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1-Aminotetralins
1-Aminotetralin (1-AT), also known as 1-amino-1,2,3,4-tetrahydronaphthalene, is a chemical compound and one of the possible positional isomers of aminotetralin. It consists of a tetralin core with an amino substituent on one of the carbon atoms. Derivatives 1-Aminotetralin is the parent structure of a number of drugs, including the following: Tramazoline is another related compound. See also * 2-Aminotetralin * Aminoindane References External links 1-Aminotetralin - Isomer Design 1-Aminotetralins, {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lometraline
Lometraline (International Nonproprietary Name, INN; developmental code name CP-14,368) is a drug and an aminotetralin chemical derivative, derivative. A structural modification of tricyclic compound, tricyclic neuroleptics, lometraline was originally patented by Pfizer as an antipsychotic, tranquilizer, and Management of Parkinson's disease#Medication, antiparkinsonian agent. However, it was instead later studied as a potential antidepressant and/or anxiolytic agent, though clinical studies revealed no psychoactivity at the doses used and further investigation was suspended. Further experimental modifications of the chemical structure of lometraline resulted in the discovery of tametraline, a potency (pharmacology), potent reuptake inhibitor, inhibitor of the reuptake of dopamine and norepinephrine, which in turn led to the discovery of the antidepressant sertraline, a selective serotonin reuptake inhibitor (SSRI). References {{Reflist Dimethylamino compounds Chloroarenes Ps ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LP-44
LP-44 is a drug which acts as a potent and selective agonist at the 5HT7 serotonin receptor. While LP-44 is less selective than the related compound LP-12, it has been more widely used in research and has been used to show the complex role of 5-HT7 receptors in several aspects of brain function, including regulation of the sleep-wake cycle and roles in stress, learning and memory. See also * AS-19 * E-55888 E-55888 is a drug developed by Esteve, which acts as a potent and selective full agonist at the 5HT7 serotonin receptor, and is used for investigating the role of 5-HT7 receptors in the perception of pain. When administered by itself, E-55888 i ... * LP-211 References {{Piperazines 5-HT7 agonists 1-Aminotetralins Phenylpiperazines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tochergamine
Tochergamine, also known as 621 I.S. or as ''N'',''N''-diethyl-''N''′-(1,2,3,4-tetrahydronaphthyl)glycinamide, is an oxytocic drug related to ergometrine which does not appear to have been marketed. It was reported to be effective as an oxytocic agent in animal studies, with oxytocic activity equivalent to that of ergometrine. In addition, the drug was reported to be effective in clinical studies at doses of 2 to 6mg parenterally. However, subsequent research found that it was inactive on the intact human uterus at doses of up to 20mg, and further investigation of tochergamine was abandoned. Tochergamine has a simplified lysergamide-like chemical structure, with a 1-aminotetralin ring system, and is structurally related to lysergamides like ergometrine and LSD. However, it is not technically a partial ergoline or lysergamide, only partial ergoline-like, as its structural features differ in certain regards from those of ergolines and lysergamides. The oxytocic effects of lyse ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tametraline
Tametraline (CP-24,441) is the parent of a series of chemical compounds investigated at Pfizer that eventually led to the development of sertraline. Sertraline has been called "3,4-dichloro-tametraline". This is correct but it is an oversimplification in the sense that sertraline is the ''S'',''S''-isomer whereas tametraline is the 1''R'',4''S''-stereoisomer. 1''R''-Methylamino-4''S''-phenyl-tetralin is a potent inhibitor of norepinephrine uptake in rat brain synaptosomes, reverses reserpine induced hypothermia in mice, and blocks uptake of 3H-Norepinephrine into rat heart. Tametraline is a norepinephrine–dopamine reuptake inhibitor. Indatraline is an indanamine homolog of tetralin-based tametraline, although in the case of indatraline the product is pm-dichlorinated. See also * Cyproheptadine * Dasotraline * Desmethylsertraline * EXP-561 (1-amino-4-phenylbicyclo .2.2ctane) * JNJ-7925476 * Lometraline * Nefopam * Sertraline Sertraline, sold under the brand name ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SR 59230A
SR 59230A is a selective antagonist of the beta-3 adrenergic receptor, but was subsequently shown to also act at α1 adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA 3,4-Methylenedioxymethamphetamine (MDMA), commonly known as ecstasy (tablet form), and molly (crystal form), is an empathogen–entactogenic drug with stimulant and minor Psychedelic drug, psychedelic properties. In studies, it has been used ... in animal studies. References Beta blockers Phenol ethers Secondary alcohols 1-Aminotetralins {{Alcohol-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dasotraline
Dasotraline (INN; former developmental code name SEP-225,289) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) that was under development by Sunovion for the treatment of attention-deficit hyperactivity disorder (ADHD) and binge eating disorder (BED). Structurally, dasotraline is a stereoisomer of desmethylsertraline (DMS), which is an active metabolite of the marketed selective serotonin reuptake inhibitor (SSRI) antidepressant sertraline (Zoloft). Adverse Effects In phase I clinical trials for attention deficit hyperactivity disorder, test subjects reported the following side effects: * Loss of appetite * Dehydration * Dry mouth * Nausea * Insomnia * Anxiety * Panic attacks * Headaches History In 2017, the U.S. Food and Drug Administration accepted Sunovion's New Drug Application (NDA) for review for the treatment of ADHD; however, the NDA was ultimately rejected citing the need for additional studies to determine efficacy and tolerability. In July 2019, S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Desmethylsertraline
