Lisuride: An ergot derivative that acts as an agonist at dopamine D2 receptors (DOPAMINE AGONISTS). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (SEROTONIN RECEPTOR AGONISTS).Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.Lysergic Acid Diethylamide: Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood.Bulbar Palsy, Progressive: A motor neuron disease marked by progressive weakness of the muscles innervated by cranial nerves of the lower brain stem. Clinical manifestations include dysarthria, dysphagia, facial weakness, tongue weakness, and fasciculations of the tongue and facial muscles. The adult form of the disease is marked initially by bulbar weakness which progresses to involve motor neurons throughout the neuroaxis. Eventually this condition may become indistinguishable from AMYOTROPHIC LATERAL SCLEROSIS. Fazio-Londe syndrome is an inherited form of this illness which occurs in children and young adults. (Adams et al., Principles of Neurology, 6th ed, p1091; Brain 1992 Dec;115(Pt 6):1889-1900)Home Infusion Therapy: Use of any infusion therapy on an ambulatory, outpatient, or other non-institutionalized basis.Akinetic Mutism: A syndrome characterized by a silent and inert state without voluntary motor activity despite preserved sensorimotor pathways and vigilance. Bilateral FRONTAL LOBE dysfunction involving the anterior cingulate gyrus and related brain injuries are associated with this condition. This may result in impaired abilities to communicate and initiate motor activities. (From Adams et al., Principles of Neurology, 6th ed, p348; Fortschr Neurol Psychiatr 1995 Feb;63(2):59-67)Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.Serotonin 5-HT2 Receptor Agonists: Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Antiparkinson Agents: Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists.Hallucinogens: Drugs capable of inducing illusions, hallucinations, delusions, paranoid ideations, and other alterations of mood and thinking. Despite the name, the feature that distinguishes these agents from other classes of drugs is their capacity to induce states of altered perception, thought, and feeling that are not experienced otherwise.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.

