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4′-Fluorococaine
4′-Fluorococaine is a tropane derivative drug which is a synthetic analogue of cocaine. Unlike related compounds such as the corresponding 4′-fluorophenyltropane derivative CFT and the 2′-hydroxy analogue salicylmethylecgonine, 4′-fluorococaine has only around the same potency as cocaine as an inhibitor of dopamine reuptake, but conversely it is a much stronger serotonin reuptake inhibitor than cocaine, resulting in a significantly altered pharmacological profile in animal studies. See also * pFBT * Cocaethylene * 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 co ... References Tropanes Serotonin–norepinephrine–dopamine reuptake inhibitors Stimulants Local anesthetics Cocaine 4-Fluorophenyl compounds {{Illegal-drug-trade-s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Reuptake Inhibitor
A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin (5-hydroxytryptamine, or 5-HT) by blocking the drug action, action of the serotonin transporter (SERT). This in turn leads to increased extracellular concentrations of serotonin and, therefore, an increase in Serotonin, serotonergic neurotransmission. It is a type of monoamine reuptake inhibitor (MRI); other types of MRIs include dopamine reuptake inhibitors and norepinephrine reuptake inhibitors. SRIs are not synonymous with selective serotonin reuptake inhibitors (SSRIs), as the latter term is usually used to describe the chemical class, class of antidepressants of the same name, and because SRIs, unlike SSRIs, can either be binding selectivity, selective or non-selective in their drug action, action. For example, cocaine, which non-selectively inhibits the reuptake of serotonin, norepinephrine, and dopamine, is an SRI but not an SSRI. SRIs are used pred ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3-(p-Fluorobenzoyloxy)tropane
3β-(''p''-Fluorobenzoyloxy)tropane, (8-Methyl-8-azabicyclo .2.1ct-3-yl 4-fluorobenzoic acid ester, 4-fluorotropacocaine, 3-Pseudotropyl-4-fluorobenzoate, 3-pseudotropyl-4-fluorobenzoate, pFBT) is a tropane derivative drug which acts as a local anaesthetic, having around 30% the stimulant potency of cocaine but around the same potency as a local anaesthetic. It has been investigated as a potential radiolabelled agent for studying receptor binding, but was not adopted for this application. The main application for fluorotropacocaine, however, has been as a designer drug analogue of cocaine, first detected by the EMCDDA in 2008, and subsequently sold as an ingredient of various "bath salt" powder products, usually mixed in combination with other stimulant drugs such as caffeine, dimethocaine, desoxypipradrol or substituted cathinone derivatives. See also * Hygrine * 4′-Fluorococaine * RTI-160 * Tropacocaine * List of cocaine analogues This is a list of cocaine analogue ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salicylmethylecgonine
Salicylmethylecgonine, (2′-Hydroxycocaine) is a tropane derivative drug which is both a synthetic analogue and a possible active metabolite of cocaine. Its potency ''in vitro'' is around 10x that of cocaine, although it is only around three times more potent than cocaine when administered to mice (likely owing to it having a higher LogP: 2.89 than that of cocaine: 2.62) Note however that the compound 2′-Acetoxycocaine would act as a prodrug to Salicylmethylecgonine in humans, and has a more efficient partition coefficient which would act as a delivery system and would circumvent this reason for a drop in potency. Salicylmethylecgonine also shows increased behavioral stimulation compared to cocaine similar to the phenyltropanes. The hydroxy branch renders the molecule a QSAR of a 10-fold increase over cocaine in its binding potency for the dopamine transporter & a 52-fold enhanced affinity for the norepinephrine transporter. It also has a reduced selectivity for the seroton ... [...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] |
Local Anesthetics
A local anesthetic (LA) is a medication that causes absence of all sense, sensation (including pain) in a specific body part without loss of consciousness, providing local anesthesia, as opposed to a general anesthetic, which eliminates all sensation in the entire body and causes unconsciousness. Local anesthetics are most commonly used to eliminate pain during or after surgery. When it is used on specific nerve pathways (local anesthetic nerve block), paralysis (loss of muscle function) also can be induced. Classification LAs are of 2 types: *Clinical LAs: **amino amide LAs **amino ester LAs *Synthetic LAs **Cocaine derivatives Synthetic cocaine-derived LAs differ from cocaine because they have a much lower abuse potential and do not cause hypertension vasoconstriction (with few exceptions). The suffix "-caine" at the ends of these medication names is derived from the word "cocaine", because cocaine was formerly used as a local anesthetic. Examples Short Duration of Actio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stimulants
