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Methylphenylpiracetam
Methylphenylpiracetam is a derivative of piracetam and a positive allosteric modulator of the sigma-1 receptor. It differs from phenylpiracetam by having a methyl group. E1R is the (4''R'',5''S'') stereoisomer of methylphenylpiracetam. Enantiomers The two R-configuration enantiomers, i.e. (4''R'',5''S'') and (4''R'',5''R''), of methylphenylpiracetam are more active positive allosteric modulators of the sigma-1 receptor than the two S-configuration enantiomers, i.e. (4''S'',5''R'') and (4''S'',5''S''). Effects E1R enhances cognition and has efficacy against cholinergic dysfunction in mice without affecting locomotor activity. Pretreatment with E1R enhanced the σ1R agonist PRE-084's stimulating effect and facilitated passive avoidance retention. It alleviated scopolamine-induced cognitive impairment. The cognition enhancing activity of E1R is higher than that of (''R'')-phenylpiracetam. Because E1R had no effect on locomotor activity, it was found to be free of potential ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Racetams
Racetams are a class of drugs that share a pyrrolidone nucleus. Some, such as piracetam, aniracetam, oxiracetam, pramiracetam and phenylpiracetam are considered nootropics. Others such as levetiracetam, brivaracetam, and seletracetam are anticonvulsants. Mechanism There is no universally accepted mechanism of action for racetams. Racetams generally show negligible affinity for common central nervous system receptors, but modulation of central neurotransmitters, including acetylcholine and glutamate, has been reported. Although aniracetam and nebracetam show affinity for muscarinic receptors, only nefiracetam demonstrates nanomolar interactions. Modification of membrane-located mechanisms of central signal transduction is another hypothesis. Like some ampakines, some racetams such as piracetam and aniracetam are positive allosteric modulators of the AMPA receptor. Racetams are understood to work by allosterically modulating glutamate receptors, specifically AMPA receptors, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma-1 Receptor
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the ''SIGMAR1'' gene. The σ1 receptor is a transmembrane protein expressed in many different tissue types. It is particularly concentrated in certain regions of the central nervous system. It has been implicated in several phenomena, including cardiovascular function, schizophrenia, clinical depression, the effects of cocaine abuse, and cancer. Much is known about the binding affinity of hundreds of synthetic compounds to the σ1 receptor. An endogenous ligand for the σ1 receptor has yet to be conclusively identified, but tryptaminergic trace amines and neuroactive steroids have been found to activate the receptor. Especially progesterone, but also testosterone, pregnenolone sulfate, and dehydroepiandrosterone sulfate (DHEA-S) bind to the σ1 receptor. C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenylpiracetam
Phenylpiracetam (INN: fonturacetam, brand names Phenotropil Фенотропил, Carphedon), is a phenylated analog of the drug piracetam. It was developed in 1983 as a medication for Soviet Cosmonauts to treat the prolonged stresses of working in space. Phenylpiracetam was created at the Russian Academy of Sciences Institute of Biomedical Problems in an effort led by psychopharmacologist Valentina Ivanovna Akhapkina (Валентина Ивановна Ахапкина). In Russia it is now available as a prescription drug. Research on animals has indicated that phenylpiracetam may have anti-amnesic, antidepressant, anticonvulsant, anxiolytic, and memory enhancement effects. Uses A few small clinical studies have shown possible links between prescription of phenylpiracetam and improvement in a number of encephalopathic conditions, including lesions of cerebral blood pathways, traumatic brain injury and certain types of glioma. Phenylpiracetam reverses the depressant ef ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Passive Avoidance
Passive may refer to: * Passive voice, a grammatical voice common in many languages, see also Pseudopassive * Passive language, a language from which an interpreter works * Passivity (behavior), the condition of submitting to the influence of one's superior * Passive-aggressive behavior, resistance to following through with expectations in interpersonal or occupational situations * Passive income, income resulting from cash flow received on a regular basis * Passive immunity, the transfer of active humoral immunity * Passive experience, observation lacking recipricol interaction; and wrought with delusion of control. Science and technology * Passivation (chemistry), process of making a material "passive" in relation to another material prior to using the materials together * Passivity (engineering) a property of engineering systems, particularly in analog electronics and control systems * Passive solar building design, which uses (or avoids) sunlight as an energy source without ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diastereomer
In stereochemistry, diastereomers (sometimes called diastereoisomers) are a type of stereoisomer. Diastereomers are defined as non-mirror image, non-identical stereoisomers. Hence, they occur when two or more stereoisomers of a compound have different configurations at one or more (but not all) of the equivalent (related) stereocenters and are not mirror images of each other. When two diastereoisomers differ from each other at only one stereocenter, they are epimers. Each stereocenter gives rise to two different configurations and thus typically increases the number of stereoisomers by a factor of two. Diastereomers differ from enantiomers in that the latter are pairs of stereoisomers that differ in all stereocenters and are therefore mirror images of one another. Enantiomers of a compound with more than one stereocenter are also diastereomers of the other stereoisomers of that compound that are not their mirror image (that is, excluding the opposing enantiomer). Diastereomers h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Standard For The Uniform Scheduling Of Medicines And Poisons
The Standard for the Uniform Scheduling of Medicines and Poisons (SUSMP) is an Australian legislative instrument produced by the Therapeutic Goods Administration (TGA)., subsection 4A. Before 2010, it was known as the ''Standard for the Uniform Scheduling of Drugs and Poisons'' (''SUSDP'').. The SUSMP classifies drugs and poisons into different Schedules signifying the degree of control recommended to be exercised over their availability to the public.. , the most recent version is the ''Poisons Standard October 2022''. The Schedules are referred to under State and Territory legislation for regulatory purposes. Although each State and Territory has its own laws, the vast majority of medicines and poisons are classified according to the SUSMP to achieve uniform national regulation. Schedules Schedule 1 Schedule 1 is blank. Schedule 1 does not currently contain any medicines or poisons. Schedule 2: Pharmacy Medicine Schedule 2 (S2) drugs and poisons, otherwise known ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Extrapyramidal Symptoms
