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JJC8-089
JJC8-089 is a dopamine reuptake inhibitor (DRI) that was chemical derivative, derived from modafinil and is related to JJC8-016, JJC8-088, and JJC8-091. Its affinity (pharmacology), affinity (Ki) for the dopamine transporter (DAT) is 37.8nM, for the norepinephrine transporter (NET) is 11,820nM (313-fold lower than for the DAT), for the serotonin transporter (SERT) is 6,800nM (180-fold lower than for the DAT), and for the sigma receptor, sigma sigma-1 receptor, σ1 receptor is 2.24nM (17-fold higher than for the DAT). It also has significant affinity for several dopamine receptors. JJC8-089 has substantially higher affinity for the DAT than modafinil. The drug shows pro-motivational agent, pro-motivational effects in animals. It was first described in the scientific literature by 2016. See also * List of modafinil analogues and derivatives References Dopamine reuptake inhibitors 4-Fluorophenyl compounds Pro-motivational agents Sigma receptor modulators Thioethers Stimulan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JJC8-091
JJC8-091 is an atypical dopamine reuptake inhibitor (DRI) that was chemical derivative, derived from modafinil. It is a lead chemical compound, compound for potential treatment of psychostimulant use disorder (PSUD) and is under development by Encepheal Therapeutics for use as a pharmaceutical drug. The affinity (pharmacology), affinity (Ki) of JJC8-091 for the dopamine transporter (DAT) is 230 to 289nM. In another study however, its affinities for the monoamine transporters were 16.7nM for the DAT, 17,800nM for the norepinephrine transporter (NET) (1,066-fold lower than for the DAT), and 1,770nM for the serotonin transporter (SERT) (106-fold lower than for the DAT). It has substantially higher affinity for the DAT than modafinil (Ki = 2,600–8,160nM). Besides the DAT, JJC8-091 is a sigma receptor, sigma sigma-1 receptor, σ1 receptor ligand (biochemistry), ligand (Ki = 454–1,010nM; 2.0–3.5-fold lower than for the DAT). It also has high affinity for the dopamine receptor, do ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pro-motivational Agents
A motivation-enhancing drug, also known as a pro-motivational drug, is a drug which increases motivation. Drugs enhancing motivation can be used in the treatment of motivational deficits, for instance in depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD). They can also be used in the treatment of disorders of diminished motivation (DDMs), including apathy, abulia, and akinetic mutism, disorders that can be caused by conditions like stroke, traumatic brain injury (TBI), and neurodegenerative diseases. Motivation-enhancing drugs are used non-medically by healthy people to increase motivation and productivity as well, for instance in educational contexts. There are limited clinical data on medications in treating motivational deficits and disorders. In any case, drugs used for pro-motivational purposes are generally dopaminergic agents, for instance dopamine reuptake inhibitors (DRIs) like methylphenidate and modafinil, dopamine releasing agents (DRAs) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Modafinil Analogues And Derivatives
This page lists chemical compounds similar to modafinil, known as modafinil analogues and derivatives. These are structural analogues and derivatives of modafinil, a drug that affects dopamine levels in the brain in an unusual way (atypical dopamine reuptake inhibitor or DRI). Modafinil is a drug that helps keep people awake and alert (wakefulness-promoting agent or "eugeroic"). Most of the listed modafinil analogues are drugs that specifically target dopamine reuptake (reabsorption of a neurotransmitter by a neurotransmitter transporter) with stronger effects ( selective DRIs with improved potency) compared to modafinil. The modafinil analogues are of interest in the potential treatment of a condition involving the misuse of stimulant drugs ( psychostimulant use disorder or PSUD), as drugs that help increase motivation (pro-motivational agents) to treat motivational disorders, and for treatment of neurodegenerative diseases such as Alzheimer's disease. Modafinil analogues ac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pro-motivational Agent
A motivation-enhancing drug, also known as a pro-motivational drug, is a drug which increases motivation. Drugs enhancing motivation can be used in the treatment of motivational deficits, for instance in depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD). They can also be used in the treatment of disorders of diminished motivation (DDMs), including apathy, abulia, and akinetic mutism, disorders that can be caused by conditions like stroke, traumatic brain injury (TBI), and neurodegenerative diseases. Motivation-enhancing drugs are used non-medically by healthy people to increase motivation and productivity as well, for instance in educational contexts. There are limited clinical data on medications in treating motivational deficits and disorders. In any case, drugs used for pro-motivational purposes are generally dopaminergic agents, for instance dopamine reuptake inhibitors (DRIs) like methylphenidate and modafinil, dopamine releasing agents (DRA ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Reuptake Inhibitor