Desmethylsertraline (DMS), also known as norsertraline, is an active metabolite of the antidepressant drug sertraline. Like sertraline, desmethylsertraline acts as a monoamine reuptake inhibitor, and may be responsible for some of its parent's therapeutic benefits; however, the effects of DMS's main activity of increasing serotonin levels via binding to the serotonin transporter appears to be negligible as in vivo testing showed no measurable change in brain activity despite a nearly 20-fold increase in DMS blood levels compared to the EC50 (i.e. the amount required to achieve the desired effect in 50% of the population) of its parent drug sertraline. DMS is significantly less potent relative to sertraline as a serotonin reuptake inhibitor (''K''i = 76 nM vs. 3 nM, respectively), but conversely, is more balanced as a monoamine reuptake inhibitor (serotonin, 5-HT (''K''i) = 76 nM; norepinephrine, NE (''K''i) = 420 nM; dopamine, DA (''K''i) = 440 nM), which h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ethonam
Ethonam is an antifungal agent. Synthesis 2- Aminotetralin () is alkylated with ethylchloroacetate to afford the glycine derivative. Heating with formic acid then affords the amide (2). This compound is then reacted with ethyl formate to yield hydroxymethylene ester (3). Rxn with isothiocyanic acid gives the imidazole-2-thiol (5). Desulfurization Desulfurization or desulphurisation is a chemical process for the removal of sulfur from a material. The term usually refers to the removal of sulfur from a molecule or a material by hydrogenolysis: : Hydrogen is the ultimate sulfur acceptor. A ... by means Raney-Nickel finishes the synthesis of ethnonam (6). References Antifungals Ethyl esters Imidazoles 1-Aminotetralins {{antiinfective-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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, social anxiety disorder, obsessive–compulsive disorder (OCD), panic disorder, and premenstrual dysphoric disorder. Although also having approval for post-traumatic stress disorder (PTSD), findings indicate it leads to only modest improvements in symptoms associated with this condition. The drug shares the common Side effect, side effects and contraindications of other SSRIs, with high rates of nausea, diarrhea, headache, insomnia, mild somnolence, sedation, dry mouth, and sexual dysfunction, but it appears not to lead to much weight gain, and its effects on cognition, cognitive performance are mild. Similar to other antidepressants, the use of sertraline for depression may be associated with a mildly elevated rate of suicidal thoughts in peo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LP-12
LP-12 is a drug which acts as a potent agonist at the 5HT7 serotonin receptor, with very high selectivity over other tested receptor subtypes such as the serotonin 5-HT1A and 5-HT2A, and the dopamine D2 receptor. It has been used to research the involvement of the 5-HT7 receptor in as yet poorly understood processes such as allodynia and hyperalgesia Hyperalgesia ( or ; ''hyper'' from Greek ὑπέρ (''huper'') 'over' + ''-algesia'' from Greek ἄλγος (algos) 'pain') is an abnormally increased sensitivity to pain, which may be caused by damage to nociceptors or peripheral nerves and .... See also * AS-19 * E-55888 * LP-44 * LP-211 References {{Piperazines 5-HT7 agonists 1-Aminotetralins Phenylpiperazines Carboxamides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2-Aminotetralin
2-Aminotetralin (2-AT), also known as 1,2,3,4-tetrahydronaphthalen-2-amine (THN), is a stimulant drug with a chemical structure consisting of a tetralin core with an amine as substituent. 2-AT is a rigid analogue of phenylisobutylamine and fully substitutes for d-amphetamine in rat drug discrimination tests, although at one-half to one-eighth the potency. It showed greater potency than a variety of other amphetamine homologues, including 2-amino-1,2-dihydronapthalene (2-ADN), 2-aminoindane (2-AI), 1-naphthylaminopropane (1-NAP), 2-naphthylaminopropane (2-NAP), 1-phenylpiperazine (1-PP), , and . 2-AT has been shown to inhibit the reuptake of serotonin and norepinephrine, and might induce their release as well. It is also likely to act on dopamine on account of its full substitution of d-amphetamine in rodent studies. Chemical derivatives A number of derivatives of 2-aminotetralin exist, including: See also * 1-Aminotetralin 1-Aminotetralin (1-AT), also known as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tramazoline
Tramazoline is a chemical that is used in the form of tramazoline hydrochloride in nasal decongestant preparations. It is an α-adrenergic receptor agonist that inhibits secretion of nasal mucus. It was patented in 1961 and came into medical use in 1962. Society and culture Brand names *Australia ** Spray-Tish ** Rhinaspray *Austria ** Rhinorix *Belgium ** Rhinospray *Bulgaria ** Muconasal Plus *Czech Republic ** Muconasal Plus *Germany ** Biciron ** Ellatun ** Rhinospray *Hungary ** Rhinospray Plus *Italy ** Rinogutt ** Fexallegra nasale (Tramazoline + Chlorpheniramine, 1 mg/mL + 3.55 mg/mL) *The Netherlands **Bisolnasal *Portugal ** Rhinospray *Romania ** Muconasal Plus (older) ** Muconasal (newer) *Russia ** Adrianol (tramazoline + phenylephrine Phenylephrine, sold under the brand names Neosynephrine and Sudafed PE among others, is a medication used as a decongestant for uncomplicated nasal congestion in the form of a nasal spray or oral tablet, to dilat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
