- 関
- lisuride
WordNet
- a salt or ester of maleic acid; used as a nontricyclic antidepressant drug for psychomotor activation
UpToDate Contents
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English Journal
- Quantitative Phosphoproteomics Unravels Biased Phosphorylation of Serotonin 5-HT2A Receptor at Ser280 by Hallucinogenic versus non-Hallucinogenic Agonists.
- Karaki S1, Becamel C, Murat S, Mannoury la Cour C, Millan MJ, Prezeau L, Bockaert J, Marin P, Vandermoere F.Author information 1Institute of Functional Genomics, Montpellier, France;AbstractThe serotonin 5-HT2A receptor is a primary target of psychedelic hallucinogens such as lysergic acid diethylamine, mescaline and psilocybin, which reproduce some of the core symptoms of schizophrenia. An incompletely resolved paradox is that only some 5-HT2A receptor agonists exhibit hallucinogenic activity, whereas structurally related agonists with comparable affinity and activity lack such a psychoactive activity. Using a strategy combining stable isotope labeling by amino acids in cell culture and enrichment of peptide samples in phosphorylated peptides by hydrophilic interaction liquid chromatography followed by immobilized metal affinity chromatography, we compared the phosphoproteome in HEK-293 cells transiently expressing the 5-HT2A receptor and exposed to either vehicle or the synthetic hallucinogen 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI) or the non-hallucinogenic 5-HT2A agonist lisuride. Among the 5,995 identified phosphorylated peptides, 16 sites were differentially phosphorylated upon exposure of cells to DOI vs. lisuride. These include a serine (Ser280) located in the third intracellular loop of the receptor, a region important for desensitization. Specific phosphorylation of Ser280 by hallucinogens compared with non-hallucinogenic agonists was further validated by quantitative mass spectrometry on purified receptor and by using a phosphosite specific antibody. Administration of DOI, but not lisuride, to mice also enhanced 5-HT2A receptor phosphorylation at Ser280 in prefrontal cortex. Moreover, hallucinogens induced less pronounced desensitization of receptor-operated signaling in HEK-293 cells and neurons than exposure to non-hallucinogenic agonists. Mutation of Ser280 into aspartate (to mimic phosphorylation) reduced receptor desensitization by non-hallucinogenic agonists, while its mutation to alanine increased the ability of hallucinogens to desensitize the receptor. This study reveals biased phosphorylation of 5-HT2A receptor by hallucinogenic vs. non-hallucinogenic agonists, which underlies their distinct capacity to desensitize the receptor.
- Molecular & cellular proteomics : MCP.Mol Cell Proteomics.2014 Mar 17. [Epub ahead of print]
- The serotonin 5-HT2A receptor is a primary target of psychedelic hallucinogens such as lysergic acid diethylamine, mescaline and psilocybin, which reproduce some of the core symptoms of schizophrenia. An incompletely resolved paradox is that only some 5-HT2A receptor agonists exhibit hallucinogenic
- PMID 24637012
- Feeding condition and the relative contribution of different dopamine receptor subtypes to the discriminative stimulus effects of cocaine in rats.
- Baladi MG1, Newman AH, France CP.Author information 1Department of Pharmacology, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, Mail Code 7764, San Antonio, TX, 78229, USA.AbstractRATIONALE: The contribution of dopamine receptor subtypes in mediating the discriminative stimulus effects of cocaine is not fully established. Many drug discrimination studies use food to maintain responding, necessitating food restriction, which can alter drug effects.
- Psychopharmacology.Psychopharmacology (Berl).2014 Feb;231(3):581-91. doi: 10.1007/s00213-013-3271-x. Epub 2013 Sep 13.
- RATIONALE: The contribution of dopamine receptor subtypes in mediating the discriminative stimulus effects of cocaine is not fully established. Many drug discrimination studies use food to maintain responding, necessitating food restriction, which can alter drug effects.OBJECTIVE: This study establi
- PMID 24030470
- Drug-related cardiac valve disease.
- [No authors listed]AbstractCardiac valve disease can involve one or more of the four heart valves. Chronic valve damage may remain asymptomatic for long periods but ultimately leads to haemodynamic overload of the heart. The most common causes of valve disease are rheumatic diseases, infections, chronic renal failure, malformations, and genetic diseases. Valve disease is often attributed to degeneration with no known cause.The frequency of drug-related valve disease has long been underestimated. Most implicated drugs have serotonergic properties, such as fenfluramine-derived amphetamines, including benfluorex. Rye ergot derivatives can also be implicated: these include dopamine agonists (bromocriptine, lisuride, pergolide and cabergoline), migraine treatments (methysergide, ergotamine and dihydroergotamine), and drugs used for cognitive and neurosensory deficits (nicergoline, dihydroergocryptine, etc.). "Ecstasy", an amphetamine, is sometimes also involved. The risk increases after a few months of exposure. Drug withdrawal is sometimes followed by an improvement. Patients exposed to a drug known to cause valve damage should be informed of the risk and receive long-term monitoring to detect these lesions before they become irreversible. The possible role of a drug should always be considered when cardiac valve disease is diagnosed, in order to facilitate active research and to avoid exposing other patients to this risk.
- Prescrire international.Prescrire Int.2013 Dec;22(144):292-5.
- Cardiac valve disease can involve one or more of the four heart valves. Chronic valve damage may remain asymptomatic for long periods but ultimately leads to haemodynamic overload of the heart. The most common causes of valve disease are rheumatic diseases, infections, chronic renal failure, malform
- PMID 24600729
Japanese Journal
- 脳血管障害後のうつ状態に対するlisuride maleateの効果
Related Links
- Lisuride is described as free base (see table on the right) and as hydrogen maleate salt. Lisuride is used to lower prolactin and, in low doses, to prevent migraine attacks. The use of lisuride as initial anti-Parkinsonian treatment has been ...
- Lisuride Maleate is a medicine available in a number of countries worldwide. A list of US medications equivalent to Lisuride Maleate is available on the Drugs. com website.
★リンクテーブル★
[★]
- 英
- lisuride、lisuride maleate
- 関
- マレイン酸リスリド
[★]
- 英
- lisuride maleate
- 関
- リスリド
[★]
マレイン酸、マレイン酸塩、マレイン酸エステル
- 関
- maleic acid