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Dichloropane
Dichloropane ((−)-2β-Carbomethoxy-3β-(3,4-dichlorophenyl)tropane, RTI-111, O-401) is a stimulant of the phenyltropane class that acts as a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) with IC50 values of 3.13, 18, and 0.79 nM, respectively. In animal studies, dichloropane had a slower onset and longer duration of action compared to cocaine. Methylecgonidine is the direct precursor to this compound. Trans -CO2Me group The thermodynamic isomer with a trans -CO2Me group is still active. This isomer was used by Neurosearch to make three different phenyltropanes which were tested in clinical trials. *Tesofensine * Brasofensine *NS-2359 NS-2359 (GSK-372475) is a serotonin-norepinephrine-dopamine reuptake inhibitor. It was under development by GlaxoSmithKline (GSK) as an antidepressant, but was discontinued in 2009 when phase II clinical trials showed the drug was not effective ... (GSK-372,475) See also * 3,4-DCMP * O-2390 * List of cocaine anal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3,4-DCMP
3,4-dichloromethylphenidate (abbreviated as 3,4-DCMP, and incorrectly as 3,4-CTMP for the d,l-threo diastereomer) is a potent stimulant drug from the List of methylphenidate analogues, phenidate class closely related to methylphenidate. It acts as a potent Serotonin–norepinephrine–dopamine reuptake inhibitor, serotonin-norepinephrine-dopamine reuptake inhibitor with a long duration of action. It has been sold online as a designer drug. Chemistry 3,4-DCMP is the 3,4-dichlorinated analogue of methylphenidate. The 3,4-dichlorination is a common modification done to most monoamine reuptake inhibitors. Pharmacology Pharmacodynamics The result of the 3,4-dichlorination on 3,4-DCMP is a higher selectivity for the serotonin transporter and serotonin uptake inhibition. Serotonergic activity among phenidates is very rare, and 3,4-DCMP is one of only three compounds from this class with appreciable serotoninergic activity, the other two being HDMP-28 & HDEP-28. The reason for t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
O-2390
O-2390 (3,4-Dichloro-alpha-PVP, DCPVP) is a recreational designer drug from the substituted cathinone family, which acts as a potent inhibitor of dopamine and noradrenaline reuptake ''in vitro'', with weaker but still significant inhibition of serotonin reuptake. See also * 3F-PVP * 4F-PVP * 4Cl-PVP * 3,4-DCMP * Chlorosipentramine * Cilobamine * Dichloropane * LR-5182 * MDPV * MFPVP * Naphyrone * Sertraline Sertraline, sold under the brand name Zoloft among others, is an Antidepressant, antidepressant medication of the selective serotonin reuptake inhibitor (SSRI) class used to treat major depressive disorder, generalized anxiety disorder, socia ... * TH-PVP References Alpha-Propylphenethylamines Designer drugs Pyrrolidinophenones Serotonin-norepinephrine-dopamine releasing agents {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RTI Compounds
RTI or Rti may refer to: Broadcasters * Radiodiffusion Television Ivoirienne, state broadcaster of Ivory Coast * Radio Taiwan International, an international radio station in Taiwan * Reti Televisive Italiane, a subsidiary of Italian media company Mediaset * Rádio e Televisão Independente, a proposed Portuguese television channel Other businesses * RTI International, formerly Research Triangle Institute, a not-for-profit American research organization * RTI International Metals, an American company producing titanium * RTI Producciones, a Colombian television production company In science and technology In computing and telecommunications * Run-time infrastructure (simulation) In medicine * Reproductive tract infection * Respiratory tract infection * Reverse-transcriptase inhibitor, a class of antiretroviral drug Other uses in science and technology * Ramp travel index, a measure of an off road vehicle articulation, ability to keep all wheels in contact with th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union, Australia, and New Zealand, as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these designer drugs were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Cocaine Analogues
