Ritanserin - Serotonin Antagonist For R&D Use Only

Discussion in 'IdeaLabs' started by haidut, Jun 29, 2016.

  1. haidut

    haidut Member

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    As promised, I finally got around to releasing the unicorn of the anti-serotonin world - i.e. the chemical known as ritanserin. It does not have a trade name as it is a research/lab chemical only and was never submitted for approval by the FDA. However, research with ritanserin is thriving and there are quite a few studies and even humans trials. Ritanserin was developed as an alternative to cyproheptadine with the goal of causing less sedation, having less anti-cholinergic effects, and no antagonism to dopamine "receptors". In fact, ritanserin has been found to have a pronounced pro-dopamine effect and robustly increases libido in animals models, which is consistent with its dopaminergic effects.
    http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1290899/pdf/jrsocmed00173-0013.pdf

    "...Ritanserin is the first extremely potent, specific and pure serotonin-S2 antagonist that passes the blood-brain barrier easily. It belongs to a new series of chemically related compounds of which ketanserin, a peripherally acting 5-HT2 receptor antagonist under clinical investigation for cardiovascular diseases, is the prototype. From the receptor binding point of view [31], the most remarkable feature of ritanserin is its high binding affinity for serotonin-S2 receptors. In rat frontal cortex, only 0.9 nmol concentration of ritanserin is needed to displace the ligand ketanserin from the receptor binding sites. The IC50 values for binding to other sites (histamine H1, dopamine-D2, a, and a2-adrenergic sites) are so much higher that they are of no pharmacological importance. The fact that ritanserin is devoid of any dopamine-D2 antagonism means that it is devoid of any neuroleptic activity."

    However, please note that similar to the products sold by companies like BluePeptides, 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

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    Ritanserin is a potent general serotonin antagonist targeting mostly the 5-HT2 receptor, as well as the 5-HT1, 5-HT5, 5-HT6, and 5-HT7, H1, and alpha1 / alpha2 adrenergic receptors. Ritanserin is extensively used in clinical and experimental studies and is widely considered the most selective antagonist of serotonin "receptors" when used in the appropriate dose range. It has no known dopamine antagonism when used in relevant pharmacological doses.

    Drops per container: about 360
    Each drop contains the following ingredients:

    Ritanserin: 0.5 mg

    Other ingredients: DMSO, ethanol
    *******************************************************************************

    References:
    Ritanserin - Wikipedia, the free encyclopedia
    Effect of ritanserin, a 5HT2A/2C antagonist, on negative symptoms of schizophrenia: a double-blind randomized placebo-controlled study. - PubMed - NCBI
    Ritanserin improves sleep quality in narcolepsy. - PubMed - NCBI
    Ritanserin, a selective 5-HT2/1C antagonist, and negative symptoms in schizophrenia. A placebo-controlled double-blind trial. - PubMed - NCBI
    [Ritanserin in autistic children]. - PubMed - NCBI
    Ritanserin, a serotonin-2 receptor antagonist, improves ultradian sleep rhythmicity in young poor sleepers. - PubMed - NCBI
    Effect of the serotonin antagonists ritanserin and ketanserin in Cushing's disease. - PubMed - NCBI
    A randomized, double-blind, placebo-controlled study of ritanserin pharmacotherapy for cocaine dependence. - PubMed - NCBI
    Effects of ritanserin on ethanol withdrawal-induced anxiety in rats. - PubMed - NCBI
    Ritanserin in relapse prevention in abstinent alcoholics: results from a placebo-controlled double-blind international multicenter trial. Ritanseri... - PubMed - NCBI
    Ritanserin, a 5-HT2 receptor antagonist, increases subcortical blood flow following photothrombotic middle cerebral artery occlusion in rats. - PubMed - NCBI
    A randomised double-blind 16-week study of ritanserin in fibromyalgia syndrome: clinical outcome and analysis of autoantibodies to serotonin, gangl... - PubMed - NCBI
    Effects of ritanserin, a novel serotonin-S2 receptor antagonist, on the secretion of pituitary hormones in normal humans. - PubMed - NCBI
    Potential therapeutic effects of ritanserin in Cushing's disease. - PubMed - NCBI
    Effect of ritanserin, a highly selective 5-HT2 receptor antagonist, on Parkinson's disease. - PubMed - NCBI
    Inhibitory effect of ritanserin on the 5-hydroxytryptophan-mediated cortisol, ACTH and prolactin secretion in humans. - PubMed - NCBI
    Effect of ritanserin, specific 5HT-2 antagonist, on PRL secretion in normal subjects and in different hyperprolactinaemic conditions. - PubMed - NCBI
    Psychotropic effects of ritanserin, a selective S2 antagonist: an open study. - PubMed - NCBI
    Ritanserin decreases portal pressure in conscious and unrestrained cirrhotic rats. - PubMed - NCBI
    The effects of the 5 HT2 antagonist ritanserin on blood pressure and serotonin-induced platelet aggregation in patients with untreated essential hy... - PubMed - NCBI
    Serotonin antagonism in panic disorder: an open trial with ritanserin. - PubMed - NCBI
    Serotonin as a modulator of skeletal muscle oxygenation: effects of ketanserin and ritanserin on oxygen pressure distributions. - PubMed - NCBI
    Does ritanserin, a potent serotonin-S2 antagonist, restore energetic functions during the night? - PubMed - NCBI
    The 5-HT2 antagonist ritanserin blocks dopamine re-uptake in the rat frontal cortex. - PubMed - NCBI
    Facilitatory effect of ritanserin is mediated by dopamine D(1) receptors on olfactory learning in young rats. - PubMed - NCBI
    Behavioral and neuroendocrine assessment of ritanserin exposure in the developing chicken: lack of toxicity at effective doses. - PubMed - NCBI
    Ritanserin administration potentiates amphetamine-stimulated dopamine release in the rat prefrontal cortex. - PubMed - NCBI
    Local infusion of the serotonin antagonists ritanserin or ICS 205,930 increases in vivo dopamine release in the rat medial prefrontal cortex. - PubMed - NCBI
     
