Lisuride - CAS 18016-80-3
Catalog number: 18016-80-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H26N4O
Molecular Weight:
338.45
COA:
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Targets:
5-HT Receptor | Dopamine Receptor
Description:
Lisuride, an indoloquinoline derivative, has been found to be a dopamine D2 receptor agonist and could probably be effective in antimigraine as well as antiparkinsonian studies.
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Purity:
98%
Appearance:
Powder
Synonyms:
LISURIDE;S-(-)-LISURIDE;CABERQOLINE;3-[(8α)-9,10-Didehydro-6-methylergolin-8-yl]-1,1-diethylurea;Lysuride;Methylergol carbamide;N'-[(5β)-9,10-Didehydro-6-methylergoline-8α-yl]-N,N-diethylurea;Lisuride (S)(-)
Storage:
Store in a cool and dry place and at 0 - 4 °C for short term (days to weeks) or -20 °C for long term (months to years).
MSDS:
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Quality Standard:
In-house standard
Quantity:
Milligram-Grams
InChIKey:
BKRGVLQUQGGVSM-KBXCAEBGSA-N
InChI:
InChI=1S/C20H26N4O/c1-4-24(5-2)20(25)22-14-10-16-15-7-6-8-17-19(15)13(11-21-17)9-18(16)23(3)12-14/h6-8,10-11,14,18,21H,4-5,9,12H2,1-3H3,(H,22,25)/t14-,18+/m0/s1
Canonical SMILES:
CCN(CC)C(=O)NC1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C
Current Developer:
axxonis Pharma
1.Relationships between serotoninergic system and skin fibrotic.
Huang J, Gong Q, Huang C, Li G1. Antiinflamm Antiallergy Agents Med Chem. 2014 Mar;13(1):9-16.
Cutaneous fibrosis seen in systemic sclerosis (SSc) is a generalized connective tissue disorder, characterized by a wide spectrum of microvascular and immunological abnormalities. Serotonin (5-hydroxytryptamine; 5-HT) is a neurotransmitter and immune modulator, is also an important mediator of bidirectional interactions between the vasoactive amines and the skin.5-HT, a commonly secreted amine, is a known inducer of fibrosis, although the mechanistic basis for it and growth factors regulating fibrosis and proliferation in the microenvironment are unclear. We review that as serotonin has powerful vasodilator, immunomodulator, and growth factor actions, this pathway could be involved in skin fibrotic. Since serotoninergic system play a role in skin fibrotic, and 5-HTs drugs, an usual treatment for this type of patients. These provides a future perspective for research and drug development.
2.Drug-related cardiac valve disease.
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, 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.
3.Quantitative phosphoproteomics unravels biased phosphorylation of serotonin 2A receptor at Ser280 by hallucinogenic versus nonhallucinogenic agonists.
Karaki S1, Becamel C, Murat S, Mannoury la Cour C, Millan MJ, Prézeau L, Bockaert J, Marin P, Vandermoere F. Mol Cell Proteomics. 2014 May;13(5):1273-85. doi: 10.1074/mcp.M113.036558. Epub 2014 Mar 17.
The serotonin 5-HT(2A) 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-HT(2A) 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 with enrichment in phosphorylated peptides by means of hydrophilic interaction liquid chromatography followed by immobilized metal affinity chromatography, we compared the phosphoproteome in HEK-293 cells transiently expressing the 5-HT(2A) receptor and exposed to either vehicle or the synthetic hallucinogen 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI) or the nonhallucinogenic 5-HT(2A) agonist lisuride. Among the 5995 identified phosphorylated peptides, 16 sites were differentially phosphorylated upon exposure of cells to DOI versus lisuride.
4.[Post-partum: Guidelines for clinical practice--Short text].
Sénat MV1, Sentilhes L2, Battut A3, Benhamou D4, Bydlowski S5, Chantry A6, Deffieux X7, Diers F8, Doret M9, Ducroux-Schouwey C8, Fuchs F10, Gascoin G11, Lebot C12, Marcellin L13, Plu-Bureau G14, Raccah-Tebeka B15, Simon E16, Bréart G17, Marpeau L18. J Gynecol Obstet Biol Reprod (Paris). 2015 Dec;44(10):1157-66. doi: 10.1016/j.jgyn.2015.09.017. Epub 2015 Oct 31.
OBJECTIVE: To determine the post-partum management of women and their newborn whatever the mode of delivery.
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CAS 18016-80-3 Lisuride

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