Lisuride - Liquid Lisuride (maleate) For Lab/research Use

Discussion in 'IdeaLabs' started by haidut, Aug 5, 2016.

  1. haidut

    haidut Member

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    After many months of often fruitless searching and negotiations with chemical vendors from all over the world, I am pleased to finally announce the release of our Lisuride product. This is perhaps the most anticipated product we have ever released and it is for a good reason. The recent acquisition of terguride (a lisuride isomer) by Pfizer with the intent of treating heart, liver, lung, and other fibrosis demonstrates the commitment of Big Pharma to the correct idea that serotonin is a causative factor in the pathology of so many conditions. It is not a "happy hormone" at all, unless you consider a zombified, fibrotic state to be a form of bliss. Lisuride is the most potent dopamine agonist currently in clinical or research use, across all known dopamine receptors (D1, D2, D3, D4, and D5). In addition, it is an antagonist on several serotonin receptors such as 5-HT2B, 5-HT6, and 5-HT7. The systemic effects of lisuride are profoundly dopaminergic and anti-serotonergic. It is the antagonism specifically of 5-HT2B that makes lisuride and its cousin terguride therapeutic for various fibrotic conditions. It is also worth noting, that lisuride is one of the few known so-called "inactivating" antagonists on the serotonin receptors 5-HT6 and 5-HT7.
    5-HT7 receptor - Wikipedia, the free encyclopedia
    An inactivaing antagonist renders a receptor persistently unable to react to an agonist such as serotonin or a serotonergic drug. This is similar to the effects of "suicidal" aromatase inhibitors like exemestane, which permanently deactivate the aromatase enzyme. These properties of lisuride suggest that it can have a very long-term serotonin antagonistic effects on specific receptors, and even a single dose can manifest its effects long after the lisuride is excreted from the body. This makes lisuride able to achieve therapeutic effects even with very infrequent dosing, which has been confirmed in clinical trials at least in regards to lowering prolactin.
    What makes our product different is its ability for topical administration. Lisuride has very low bioavailability when administered orally and also a very short half-life. Btw, this is nothing to be surprised at as the drug was designed for subcutaneous administration. The two poor features of oral administration is what essentially prevented lisuride from being approved in the USA given the better oral pharmacokinetcis of bromocriptine, cabergoline, pramipexole, etc. However, when administered transdermally dissolved in an effective solvent lisuride is a very different animal. It has close to 100% bioavailability and half-life of up to 6 hours. Given the much improved pharmacokinetics profile from transdermal adminsitration, combined with its serotonin inactivating antagonism and full spectrum of dopamine agonism lisuride is a potentially vastly superior chemical compared to the other dopaminergic drugs of the same class.
    Lisuride - Wikipedia, the free encyclopedia
    "...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 advocated, delaying the need for levodopa until lisuride becomes insufficient for controlling the parkinsonian disability. Preliminary trials suggest the dermal application of lisuride may be useful in the treatment of Parkinson's disease. As lisuride is very poorly absorbed when take orally and has a short half-life, continuous transdermal administration offers significant advantages and could make the compound a far more consistent therapeutic. Lisuride is not currently available in the US, as the drug was not a commercial success in comparison with other dopamine receptor agonist antiparkinsonian compounds."

    The units listed on the label are just for measurement purposes. They do not indicate suggested or optimal dose. Please note that similar to the products sold by companies like BlueSky, this product if for lab/research use only. The product can be ordered from the link below:
    IdeaLabs Online Store - Worldwide Ordering And Delivery - Laboratory Research Chemicals

    *******************************************************************************
    Lisuride is a chemical agent of the iso-ergoline class, related to the dopaminergic ergoline Parkinson's drugs. Lisuride is a full dopamine and a mixed agonist/antagonist for several serotonin receptors. It is an antagonist at the serotonin 5-HT2B receptor, which is its main mechanism of action in reversing fibrosis of various tissues and organs. It has a high affinity for the dopamine D2, D3 and D4 receptors, as well as D1, and D5. It is an agonist of 5-HT1Aand 5-HT2C receptors, and putative antagonist on 5-HT2A (which explains its antagonism to LSD hallucinogenic effects). Lisuride is also a putative histamine antagonist, on both H1 and H2 receptors.