This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel chemical compound from (often the starting point of natural) cocaine's molecular structure, with the result product sufficiently similar to cocaine to display similarity in, but alteration to, its chemical function. Within the scope of analogous compounds created from the structure of cocaine, so named "cocaine analogues" retain 3''β''-benzoyloxy or similar functionality (the term specifically used usually distinguishes from phenyltropanes, but in the broad sense generally, as a category, includes them) on a tropane skeleton, as compared to other stimulants of the kind. Many of the semi-synthetic cocaine analogues ''proper'' which have been made & studied have consisted of among the nine following classes of compounds: * stereoisomers of cocaine * 3''β''-phenyl ring substituted analogues * 2''β''-substituted analogues * ''N''-modified analogues of cocaine * 3''β''-carbamoyl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stimulant
Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, Mood disorder, mood, and physical activity, physical performance. Some stimulants occur naturally, while others are exclusively synthetic. Common stimulants include caffeine, nicotine, amphetamines, cocaine, methylphenidate, and modafinil. Stimulants may be subject to varying forms of regulation, or outright prohibition, depending on jurisdiction. Stimulants increase activity in the sympathetic nervous system, either directly or indirectly. Prototypical stimulants increase synaptic concentrations of neurotransmitter, excitatory neurotransmitters, particularly norepinephrine and dopamine (e.g., methylphenidate). Other stimulants work by binding to the Receptor (biochemistry), receptors of excitatory neurotransmitters (e.g., nicotine) or by ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenyltropane
Phenyltropanes (PTs) were originally developed to reduce cocaine addiction and dependency. In general these compounds act as inhibitors of the plasmalemmal monoamine reuptake transporters. This research has spanned beyond the last couple decades, and has picked up its pace in recent times, creating numerous phenyltropanes as research into cocaine analogues garners interest to treat addiction. Uses Addiction The phenyltropane compounds were initially discovered by R. Clarke et al. during research to try and dissociate the stimulant properties of cocaine from its abuse and dependence liability. The first simple phenyltropanes to be made (WIN 35065-2 and WIN 34,428) were shown to be active in behavioral assays only for the ββ-isomers. The activity of the corresponding αβ-isomers was disappointing. It was later shown that WIN 35065-2 and WIN 34,428 are mostly dopamine selective reuptake inhibitors with some residual actions at the norepinephrine transporter (NET) and seroton ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NS-2359
NS-2359 (GSK-372475) is a serotonin-norepinephrine-dopamine reuptake inhibitor. It was under development by GlaxoSmithKline (GSK) as an antidepressant, but was discontinued in 2009 when phase II clinical trials showed the drug was not effective and not well tolerated. The results did not support further effort by the company. NS-2359 was also in clinical trials for the treatment of ADHD, phase II having been completed in 2007. A phase I clinical trial exploring the effect of NS-2359 on cocaine- dependent individuals was completed in 2002. See also * Tesofensine Tesofensine (NS2330) is a serotonin-noradrenaline-dopamine reuptake inhibitor, serotonin–noradrenaline–dopamine reuptake inhibitor from the phenyltropane family of drugs, which is being developed for the treatment of obesity. Tesofensine was ... References Methoxy compounds Serotonin–norepinephrine–dopamine reuptake inhibitors Chlorobenzene derivatives Tropanes Abandoned drugs {{nervous-s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Brasofensine
Brasofensine (NS-2214, BMS-204756) is a phenyltropane dopamine reuptake inhibitor that had been under development by Bristol-Myers Squibb and defunct company NeuroSearch for the treatment of Parkinson's and Alzheimer's diseases. History In 1996, brasofensine entered phase I trials in the United States and phase II trials in Denmark. From 1996 to 1999, Bristol-Myers Squibb (BMS) was involved in development and testing before exiting the collaboration with NeuroSearch. In 2001, its development was confirmed to be discontinued. Pharmacology In animal models of Parkinson's disease, brasofensine was effective in stimulating locomotor activity and reversing akinesia. Phase II trials in humans were conducted in 1996 and brasofensine was shown to be both effective and well tolerated at a dose of 4 mg; however, development was stopped after ''in vivo'' cis-anti isomerization of the 2α-methyloxime group was reported. In Parkison's disease, symptoms do not begin to manifest until ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