*  Lisuride - Wikipedia
Lisuride is described as free base (see table on the right) and as hydrogen maleate salt. Lisuride is used to lower prolactin ... The use of lisuride as initial anti-Parkinsonian treatment has been advocated, delaying the need for levodopa until lisuride ... Bromination of Lisuride gives bromerguride. Lisuride is a dopamine and a partial agonist for several serotonin receptors. It is ... Lisuride is not currently available in the US, as the drug was not a commercial success in comparison with other dopamine ...
  https://en.wikipedia.org/wiki/Lisuride
*  Patent US4406658 - Iontophoretic device with reversible polarity - Google Patents
Electrotransport Of Lisuride. US20090216175 *. Aug 4, 2006. Aug 27, 2009. Transcu Ltd.. Transdermal Administration Device and ...
  http://www.google.com/patents/US4406658?dq=7,194,691
*  HTR2A - 5-hydroxytryptamine receptor 2A - Homo sapiens (Human) - HTR2A gene & protein
DB00589. Lisuride. DB00408. Loxapine. DB06077. Lumateperone. DB08815. Lurasidone. DB05743. MAP-0004. DB00934. Maprotiline. ... DB00589. Lisuride. DB00408. Loxapine. DB06077. Lumateperone. DB08815. Lurasidone. DB05743. MAP-0004. DB00934. Maprotiline. ...
  http://www.uniprot.org/uniprot/P28223
*  KEGG PATHWAY: hsa04728
Dopamine (DA) is an important and prototypical slow neurotransmitter in the mammalian brain, where it controls a variety of functions including locomotor activity, motivation and reward, learning and memory, and endocrine regulation. Once released from presynaptic axonal terminals, DA interacts with at least five receptor subtypes in the central nervous system (CNS), which have been divided into two groups: the D1-like receptors (D1Rs), comprising D1 and D5 receptors, both positively coupled to adenylyl cyclase and cAMP production, and the D2-like receptors (D2Rs), comprising D2, D3, and D4 receptors, whose activation results in inhibition of adenylyl cyclase and suppression of cAMP production. In addition, D1Rs and D2Rs modulate intracellular Ca2+ levels and a number of Ca2+ -dependent intracellular signaling processes. Through diverse cAMP- and Ca2+-dependent and - independent mechanisms, DA influences neuronal activity, synaptic plasticity, and behavior. Presynaptically localized D2Rs ...
  http://www.genome.jp/dbget-bin/www_bget?hsa04728
*  Pivhydrazine - DrugBank
Lisuride. The metabolism of Lisuride can be decreased when combined with Pivhydrazine.. Approved, Investigational. ...
  https://www.drugbank.ca/drugs/DB09252
*  Levosalbutamol - DrugBank
Lisuride. The risk or severity of adverse effects can be increased when Lisuride is combined with Levosalbutamol.. Approved, ...
  https://www.drugbank.ca/drugs/DB13139
*  Alpha-2B adrenergic receptor - DrugBank
Lisuride. approved, investigational. unknown. other/unknown. Details. DB00248. Cabergoline. approved. unknown. antagonist. ...
  https://www.drugbank.ca/biodb/polypeptides/P18089
*  Toloxatone - DrugBank
Lisuride. The metabolism of Lisuride can be decreased when combined with Toloxatone.. Approved. ...
  https://www.drugbank.ca/drugs/DB09245
*  5-hydroxytryptamine receptor 7 - DrugBank
Lisuride. approved, investigational. unknown. Details. DB01267. Paliperidone. approved. unknown. Details. DB00734. Risperidone ...
  https://www.drugbank.ca/biodb/bio_entities/BE0000650
*  WHOCC - ATC/DDD Index
lisuride N02CA51 dihydroergotamine, combinations N02CA52 ergotamine, combinations excl. psycholeptics 4 mg O Refers to ...
  https://www.whocc.no/atc_ddd_index/?code=N02CA&showdescription=yes
*  Brevet US7045118 - Delivery of compounds for the treatment of migraine through an inhalation route - Google Brevets
Salt forms of migraine headache drugs (e.g., lidocaine, verapamil, diltiazem, isometheptene, and lisuride) are either ... and lisuride.. It is desirable to provide a new route of administration for migraine headache drugs that rapidly produces peak ... or lisuride); as a mixture of active compound and a pharmaceutically acceptable excipient; as a salt form of the pure active ...
  http://www.google.fr/patents/US7045118
*  Platelet-derived serotonin links vascular disease and tissue fibrosis | JEM
Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug ... including cyproheptadine and terguride used in our study as well as mianserin and lisuride, are already in clinical use and are ...
  http://jem.rupress.org/content/early/2011/04/21/jem.20101629
*  Effects of a new long-acting form of bromocriptine on tumorous hyperprolactinemia | Springer for Research & Development
In: Calne D.B. (Eds.), Lisuride and other dopamine agonists. Raven Press, New York, 1983, p. 239.Google Scholar ... In: Calne D.B. (Eds.), Lisuride and other dopamine agonists. Raven Press, New York, 1983, p. 231.Google Scholar ...
  https://rd.springer.com/article/10.1007/BF03347187
*  Patent US7473710 - Bronchodilating beta-agonist compositions and methods - Google Patents
Lisuride (N′-((8a)-9,10-didehydro-6-methylergolin-8-yl)-N,N-diethylurea); Pergolide ((8a)-8-((methylthio)methyl)-6- ...
  http://www.google.com/patents/US7473710?dq=7,013,345/
*  Brevet US6372255 - Tablet for instant and prolonged release of one or more active substances - Google Brevets
antiparkinsonians such as levodopa, selegiline, lisuride, bromocriptine, biperiden, orphenadrine, procyclidine, tropatepin, ...
  http://www.google.fr/patents/US6372255
*  Periodic limb movement disorder - Wikipedia
Other dopaminergic agents such as co-careldopa, co-beneldopa, pergolide, or lisuride may also be used. These drugs decrease or ...
  https://en.wikipedia.org/wiki/Periodic_limb_movement_disorder
*  Prevalence of orthostatic hypotension in Parkinson's disease | Journal of Neurology, Neurosurgery & Psychiatry
Forty three patients were also treated with bromocriptine and five received lisuride. Some patients were taking other ... lisuride, and 25.7% deprenyl. The number of patients receiving antihypertensive drugs or of patients being treated with ... difference between patients with or without orthostatic hypotension for other antiparkinsonian drugs such as lisuride (5.7% v ...
  http://jnnp.bmj.com/content/63/5/584
*  List of dopaminergic drugs - Wikipedia
Lisuride • Lysergic acid diethylamide (LSD) • Pergolide Dihydrexidine derivatives: 2-OH-NPA • A-86,929 • Ciladopa • ...
  https://en.wikipedia.org/wiki/List_of_dopaminergic_drugs
*  Liaquat University of Medical & Health Sciences (LUMHS)
Outcome of Treatment with Lisuride in Hyperprolactinemic Infertile Women Bekha Ram Devrajani, Nizamuddin Memon, Khairunisa ...
  http://www.lumhs.edu.pk/research/published-papers.php
*  Atti Accademia Pontaniana Vol
The dopamine receptor agonist lisuride attenuates iron-mediated dopaminergic neurodegeneration.. Exp Neurol. 2003 ,184, 530-535 ...
  http://www.tightrope.it/nicolaus/link%2024.htm
*  Metergoline - Serotonin Antagonist & Dopamine Agonist For R&D | Page 14 | Ray Peat Forum
When taking metergoline and lisuride simultaneaously isn't the 5-HT1A antagonism of metergoline cancelled out by the lisuride ... When taking metergoline and lisuride simultaneaously isn't the 5-HT1A antagonism of metergoline cancelled out by the lisuride ... Is Metergoline Or Lisuride Legal To Bring Into Japan?. Dezz, Aug 8, 2017, in forum: Pharmaceutical Drugs ... Selling Metergoline, Lisuride, And A Scale. Elchapchapchapo, Apr 25, 2017, in forum: Merchant Forums ...
  https://raypeatforum.com/community/threads/metergoline-serotonin-antagonist-dopamine-agonist-for-r-d.12908/page-14
*  Metergoline - Serotonin Antagonist & Dopamine Agonist For R&D | Page 3 | Ray Peat Forum
Is Metergoline Or Lisuride Legal To Bring Into Japan?. Dezz, Aug 8, 2017, in forum: Pharmaceutical Drugs ... Selling Metergoline, Lisuride, And A Scale. Elchapchapchapo, Apr 25, 2017, in forum: Merchant Forums ... Is this thought to be more or less dopaminergic and more or less anti-prolactin than lisuride? If one has a stockpile of ... Is this thought to be more or less dopaminergic and more or less anti-prolactin than lisuride? If one has a stockpile of ...
  https://raypeatforum.com/community/threads/metergoline-serotonin-antagonist-dopamine-agonist-for-r-d.12908/page-3