  2. Tarmander

    Tarmander Member

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    If I were going to do research on rats or humans, and giving them this, what would be the longest duration I would be able to give them ritanserin without any toxicity?
     
  3. firebreather

    firebreather Member

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    is it possible to order this along with your K2 supplement at the same time?

    I'm trying to order but paypal doesn't seem to want to put both in the same cart
     
  4. GAF

    GAF Member

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    Ordered 2...will report results.

    It would be fun to start doing our own RPF "scientific" studies

    Send placebo to some and real to some and then require the participants to track something or fill out a questionnaire or whatever these studies require and then compile the results etc.
     
  5. GAF

    GAF Member

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    Idealabs is now an order filling machine...I ordered at about 1:58pm Texas time and I received a shipping tracking # at 2:20 pm - a whopping 22 minutes.
     
  6. OP
    haidut

    haidut Member

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    Send me a PM please.
     
  7. OP
    haidut

    haidut Member

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    Thank you! And the package is already in transit actually. The warehouse is right next to a major post office and they pick up packages twice daily - at 3pm and 5pm. So, yours was picked up with the 3pm batch and is on its way. Just a little something separating us from the crowd :):
     
  8. OP
    haidut

    haidut Member

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    Human studies posted above show trials using 10mg - 15mg for Cushign disease and lasting for up to a year with no side effects except sleepiness. At 6mg daily, the risk is even lower IMO.
     
  9. firebreather

    firebreather Member

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    Sent, thanks so much
     
  10. OP
    haidut

    haidut Member

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    It's funny you mention that. I am actually setting up several (rodent) studies in Europe this summer. I plan on replicating the studies with EFA deficiency, as well as the original studies on the Hayflick limit related to cell immortality. We should have some preliminary results this fall.
    But in regards to the studies with forum people, it's called Health Hacking and some groups in US are doing a lot of that. Not sure how that affects the forum legally but maybe @charlie can chime in with his opinion. I know the health hacking groups are definitely not limiting themselves with OTC supplements. It may be possible with a group of people that has a valid prescription for a given drug and signs a disclaimer that they will share health information with other. Anyways, it would be exciting indeed if it is legally OK.
     
  11. Pet Peeve

    Pet Peeve Member

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    Awesome, but no anti-histamine effect then?
     
  12. OP
    haidut

    haidut Member

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    There is some but not as strong as cyproheptadine or Benadryl.
     
  13. Drareg

    Drareg Member

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    This sounds incredible. Thanks.
     
  14. DaveFoster

    DaveFoster Member

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    Exactly this. Unbelievable. Euphoric about this.

    Do you know of any contraindications between this and cyproheptadine? I'm thinking about a low-dose cypro and some of this, perhaps.
     
  15. OP
    haidut

    haidut Member

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    I don't think there would be any contraindication, the phrmacological profile is pretty similar. On the contrary, if using both ritanserin and cyproheptadine much lower doses of each can probably be used to achieve the same results. I'd venture a guess that 1mg cypro and 1m gritanserin would be equivalent in effects to maybe 4mg - 6mg cypro on its own.
     
  16. DaveFoster

    DaveFoster Member

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    Perfect. That's right in the range that Ray recommends for therapeutic use of cypro. Thanks.
     
  17. Makrosky

    Makrosky Member

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    This is huge haidut! Thank you so much!!
     
  18. johnwester130

    johnwester130 Member

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    where is this ??
     
  19. TheHound

    TheHound Member

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    would this be better than lisuride? I know you had plans to release a lisuride supplement so I'm wondering if I should just wait for that
     
  20. Rose Heiress

    Rose Heiress Member

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    I'll happily pretend to be a rat
     
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