Extrapyramidal symptoms (EPS) are symptoms that are archetypically associated with the extrapyramidal system of the brain's cerebral cortex. When such symptoms are caused by medications or other drugs, they are also known as extrapyramidal side effects (EPSE). The symptoms can be acute (short-term) or chronic (long-term). They include movement dysfunction such as dystonia (continuous spasms and muscle contractions), akathisia (may manifest as motor restlessness), parkinsonism characteristic symptoms such as rigidity, bradykinesia (slowness of movement), tremor, and tardive dyskinesia (irregular, jerky movements). Extrapyramidal symptoms are a reason why subjects drop out of clinical trials of antipsychotics; of the 213 (14.6%) subjects that dropped out of one of the largest clinical trials of antipsychotics (the CATIE trial (Clinical Antipsychotic Trials for Intervention Effectiveness), which included 1460 randomized subjects), 58 (27.2%) of those discontinuations were due to E ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cognitive Impairment
Cognitive deficit is an inclusive term to describe any characteristic that acts as a barrier to the cognition process. The term may describe * deficits in overall intelligence (as with intellectual disabilities), * specific and restricted deficits in cognitive abilities (such as in learning disorders like dyslexia), * neuropsychological deficits (such as in attention, working memory or executive function), * or it may describe drug-induced impairment in cognition and memory (such as that seen with alcohol, glucocorticoids, and the benzodiazepines.) Cause It usually refers to a durable characteristic, as opposed to altered level of consciousness, which may be acute and reversible. Cognitive deficits may be inborn or caused by environmental factors such as brain injuries, neurological disorders, or mental illness. Screening Screening for cognitive impairment in those over the age of 65 without symptoms is of unclear benefit versus harm as of 2020. In a large population-base ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyoscine Hydrobromide
Scopolamine, also known as hyoscine, or Devil's Breath, is a natural or synthetically produced tropane alkaloid and anticholinergic drug that is formally used as a medication for treating motion sickness and postoperative nausea and vomiting. It is also sometimes used before surgery to decrease saliva. When used by injection, effects begin after about 20 minutes and last for up to 8 hours. It may also be used orally and as a transdermal patch since it has been long known to have transdermal bioavailability Scopolamine is in the antimuscarinic family of drugs and works by blocking some of the effects of acetylcholine within the nervous system. Scopolamine was first written about in 1881 and started to be used for anesthesia around 1900. Scopolamine is also the main active component produced by certain plants of the nightshade family, which historically have been used as psychoactive drugs (known as ''deliriants'') due to their antimuscarinic-induced hallucinogenic ef ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Derivative (chemistry)
In chemistry, a derivative is a compound that is derived from a similar compound by a chemical reaction. In the past, derivative also meant a compound that ''can be imagined to'' arise from another compound, if one atom or group of atoms is replaced with another atom or group of atoms, but modern chemical language now uses the term structural analog for this meaning, thus eliminating ambiguity. The term "structural analogue" is common in organic chemistry. In biochemistry, the word is used for compounds that at least theoretically can be formed from the precursor compound. Chemical derivatives may be used to facilitate analysis. For example, melting point (MP) analysis can assist in identification of many organic compounds. A crystalline derivative may be prepared, such as a semicarbazone or 2,4-dinitrophenylhydrazone (derived from aldehydes or ketones), as a simple way of verifying the identity of the original compound, assuming that a table of derivative MP values is available ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PRE-084
PRE-084 is a sigma receptor agonist, selective for the σ1 subtype. It has nootropic and antidepressant actions in animal studies, as well as antitussive and reinforcing effects. PRE-084 increases the expression of GDNF Glial cell line-derived neurotrophic factor (GDNF) is a protein that, in humans, is encoded by the ''GDNF'' gene. GDNF is a small protein that potently promotes the survival of many types of neurons. It signals through GFRα receptors, particula .... Synthesis Sodium hydride mediated alkylation between Benzyl cyanide (1) and 1,5-dibromopentane 11-24-0(2) gives 1-phenylcyclohexanecarbonitrile 201-23-2(3). Hydrolysis of the nitrile by treatment with aqueous potassium hydroxide in DEG gives 1-phenylcyclohexanecarboxylic acid 135-67-7(4). Halogenation with thionyl chloride gives 1-phenylcyclohexanecarbonyl chloride 890-42-8 This intermediate was not isolated but reacted with 2-morpholinoethanol 22-40-2(5) to give the ester and hence, completing the synth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piracetam
Piracetam is a drug marketed as a treatment for myoclonus. It is also used as a cognitive enhancer to improve memory, attention, and learning. Evidence to support its use is unclear, with some studies showing modest benefits in specific populations and others showing minimal or no benefit. Piracetam is sold as a medication in many European countries. Sale of piracetam is not illegal in the United States, although it is not regulated nor approved by the FDA so it is legally sold for research use only. Piracetam is in the racetams group, with chemical name ''2-oxo-1-pyrrolidine acetamide''. It is a derivative of the neurotransmitter GABA and shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid. Piracetam is a cyclic derivative of GABA (gamma-aminobutyric acid). Related drugs include the anticonvulsants levetiracetam and brivaracetam, and the putative nootropics aniracetam and phenylpiracetam. Efficacy Dementia A 2001 Cochrane review concluded that there was n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