(1/45) Antagonism of a PCP drug discrimination by hallucinogens and related drugs.

Drugs such as PCP and MK-801 can cause psychotic reactions in humans by antagonizing NMDA receptors. This action is ultimately toxic to certain cortical neurons and may be one mechanism underlying neurodegenerative diseases, including schizophrenia. It has been reported that hallucinogens such as LSD, DOM, and DOI can block the neurotoxic effects of NMDA antagonists, possibly by activating inhibitory 5-HT2A receptors on GABAergic interneurons that normally inhibit glutamatergic projections to the retrosplenial and cingulate cortexes. The purpose of this experiment was to determine the extent to which similar drugs might also alter the behavioral effects of one NMDA antagonist, PCP. Rats were trained to discriminate this compound (2.5 mg/kg) from saline and were then given a series of antagonist tests. It was found that LSD (0.32 mg/kg) and DOM (4.0 mg/kg) blocked the PCP cue completely; DMT (8.0 mg/kg) and a structural congener of LSD, lisuride (LHM; 0.4 mg/kg), blocked the effects of PCP partially. The 5-HT/DA antagonists spiperone and ritanserin had no effect on the PCP cue. These data suggest that LSD, DOM, and, less effectively, DMT and LHM can block the behavioral as well as the neurotoxic effects of NMDA antagonists most likely through agonist actions at 5-HT2 receptors.  (+info)

(2/45) Terguride attenuates prolactin levels and ameliorates insulin sensitivity and insulin binding in obese spontaneously hypertensive rats.

