Lisuride maleate - CAS 19875-60-6
Catalog number: 19875-60-6
Category: Inhibitor
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Molecular Formula:
C25H31N3O5
Molecular Weight:
454.58
COA:
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Targets:
Dopamine Receptor
Description:
Lisuride maleate, an ergot derivative, is a nonselective dopamine receptor agonist with high affinity for D2, D3 and D4 receptors along with 5-HT1A. As an anti-Parkinson's agent with anticonvulsive effects, Lisuride maleate has been shown to decrease the release of prolactin and reduce inflammatory mediators such as IL6 and TNF-α.
Purity:
>99 %
Appearance:
White Solid
Synonyms:
3-[(6aR,9S)-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-yl]-1,1-diethylurea;(Z)-but-2-enedioic acid; Lisuride Maleate ; Cuvalit; Lysenyl; Lysenyl bimaleate; Lysenyl hydrogen maleate; Lisuride hydrogen maleate; Mesylate, Lisuride; Methylergol ;Carbamide Revanil
MSDS:
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Boiling Point:
836.3℃ at 760 mmHg
InChIKey:
CVQFAMQDTWVJSV-BAXNFHPCSA-N
InChI:
1S/C20H26N4O.C4H4O4/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;5-3(6)1-2-4(7)8/h6-8,10-11,14,18,21H,4-5,9,12H2,1-3H3,(H,22,25);1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,18+;/m0./s1
Canonical SMILES:
CCN(CC)C(=O)NC1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C.C(=CC(=O)O)C(=O)O
1.Evidence for the management of mastalgia.
Gumm R;Cunnick GH;Mokbel K Curr Med Res Opin. 2004 May;20(5):681-4.
Mastalgia is the commonest breast symptom presenting to general practitioners and breast surgeons alike. To make a full assessment of the cause, all patients require a full history, examination and, sometimes, investigations. Diary cards are often helpful. The commonest cause is cyclical mastalgia. Most women require reassurance only and the pain often settles spontaneously after a few months. For the remainder, simple lifestyle changes should be suggested initially, such as wearing a well-fitted sports bra, weight reduction, regular exercise and a reduction in caffeine intake. Unfortunately, there is a paucity of evidence for the usefulness of these measures. If pain is persistent or severe, a variety of pharmacological agents exist. The most effective with least side effects is a 3-6-month course of low-dose tamoxifen (10mg). Other proven agents include danazol and bromocriptine, but these have a higher side-effect profile and are rarely indicated nowadays. Newer treatments include lisuride maleate and topical non-steroidal anti-inflammatory preparations.
2.[Treatment of premenstrual tension syndrome (PMS) with lisuride maleate].
López-Rosales C;Aguilar-Guerrero JA;García-Moreno L Ginecol Obstet Mex. 1996 Dec;64:556-60.
The etiology of PMS has not yet been defined, although there are several theories among which it is reported that there is an increase in prolactine levels involved in it. The purpose of this study was to evaluate a dopamine receptor agonist (lisuride maleate), in the treatment of PMS. 35 patients between 19 and 35 years old were recruited in a prospective study design, with diagnosis of PMS and no other gynecological disorder ruled out clinical and ultrasonographic examination, women with no previous treatment and with no use of hormonal agents, these patients were treated for three months with lisuride maleate, 0.3 mg-day in a three dosage scheme per day, the following symptoms were evaluated: headaches, mastalgia, bloating, edema of lower extremities and myalgia in legs, as well as hormonal parameters before and after treatment with estrogens, progesterone, prolactine, luteinizing hormone (LH), follicle stimulating hormone (FSH) and testosterone, which were prescribed in the luteal phase (day 21). Results obtained were: reduction of all symptoms scores versus pretreatment: Headache from 85.7 to 20%, mastalgia from 91.4 to 25%, bloating from 74.2 to 40%, edema in lower extremities from 85.
3.Mastalgia: a review of management.
Olawaiye A;Withiam-Leitch M;Danakas G;Kahn K J Reprod Med. 2005 Dec;50(12):933-9.
Mastalgia affects up to two-thirds of women at some time during their reproductive lives. It is usually benign, but thefear of underlying breast cancer is why many women present for evaluation. Mastalgia can be associated with premenstrual syndrome, fibrocystic breast disease, psychologic disturbance and, rarely, breast cancer. Occasionally, extramammary conditions, like Tietzie syndrome, present as mastalgia. A thorough clinical evaluation is required to assess the cause. The majority of women can be reassured after a clinical evaluation. Approximately 15% require pain-relieving therapy. Mechanical breast support; a low-fat, high-carbohydrate diet; and topical nonsteroidal antiinflammatory agents are reasonable first-line treatments. Hormonal agents, such as bromocriptine, tamoxifen and danazol, have all demonstrated efficacy in the treatment of mastalgia. Side effects, however, limit their extensive use. Danazol is the only FDA-approved hormonal treatment and is best used in cyclic form to limit the adverse effects. Lisuride maleate is a new agent recently studied for the treatment of mastalgia. Initial data on this medication are encouraging. Sixty percent of cyclic mastalgia recurs after treatment.
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CAS 19875-60-6 Lisuride maleate

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