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SN-22
SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of which are ligands for 5-HT1A, 5-HT6 or dopamine D2 receptors or show SSRI activity. See also * BRL-54443 * LY-334370 * LY-367,265 * MPMI * MPTP * Naratriptan * N,N-Dimethyltryptamine * RU-24969 * Sertindole Sertindole, sold under the brand name Serdolect among others, is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, ... References Piperidinylindoles Serotonin receptor agonists {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BRL-54443
BRL-54443 is a drug which acts as a selective agonist for the 5-HT1E and 5-HT1F serotonin receptor subtypes. See also * CP-94253 * RS134-49 * RU-24969 * Sertindole * SN-22 SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of ... * VU6067416 References 5-HT1E agonists 5-HT1F agonists Hydroxyarenes Piperidinylindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-334370
LY-334370 is a selective 5-HT1F receptor agonist which was under development by Eli Lilly and Company for the treatment of migraine headaches. The drug showed efficacy in a phase II clinical trial but further development was halted due to toxicity detected in animals. See also * CP-135807 * Lasmiditan Lasmiditan, sold under the brand name Reyvow, is a medication used for the acute (active but short-term) treatment of migraine with or without aura (a sensory phenomenon or visual disturbance) in adults. It is not useful for prevention. It is ... * SN-22 References External links * 5-HT1F agonists Abandoned drugs Benzamides Drugs developed by Eli Lilly and Company 4-Fluorophenyl compounds Piperidinylindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RU-24969
RU-24,969 is a serotonin receptor modulator related to 5-MeO-DMT which is used in scientific research. It is a selective agonist of the serotonin 5-HT1A and 5-HT1B receptors, with 5-fold preference for the latter receptor over the former. In studies, its affinities (Ki) were 2nM for the serotonin 5-HT1 receptor, 5nM for the serotonin 5-HT1A receptor, 4nM for the serotonin 5-HT1B receptor, 780 to 1,000nM for the serotonin 5-HT2 receptor, and 400nM for the serotonin 5-HT2C receptor. It also has affinity for the serotonin 5-HT5A, 5-HT5B, and 5-HT7 receptors. The drug produces MDMA-like locomotor hyperactivity in animals and this is thought to be mediated by activation of both serotonin 5-HT1A and 5-HT1B receptors. As with other serotonin 5-HT1B receptor agonists such as CP-94,253, RU-24,969 has also been found to increase the reinforcing properties of cocaine in animals, suggesting a role for serotonin 5-HT1B receptors in cocaine addiction as well. RU-24,969 was first d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MPMI (drug)
3-(N-methylpyrrolidin-3-ylmethyl)indole (MPMI) is a tryptamine derivative which acts as a serotonin receptor agonist. It has been studied as an analogue and trace impurity of the anti-migraine drug eletriptan but is otherwise little known. See also * α,N,N-Trimethyltryptamine * Dimethyltryptamine * 4-HO-MPMI * 5F-MPMI * 5-MeO-MPMI * NTBT * 10,11-Secoergoline (α,''N''-Pip-T) * Pyr-T * SN-22 SN-22 is a chemical compound which acts as a moderately selective agonist at the 5-HT2 family of serotonin receptors, with a Ki of 19 nM at 5-HT2 subtypes versus 514 nM at 5-HT1A receptors. Many related derivatives are known, most of ... References Alpha-Alkyltryptamines Designer drugs N,N-Dialkyltryptamines Psychedelic tryptamines Pyrrolidinylmethylindoles Serotonin receptor agonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sertindole
Sertindole, sold under the brand name Serdolect among others, is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. It is classified chemically as a phenylindole derivative. Sertindole is not approved for use in the United States and was discontinued in Australia in January 2014. Medical Uses Sertindole appears effective as an antipsychotic in schizophrenia. In a 2013 study in a comparison of 15 antipsychotic drugs in effectivity in treating schizophrenic symptoms, sertindole was found to be slightly less effective than haloperidol, quetiapine, and aripiprazole, as effective as ziprasidone, approximately as effective as chlorpromazine and asenapine, and slightly more effective than lurasidone and iloperidone. Adverse effects Very co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N,N-Dimethyltryptamine
