcoholism, and other psychiatric disorders. It is taken by mouth. It is a tryptamine derivative and is a deuterated analogue of psilocybin and psilocin. The pharmacodynamic profile of CYB003, including its interactions with serotonin receptors and its effects in animals, is similar to that of psilocin. As with psilocin, CYB003 is a potent agonist of the serotonin 5-HT2A receptor and produces psychedelic-like effects in animals. However, it was developed to have improved pharmacokinetic properties compared to psilocybin, including reduced variability in circulating levels, a faster onset of action, and a shorter duration. As of October 2024, CYB003 is in phase 3 clinical trials for major depressive disorder and is in the preclinical stage of development for alcoholism and other psy ... [...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] |
CYB005
CYB005, or CYB-005, also known as deuterated phenethylamine derivative, is a serotonin receptor agonist and serotonergic psychedelic which is under development for use at non-hallucinogenic doses in the treatment of psychiatric disorders and neuroinflammation. Pharmacology CYB005 acts as a serotonin receptor agonist and is a serotonergic psychedelic. In addition, CYB005 may also inhibit serotonin and dopamine Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized ... reuptake. Chemistry It is a substituted phenethylamine, phenethylamine chemical derivative, derivative and a deuteration, deuterated chemical compound, compound. The exact chemical structure of CYB005 does not yet seem to have been disclosed. However, it appears to be closely related to CYB210010, which itself is non-deutera ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Deuteration
Deuterium (hydrogen-2, symbol H or D, also known as heavy hydrogen) is one of two Stable isotope ratio, stable isotopes of hydrogen; the other is protium, or hydrogen-1, H. The deuterium atomic nucleus, nucleus (deuteron) contains one proton and one neutron, whereas the far more common H has no neutrons. The name ''deuterium'' comes from Greek ''Wikt:δεύτερος, deuteros'', meaning "second". American chemist Harold Urey discovered deuterium in 1931. Urey and others produced samples of heavy water in which the H had been highly concentrated. The discovery of deuterium won Urey a List of Nobel laureates in Chemistry, Nobel Prize in 1934. Nearly all deuterium found in nature was Big Bang nucleosynthesis, synthesized in the Big Bang 13.8 billion years ago, forming the primordial ratio of H to H (~26 deuterium nuclei per 10 hydrogen nuclei). Deuterium is subsequently produced by the slow stellar proton–proton chain, but rapidly destroyed by exothermic Nuclear fusio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Preclinical Research
In drug development, preclinical development (also termed preclinical studies or nonclinical studies) is a stage of research that begins before clinical trials (testing in humans) and during which important feasibility, iterative testing and drug safety data are collected, typically in laboratory animals. The main goals of preclinical studies are to determine a starting, safe dose for first-in-human study and assess potential toxicity of the product, which typically include new medical devices, prescription drugs, and diagnostics. Companies use stylized statistics to illustrate the risks in preclinical research, such as that on average, only one in every 5,000 compounds that enters drug discovery to the stage of preclinical development becomes an approved drug. Types Each class of product may undergo different types of preclinical research. For instance, drugs may undergo pharmacodynamics (what the drug does to the body) (PD), pharmacokinetics (what the body does to t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Biological Target
A biological target is anything within a living organism to which some other entity (like an endogenous ligand or a drug) is directed and/or binds, resulting in a change in its behavior or function. Examples of common classes of biological targets are proteins and nucleic acids. The definition is context-dependent, and can refer to the biological target of a pharmacologically active drug compound, the receptor target of a hormone (like insulin), or some other target of an external stimulus. Biological targets are most commonly proteins such as enzymes, ion channels, and receptors. Mechanism The external stimulus (''i.e.'', the drug or ligand) physically binds to ("hits") the biological target. The interaction between the substance and the target may be: * noncovalent – A relatively weak interaction between the stimulus and the target where no chemical bond is formed between the two interacting partners and hence the interaction is completely reversible. * reversible c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor (biochemistry)
In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and Signal_transduction, transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses, such as a change in the electrophysiology, electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter, inhibits electrical activity of neurons by binding to GABAA receptor, GABA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand (biochemistry), ligand, and integration allows the signal to be incorporated into another biochemical pathway. Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G prote ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Head-twitch Response
The head-twitch response (HTR), also sometimes known as wet dog shakes (WDS) in rats, is a rapid side-to-side head movement that occurs in mice and rats in association with serotonin 5-HT2A receptor activation. Serotonergic psychedelics like lysergic acid diethylamide (LSD) and psilocybin consistently induce the HTR in rodents. Because of this, the HTR is widely employed in scientific research as an animal behavioral model of hallucinogen effects and in the discovery of new psychedelic drugs. The HTR is one of the only behavioral paradigms for assessment of psychedelic-like effects in animals, with the other most notable test being drug discrimination. However, the HTR is far less costly and time-consuming than drug discrimination and hence has become much more popular in recent years. Limitations of the HTR include the fact that various other drugs besides serotonin 5-HT2A receptor agonists, such as NMDA receptor antagonists and muscarinic acetylcholine receptor antagonists, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