    Units per container: about 30
    Unit size: 8 drops
    Each unit contains the following ingredients:

    Lisuride (maleate): 200 mcg

    Other ingredients: DMSO, ethanol
    Note: Liquid preparations of lisuride are best kept at a temp of 20 degrees C or lower to ensure shelf-life of at least 3 months.
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    References:

    Miscellaneous
    Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, ... - PubMed - NCBI
    Treatment of restless legs syndrome: an evidence-based review and implications for clinical practice. - PubMed - NCBI
    Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. - PubMed - NCBI
    In vitro pharmacology of clinically used central nervous system-active drugs as inverse H(1) receptor agonists. - PubMed - NCBI
    Glutamate-induced cell death and formation of radicals can be reduced by lisuride in mesencephalic primary cell culture. - PubMed - NCBI
    Mastalgia: a review of management. - PubMed - NCBI
    Involvement of 5-hydroxytryptamine (HT)7 receptors in the 5-HT excitatory effects on the rat urinary bladder. - PubMed - NCBI
    No evidence of the usefulness of eye blinking as a marker for central dopaminergic activity. - PubMed - NCBI
    Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats. - PubMed - NCBI
    Lisuride acts at multiple sites to induce ocular hypotension and mydriasis. - PubMed - NCBI
    Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors. - PubMed - NCBI
    Specific involvement of central 5-HT1A receptors in the mediation of male rat ejaculatory behavior. - PubMed - NCBI
    The effects of lisuride, terguride and bromocriptine on intraocular pressure (IOP). - PubMed - NCBI
    Comparative effects of LSD and lisuride: clues to specific hallucinogenic drug actions. - PubMed - NCBI
    Antagonism of L-5-hydroxytryptophan-induced head twitching in rats by lisuride: a mixed 5-hydroxytryptamine agonist-antagonist? - PubMed - NCBI
    Influence of lisuride, a dopaminergic agonist, on the sexual function of male patients with chronic renal failure. - PubMed - NCBI
    Serotonin involvement in lisuride-induced mounting and in sleep. - PubMed - NCBI
    Stimulation of dopamine autoreceptors elicits "premature ejaculation" in rats. - PubMed - NCBI
    Lisuride, LY-141865, and 8-OH-DPAT facilitate male rat sexual behavior via a non-dopaminergic mechanism. - PubMed - NCBI
    Spinal control of sexual behavior: effects of intrathecal administration of lisuride. - PubMed - NCBI
    Spinal control of sexual behavior: Effects of intrathecal administration of lisuride - ScienceDirect
    Lysergic acid diethylamide (LSD) and lisuride: differentiation of their neuropharmacological actions. - PubMed - NCBI
    Serotonergic and dopaminergic effects of yawning in the cat. - PubMed - NCBI
    The interaction of lisuride, an ergot derivative, with serotonergic and dopaminergic receptors in rabbit brain. - PubMed - NCBI
    Inhibition of neurotransmitter receptor binding by ergot derivatives. - PubMed - NCBI
    Stimulating effects of lisuride on masculine sexual behavior of rats. - PubMed - NCBI
    Induction of mounting behaviour in female and male rats by lisuride. - PubMed - NCBI