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have been l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Receptor
Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). Dopamine receptors activate different effectors through not only G-protein coupling, but also signaling through different protein (dopamine receptor-interacting proteins) interactions. The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors. Dopamine receptors are implicated in many neurological processes, including motivational and incentive salience, cognition, memory, learning, and fine motor control, as well as modulation of neuroendocrine signaling. Abnormal dopamine receptor signaling and dopaminergic nerve function is implicated in several neuropsychiatric disorders. Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while psychostimulants are typically indirect agonists of dopamine receptors. Subtypes The existence of multiple types of receptors for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thioethers
In organic chemistry, a sulfide (British English sulphide) or thioether is an organosulfur functional group with the connectivity as shown on right. Like many other sulfur-containing compounds, volatile sulfides have foul odors. A sulfide is similar to an ether except that it contains a sulfur atom in place of the oxygen. The grouping of oxygen and sulfur in the periodic table suggests that the chemical properties of ethers and sulfides are somewhat similar, though the extent to which this is true in practice varies depending on the application. Nomenclature Sulfides are sometimes called thioethers, especially in the old literature. The two organic substituents are indicated by the prefixes. (CH3)2S is called dimethylsulfide. Some sulfides are named by modifying the common name for the corresponding ether. For example, C6H5SCH3 is methyl phenyl sulfide, but is more commonly called thioanisole, since its structure is related to that for anisole, C6H5OCH3. The modern systemati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma Receptor Modulators
Sigma ( ; uppercase Σ, lowercase σ, lowercase in word-final position ς; ) is the eighteenth letter of the Greek alphabet. In the system of Greek numerals, it has a value of 200. In general mathematics, uppercase Σ is used as an operator for summation. When used at the end of a letter-case word (one that does not use all caps), the final form (ς) is used. In ' (Odysseus), for example, the two lowercase sigmas (σ) in the center of the name are distinct from the word-final sigma (ς) at the end. The Latin letter S derives from sigma while the Cyrillic letter Es derives from a lunate form of this letter. History The shape (Σς) and alphabetic position of sigma is derived from the Phoenician letter ( ''shin''). Sigma's original name may have been ''san'', but due to the complicated early history of the Greek epichoric alphabets, ''san'' came to be identified as a separate letter in the Greek alphabet, represented as Ϻ. Herodotus reports that "san" was the name giv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Reuptake Inhibitors
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Scientific Literature
Scientific literature encompasses a vast body of academic papers that spans various disciplines within the natural and social sciences. It primarily consists of academic papers that present original empirical research and theoretical contributions. These papers serve as essential sources of knowledge and are commonly referred to simply as "the literature" within specific research fields. The process of academic publishing involves disseminating research findings to a wider audience. Researchers submit their work to reputable journals or conferences, where it undergoes rigorous evaluation by experts in the field. This evaluation, known as peer review, ensures the quality, validity, and reliability of the research before it becomes part of the scientific literature. Peer-reviewed publications contribute significantly to advancing our understanding of the world and shaping future research endeavors. Original scientific research first published in scientific journals co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma Receptor
Sigma receptors (σ-receptors) are protein receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine, and siramesine. There are two subtypes, sigma-1 receptors (σ1) and sigma-2 receptors (σ2), which are classified as sigma receptors for their pharmacological similarities, even though they are evolutionarily unrelated. The fungal protein ERG2, a C-8 sterol isomerase, falls into the same protein family as sigma-1. Both localize to the ER membrane, although sigma-1 is also reported to be a cell surface receptor. Sigma-2 is an EXPERA domain protein with a mostly intracellular (ER membrane) localization. Classification Because the σ-receptor was originally discovered to be agonized by benzomorphan opioids and antagonized by naltrexone, σ-receptors were originally believed to be a type of opioid receptor. When the σ1 receptor was isolated and cloned, it was found to have no structur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