Glucose tolerance, serum insulin, insulin receptors in epididymal fat tissue, circulating total cholesterol and triglyceride concentrations as well as serum prolactin were studied in obese and lean spontaneously hypertensive rats (SHR) of both sexes. Obese animals displayed insulin resistance and elevated insulin and triglyceride concentrations. Moreover, in obese rats the increased mass of epididymal fat tissue was accompanied with decreased capacity of high affinity binding sites of insulin receptors in the tissue plasma membranes. Terguride treatment lowered prolactin serum levels which was accompanied by ameliorated insulin sensitivity in obese animals of both sexes. In addition, terguride treatment decreased serum insulin and triglyceride concentrations in obese females and at the same time enhanced the affinity of high affinity insulin binding sites. Our results show that obesity in SHR is associated with a decreased capacity of insulin receptors and that prolactin may play a role in obesity-induced insulin resistance, particularly in female rats.  (+info)

(3/45) Real-time analysis of dopamine: antagonist interactions at recombinant human D2long receptor upon modulation of its activation state.

1. Antipsychotic drugs may mediate their therapeutic effects not only by preventing the binding of dopamine but also by decreasing the propensity of the dopamine receptor to assume an active R* state. Ligand-mediated activation and blockade of the recombinant human D(2long) receptor was investigated in CHO-K1 cells upon modulation of its R* state. 2. Both the Ala(371)Lys (A371K) and Thr(372)Arg (T372R) D2long receptor mutants could be activated in a ligand-dependent manner via a chimeric G(alphaq/o) protein, and more efficaciously so than with the promiscuous G(alpha15) protein. 3. Dopamine and partial agonists (E(max): lisuride >> (+)-UH 232 approximately bromerguride) displayed dissimilar Ca(2+) kinetic properties at wild-type and mutant receptors. A371K and T372R D2long receptor mutants demonstrated an attenuated and enhanced maximal response to these partial agonists, respectively. 4. Dopamine antagonists were unable to block the transient high-magnitude Ca(2+) phase at the wild-type D2long receptor upon simultaneous exposure to antagonist and dopamine, while full blockade of the low-magnitude Ca(2+) phase did occur at a later time (onset-time: haloperidol < bromerguride < (+)-butaclamol). A similar, though more efficacious, antagonist profile was also found at the A371K mutant receptor. Conversely, the blockade of the low-magnitude Ca(2+) phase was attenuated (haloperidol) or almost absent [(+)-butaclamol and bromerguride] at the T372R mutant receptor. 5. In conclusion, mutagenesis of the Ala(371) and Thr(372) positions affects in an opposite way the ligand-dependent activation and blockade of the D2long receptor. The observed attenuation of dopamine-mediated Ca(2+) signal generation with different decay-times may underlie distinct properties of the dopaminergic ligands.  (+info)

(4/45) Dopaminergic modulation of grooming behavior in virgin and pregnant rats.

Dopamine receptors are involved in the expression of grooming behavior. The pregnancy-induced increase in self-licking observed in rats is important for mammary gland development and lactation. This study focuses on the role of dopamine receptor subtypes in grooming behavior of virgin and pregnant female rats. General and mammary gland grooming were measured in virgin rats treated with 0.25 mg/kg of the D1-like agonist SKF-81297 and antagonist SKF-83566 and the D2-like agonist lisuride and antagonist sulpiride. The effects of 0.01 and 0.25 mg/kg doses of the same agonists and antagonists were evaluated in pregnant rats as well. In virgin animals both SKF-83566 and sulpiride treatments significantly reduced the time spent in general grooming, while none of the dopamine agonists was able to significantly change any parameter of general grooming. Time spent in grooming directed at the mammary glands was not affected significantly by any of the drug treatments in virgin rats. All drugs tested significantly decreased the frequency of and the time spent with general grooming, while SKF-81297 treatment alone did not significantly reduce the duration of mammary gland grooming in pregnant rats. These data show that in female rats the behavioral effects of D1-like and D2-like dopamine receptor stimulation and blockade differ according to physiological state. The results suggest that dopamine receptors may play specific roles modulating grooming behavior in pregnant rats. Since grooming of the mammary gland during pregnancy may influence lactation, this aspect is relevant for studies regarding the perinatal use of dopamine-related drugs.  (+info)

(5/45) Dopamine partial agonist reverses amphetamine withdrawal in rats.