    Neurological/Brain
    Lisuride reduces involuntary periodic leg movements in spinocerebellar ataxia type 2 patients. - PubMed - NCBI
    Drug Treatments for the Prevention of Migraine Headache - PubMed - NCBI
    Anticonvulsive effects of the dopamine agonist lisuride maleate after experimental traumatic brain injury. - PubMed - NCBI
    Lisuride treatment of restless legs syndrome: first studies with monotherapy in de novo patients and in combination with levodopa in advanced disease. - PubMed - NCBI
    Transdermal lisuride: short-term efficacy and tolerability study in patients with severe restless legs syndrome. - PubMed - NCBI
    Transdermal lisuride delivery in the treatment of Parkinson's disease. - PubMed - NCBI
    The dopamine receptor agonist lisuride attenuates iron-mediated dopaminergic neurodegeneration. - PubMed - NCBI
    Protection of dopaminergic neurons in primary culture by lisuride. - PubMed - NCBI
    Lisuride treatment of Alzheimer's disease. A preliminary placebo-controlled clinical trial of safety and therapeutic efficacy. - PubMed - NCBI
    Lisuride prevents learning and memory impairment and attenuates the increase in extracellular dopamine induced by transient global cerebral ischemi... - PubMed - NCBI
    Neuroprotection by dopamine agonists. - PubMed - NCBI
    [Effect of lisuride on experimental cerebral infarction in rats]. - PubMed - NCBI
    Antagonist effect of terguride in Parkinson's disease. - PubMed - NCBI
    Chronic lisuride hydrogen maleate administration enhances muscarinic receptor binding in senescent rat brain. - PubMed - NCBI
    Intravenous administration of lisuride in the treatment of neuroleptic malignant syndrome. - PubMed - NCBI
    [Lisuride for the prevention of migraine. Results of a multicenter study]. - PubMed - NCBI
    Effects of lisuride hydrogen maleate on ischemia-induced depletion of brain acetylcholine levels in gerbils. - PubMed - NCBI
    Low dose lisuride in advanced Parkinson disease. - PubMed - NCBI
    [Analysis of the clinical experience with 136 patients with headache treated with lisuride]. - PubMed - NCBI
    Acute treatment of Huntington's chorea with lisuride. - PubMed - NCBI
    Beneficial effects of lisuride in Meige disease. - PubMed - NCBI
    The use of lisuride, a potent dopamine and serotonin agonist, in the treatment of progressive supranuclear palsy. - PubMed - NCBI
    Dopamine agonists and cobalt-induced epilepsy in the rat. - PubMed - NCBI
    Lisuride, a potent drug in the treatment of muscular rigisity in rats. - PubMed - NCBI



    Mood/Cognition/Behavior/Addiction
    [Treatment of premenstrual tension syndrome (PMS) with lisuride maleate]. - PubMed - NCBI
    The dopamine agonists lisuride and piribedil protect against behavioural and histological changes following 4-vessel occlusion in the rat. - PubMed - NCBI
    Striatal dopamine receptors and adenylyl cyclase activity in a rat model of alcohol addiction: effects of ethanol and lisuride treatment. - PubMed - NCBI
    The effects of lisuride on mood and sleep during acute withdrawal in stimulant abusers: a preliminary report. - PubMed - NCBI
    Lisuride reduces intravenous cocaine self-administration in rats. - PubMed - NCBI
    [Therapeutic effect of lisuride maleate on post-stroke depression]. - PubMed - NCBI
    Lisuride reduces psychomotor retardation during withdrawal from chronic intravenous amphetamine self-administration in rats. - PubMed - NCBI
    Treating organic abulia with bromocriptine and lisuride: four case studies. - PubMed - NCBI
    [Anxiolytic effects of lisuride and its agonistic action to central 5-HT1A receptors]. - PubMed - NCBI
    [Effects in animal models of depression of lisuride alone and upon coadministration with antidepressants]. - PubMed - NCBI
    Recovery of memory following forgetting induced by depletion of biogenic amines. - PubMed - NCBI



    CVD/Circulation
    Fibrotic heart-valve reactions to dopamine-agonist treatment in Parkinson's disease. - PubMed - NCBI
    Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports sup... - PubMed - NCBI
    Potential vascular alpha1-adrenoceptor blocking properties of an array of 5-HT receptor ligands in the rat. - PubMed - NCBI
    Agonism at 5-HT2B receptors is not a class effect of the ergolines. - PubMed - NCBI
    Mechanism of decrease in heart rate by peripheral dopaminergic D2-receptors. - PubMed - NCBI
    Studies on the inhibition of adrenaline-induced aggregation of blood platelets. - PubMed - NCBI


    Fibrosis/Cancer
    [Treatment of fibrocystic breast disease with lisuride]. - PubMed - NCBI