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, and 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 excitatory neurotransmitters, particularly norepinephrine and dopamine (e.g., methylphenidate). Other stimulants work by binding to the receptors of excitatory neurotransmitters (e.g., nicotine) or by blocking the activity of endogenous agents that promote sleep ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tropanes
Tropane alkaloids are a class of bicyclic .2.1alkaloids and secondary metabolites that contain a tropane ring in their chemical structure. Tropane alkaloids occur naturally in many members of the plant family Solanaceae. Certain tropane alkaloids such as cocaine and scopolamine are notorious for their psychoactive effects, related usage and cultural associations. Particular tropane alkaloids such as these have pharmacological properties and can act as anticholinergics or stimulants. Classification Anticholinergics Anticholinergic drugs and deliriants: * Atropine, racemic hyoscyamine, from the deadly nightshade ('' Atropa belladonna'') * Hyoscyamine, the ''levo''-isomer of atropine, from henbane ('' Hyoscyamus niger''), mandrake ('' Mandragora officinarum'') and the sorcerers' tree ('' Latua pubiflora''). * Scopolamine, from henbane and ''Datura'' species (Jimson weed) All three acetylcholine-inhibiting chemicals can also be found in the leaves, stems, and flowers ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cocaethylene
Cocaethylene (ethylbenzoylecgonine) is the ethyl ester of benzoylecgonine. It is structurally similar to cocaine, which is the methyl ester of benzoylecgonine. Cocaethylene is formed by the liver in small amounts when cocaine and ethanol coexist in the blood. In 1885, cocaethylene was first synthesized (according to edition 13 of the ''Merck Index''), and in 1979, cocaethylene's side effects were discovered. Metabolic production from cocaine Cocaethylene is the byproduct of concurrent consumption of alcohol and cocaine as metabolized by the liver. Normally, metabolism of cocaine produces two primarily biologically inactive metabolites— benzoylecgonine and ecgonine methyl ester. The hepatic enzyme carboxylesterase is an important part of cocaine's metabolism because it acts as a catalyst for the hydrolysis of cocaine in the liver, which produces these inactive metabolites. If ethanol is present during the metabolism of cocaine, a portion of the cocaine undergoes transes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tropane
Tropane is a nitrogenous bicyclic organic compound. It is mainly known for the other alkaloids derived from it, which include atropine and cocaine, among others. Tropane alkaloids occur in plants of the families Erythroxylaceae (including coca) and Solanaceae (including mandrake, henbane, deadly nightshade, datura, potato, tomato). Structurally, tropane is cycloheptane with a nitrogen bridge between carbons 1 and 5 and an additional methyl group attached to the nitrogen. While carbons 1 and 5 are asymmetric carbons, tropane itself is optically inactive due to mirror symmetry. 8-Azabicyclo .2.1ctane (tropane without the ''N''-methyl group In organic chemistry, a methyl group is an alkyl derived from methane, containing one carbon atom bonded to three hydrogen atoms, having chemical formula (whereas normal methane has the formula ). In formulas, the group is often abbreviated a ...) is known as nortropane or nor-tropane. See also * Phenyltropane * Tropane alkaloid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analog (chemistry)
A structural analog, also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is screened for structural analogs of a lead compound. Chemical analogues of illegal drugs are developed and sold in order to circumvent la ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Reuptake
Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmitting a neural impulse. Reuptake is necessary for normal synaptic physiology because it allows for the recycling of neurotransmitters and regulates the level of neurotransmitter present in the synapse, thereby controlling how long a signal resulting from neurotransmitter release lasts. Because neurotransmitters are too large and hydrophilic to diffuse through the membrane, specific transport proteins are necessary for the reabsorption of neurotransmitters. Much research, both biochemical and structural, has been performed to obtain clues about the mechanism of reuptake. Protein structure The first primary sequence of a reuptake protein was published in 1990. The technique for protein sequence determination relied upon the purification, s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