Decreased motivation to work for a natural reward is a sign of amphetamine withdrawal and is thought to be associated with hypofunction of the mesolimbic dopamine system. During withdrawal from repeated amphetamine administration, rats showed reduced responding for a sweet solution in a progressive ratio schedule. Repeated systemic treatment with terguride (0.2 and 0.4 mg/kg, i.p.) twice daily during the first four days of amphetamine withdrawal reversed the decrease in responding for the sweet solution. These results suggest that dopamine partial agonists, possibly due to their agonistic-like actions under these conditions, are a potential therapeutic approach for the acute withdrawal stage of the amphetamine addition cycle.  (+info)

(6/45) Prospective randomized trial of lisuride infusion versus oral levodopa in patients with Parkinson's disease.

Motor complications are a major source of disability for patients with advanced Parkinson's disease. Surgical therapies provide benefit to some, but these treatments are expensive and associated with adverse effects. Current research indicates that motor complications are associated with abnormal, intermittent, pulsatile stimulation of denervated dopamine receptors using short acting dopaminergic agents such as levodopa. Retrospective studies suggest that the use of longer-acting more continuous dopaminergic therapies can improve both motor fluctuations and dyskinesia. We performed a prospective, long-term (4-year) trial comparing patients randomized to receive subcutaneous infusion of the dopamine agonist lisuride versus conventional therapy with oral levodopa and dopamine agonists. We demonstrate that patients receiving lisuride infusions experienced a significant reduction in both motor fluctuations and dyskinesia compared with patients receiving standard dopaminergic therapies. Benefits persisted for the 4-year duration of the study. Mean Unified Parkinson's Disease Rating Scale scores in "ON" and "OFF" states did not significantly change between baseline and 4 years for patients in the lisuride group, but deteriorated in patients in the levodopa group. This study indicates that continuous lisuride infusion can be beneficial for patients with advanced Parkinson's disease and reverse established motor fluctuations and dyskinesia.  (+info)

(7/45) In-vivo SPECT imaging of D2 receptor with iodine-iodolisuride: results in supranuclear palsy.

We assessed the potential use of [123I]iodolisuride (ILIS), a new iodine ergolene derivative, to study human striatal D2 dopamine receptors with SPECT. In normal subjects, we found that the tracer accumulated preferentially in striatum. This was prevented by high doses of haloperidol. The striatal accumulation was maximal between 60 and 180 min after injection. The striatum-to-cerebellum radioactivity concentration ratio as an index of specific binding, measured 60 min after injection, was 1.52 +/- 0.19 (mean +/- s.d.) in controls and 1.36 +/- 0.11 in patients with supranuclear palsy (p less than 0.03). Our results show that ILIS may be used to study D2 receptors with SPECT. In-vivo changes of D2 receptors in human brain may be detected with this method.  (+info)

(8/45) 8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist.

The human histamine H1 receptor (H1R) is an important, well characterized target for the development of antagonists to treat allergic conditions. Many neuropsychiatric drugs are known to potently antagonize the H1R, thereby producing some of their side effects. In contrast, the tolerability and potential therapeutic utility of H1R agonism is currently unclear. We have used a cell-based functional assay to evaluate known therapeutics and reference drugs for H1R agonist activity. Our initial functional screen identified three ergot-based compounds possessing heretofore-unknown H1R agonist activity. 8R-lisuride demonstrated potent agonist activity in various assays including receptor selection and amplification technology, inositol phosphate accumulation, and activation of nuclear factor-kappaB with pEC50 values of 8.1, 7.9, and 7.9, respectively, and with varying degrees of efficacy. Based on these assays, 8R-lisuride is the most potent stereospecific partial agonist for the human H1R yet reported. Investigation of the residues involved in histamine and lisuride binding, using H1R mutants and molecular modeling, have revealed that although these ligands are structurally different, the lisuride-binding pocket in the H1R closely corresponds to the histamine-binding pocket. The discovery of a potent stereospecific partial H1R agonist provides a valuable tool to further characterize this important therapeutic target in vitro.  (+info)