Dimethyltryptamine (DMT), also known as ''N'',''N''-dimethyltryptamine (''N'',''N''-DMT), is a serotonergic hallucinogen and investigational drug of the tryptamine family that occurs naturally in many plants and animals, including humans. DMT is used as a psychedelic drug and prepared by various cultures for ritual purposes as an entheogen. DMT has a rapid onset, intense effects, and a relatively short duration of action. For those reasons, DMT was known as the "businessman's trip" during the 1960s in the United States, as a user could access the full depth of a psychedelic experience in considerably less time than with other substances such as LSD or psilocybin mushrooms. DMT can be inhaled or injected and its effects depend on the dose, as well as the mode of administration. When inhaled or injected, the effects last about five to fifteen minutes. Effects can last three hours or more when orally ingested along with a monoamine oxidase inhibitor (MAOI), such as the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naratriptan
Naratriptan (trade names include Amerge) is a triptan drug marketed by GlaxoSmithKline and is used for the treatment of migraine headaches. It is a selective 5-HT1 receptor subtype agonist. It was patented in 1987 and approved for medical use in 1997. Medical uses Naratriptan is used for the treatment of the acute migraine attacks and the symptoms of migraine, including severe, throbbing headaches that sometimes are accompanied by nausea and sensitivity to sound or light. Efficacy A meta-analysis of 53 clinical trials has shown that all triptans are effective for treating migraine at marketed doses and that naratriptan, although less effective than sumatriptan and rizatriptan was more effective than placebo in reducing migraine symptoms at two hours and efficacy was demonstrated in almost two thirds of subjects after four hours of treatment. Side effects Side effects are similar to other triptan medications, with the incidence of side effects reportedly being lower than suma ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MPTP
MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is an organic compound. It is classified as a tetrahydropyridine. It is of interest as a precursor to the monoaminergic neurotoxin MPP+, which causes permanent symptoms of Parkinson's disease by destroying dopaminergic neurons in the substantia nigra of the brain. It has been used to study disease models in various animals. While MPTP itself has no psychoactive effects, the compound may be accidentally produced during the manufacture of MPPP, a synthetic opioid drug with effects similar to those of morphine and pethidine (meperidine). The Parkinson-inducing effects of MPTP were first discovered following accidental injection as a result of contaminated MPPP. Toxicity Injection of MPTP causes rapid onset of Parkinsonism, hence users of MPPP contaminated with MPTP will develop these symptoms. MPTP itself is not toxic, but it is a lipophilic compound and can therefore cross the blood–brain barrier. Once inside the brai ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LY-367,265
LY-367,265 is a drug of the tetrahydropyridinylindole group developed by Eli Lilly, which acts as both a potent and selective antagonist at the serotonin 5-HT2A receptor, and also a selective serotonin reuptake inhibitor (SSRI). It has antidepressant effects in animal studies, reduces glutamate signalling in the brain and increases the analgesic effects of morphine Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are .... See also * Tetrahydropyridinylindole References 5-HT2A antagonists Drugs developed by Eli Lilly and Company Selective serotonin reuptake inhibitors Tetrahydropyridinylindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Functional Selectivity
Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the μ-opioid receptor show equivalent ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SSRI
Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions. SSRIs primarily work by blocking serotonin reabsorption (reuptake) via the serotonin transporter, leading to gradual changes in brain signaling and receptor regulation, with some also interacting with sigma-1 receptors, particularly fluvoxamine, which may contribute to cognitive effects. Marketed SSRIs include six main antidepressants— citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline—while dapoxetine is indicted for premature ejaculation. Fluoxetine has been approved for veterinary use in treatment of canine separation anxiety. SSRIs are the most widely prescribed antidepressants in many countries. Their effectiveness, especially for mild to moderate depression, remains debated due to mixed research findings and concer ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