    Metabolism/Diabetes/Cortisol/Insulin/Obesity
    [The effect of noradrenaline and dopamine agonists and antagonists on oxygen consumption in some insect and crustacean species]. - PubMed - NCBI
    [Medical treatment of Cushing syndrome]. - PubMed - NCBI
    [Stimulatory effects of lisuride on local cerebral blood flow and local cerebral glucose utilization in rats]. - PubMed - NCBI
    Dopaminergic modulation of aldosterone secretion in the normal menstrual cycle. - PubMed - NCBI
    Dopamine control of aldosterone secretion in end-stage renal failure. - PubMed - NCBI
    Alpha-1 adrenergic blockade: a possible mechanism of action of dopaminergic drugs on ACTH secretion. - PubMed - NCBI
    Effect of short and long-term administration of lisuride in Cushing's disease. - PubMed - NCBI
    An in vitro stimulatory effect of indoleamines on aldosterone biosynthesis in the rat. - PubMed - NCBI
    Anorectic effect of lisuride and other ergot derivatives in the rat. - PubMed - NCBI
    Hypothermic action of lisuride in rats and differences to bromocriptine in the antagonistic effect of neuroleptics. - PubMed - NCBI


    Immune/Antirival/Antibacterial/Antiparasitic
    [Is dopaminergic therapy immunologically rejuvinating? Increased interferon-gamma production with the dopaminergic agent lisuride]. - PubMed - NCBI
     
  2. johnwester130

    johnwester130 Member

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    how does this compare to ritanserin ?
     
  3. OP
    haidut

    haidut Member

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    Different animal really. Lisuride is much more potent dopamine agonist and less of a serotonin antagonist. Ritanserin is a pure serotoi antagonist and its slight dopaminergic effects come from inhibiting the reuptake of dopamine as opposed to being agonist at dopamine receptors. As I mentioned in some threads, studies have called for combining such drugs for a synergistic effect.
     
  4. mirc12354

    mirc12354 Member

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    Could you please share your experience with it?
     
  5. Greg says

    Greg says Member

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    Stoked to try this. Well done. :clapping:
     
  6. johnwester130

    johnwester130 Member

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    can this be taken with methylene blue ?
     
  7. aarfai

    aarfai Member

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    Ordered. Just to double check can Lisuride be safety taken with Ritanserin?! Can you please post studies of combining the two.
     
  8. acrylic

    acrylic Member

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    Can you please provide more info on the safety profile (short and long term) of the substance? Thanks
     
  9. Dan Wich

    Dan Wich Member

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  10. lexis

    lexis Member

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    "It is an agonist of 5-HT1Aand 5-HT2C receptors"

    Is this a typo? It should be a 5HT2C receptor antagonist right?
     
  11. BobbyDukes

    BobbyDukes Member

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    Bought this, and the new t3. Boom. Finding it hard to keep up with what's getting released. Still a few to try that I haven't tried yet.
     
  12. Makrosky

    Makrosky Member

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    haidut, so do you think stuff like LSD or Psilocibin have also those "inactivating antagonist" properties ? It could explain why effects last a very long time (sometimes months) if you consume a big dose. Much less pronounced for microdosing though.

    Thanks for all your work man! You're top.
     
  13. lindsay

    lindsay Member

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    Hi @haidut - I was planning to buy another bottle of Ritanserin before heading away for three weeks. Do you think it's better to invest in Lisuride instead? The Ritanserin bottle is still almost full, so it could wait until return - especially since I have a lot of Cypro. Thanks!
     
  14. A.Dosko

    A.Dosko Member

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    Should lisuride have a positive effect on memory and learning?
     
  15. OP
    haidut

    haidut Member

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    They are very different chemicals, and actually best used together. So, if you have Ritanserin left then I think Lisuride is a better option to experiment on your rats in combination.
     
  16. OP
    haidut

    haidut Member

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    Yep, it reversed memory dysfunction due to stroke in a human clinical trial. I will be posting some studies in the thread later tonight.
     
  17. Pet Peeve

    Pet Peeve Member

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    Any rat reports yet?
     
  18. johnwester130

    johnwester130 Member

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    Can this be taken with methylene blue, or is that dangerous due to serotonin ?
     
  19. Dopamine

    Dopamine Member

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    Who knows? You would probaly be the first person in existence to try that combo. Both can effect blood pressure too I think. I wouldn't do it.
     
  20. Fractality

    Fractality Member

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    How long will this compound last if kept stored in a cool and dark drawer?
     
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