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Drug info - Cannabinoid CB1/CB2 Binding Affinity Chart - BETA

Discussion in 'Cannabinoids' started by msimm, Feb 10, 2010.

  1. DocBrock

    DocBrock Silver Member

    Reputation Points:
    Feb 13, 2012
    from earth
    Sorry, can't translate.

    Take it you've stopped smoking the blend.In terms of changing forever, no. Watch for some of those blends though, they can contain unexpected surprises for some. Oh, you've discovered that. Yeah, me too. AM-2201 is my bogie. The difference between happytrippyhigh and meanuglycolddrawnoutenditnow is measured for me in very small amounts.
    12mg, lovely.
    15mg, Fast and lovely. Nice place to be. Tripping, stoned, happy.
    20mg, Stop the world I want to get off. Not nice.
    25mg, due to accidently being a doofus when taring. Very horrid, scary trip.
    10-15mg is my comfort zone.
    My tolerance doesn't seem to build that high on -some- binnoids. Redose urging yes, dosage increase no. Stop for a week and the same amounts work as before. Much lower redose rate. Some however, tolerance hits very very fast indeed. I wonder about hitting 'as high as this can take me' and confusing it with tolerance?

    Are you self medicating the benzos, or are they on scrip, and how many mgs?
    Cut down on the benzos. I found they started reinforcing the anxiety instead of alleviate it. What I'd done is increase my dose, which quelled the 'overcome the anxiety' voices and drive, which, as that was one of my weapons against anxiety, left me anxious, hence increasing the dose.
    By dropping back to my taper level, I had a day of crap, but the anxiety levels dropped rapidly. Seems counter-intuitive, but worked for me.
    Last edited: May 20, 2012
  2. waldo22

    waldo22 Silver Member

    Reputation Points:
    Sep 25, 2012
    from The Netherlands
    Only tested in rats, but looks very interesting.
    Strong and good Cb1/Cb2 Ratio.
    Unknown how it reacts with Cb3 (GPR55) receptor.

    a dual CB1/CB2agonist
    CB(1)=K(i) 0.032 μM, EC(50) 0.056 μM.
    CB(2)=K(i) 0.049 μM, EC(50) 0.014 μM.
  3. Shampoo

    Shampoo entity of sorts Staff Member

    Reputation Points:
    Nov 10, 2007
    from france
    Where was this compound tested in animals? Only simple binding assays have been done, as far as I can see - no animal work. And what do you think makes it look interesting?
  4. Curioustripper297

    Curioustripper297 Newbie

    Reputation Points:
    Nov 11, 2012
    27 y/o from U.S.A.
    Swim smokes the herbal incense and he thinks am2201 is in it in all of the incense blend in his area so if you want to know what is in your bag than it is probaly am2201 and jwh's bunch does anyone know if they are putting bath salt chemicals in the incense
  5. Alfa

    Alfa Productive Insomniac Staff Member Administrator

    Reputation Points:
    Jan 14, 2003
    117 y/o from The Netherlands
    Can someone please update this chart with new cannabinoids and new research that have been done in the last years?
    Loads of reputation will be sent!
  6. stryder09

    stryder09 Silver Member

    Reputation Points:
    Dec 19, 2010
    from U.S.A.
    Here are a few updates:

    Frost, JM et al. (2010), ‘Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB2 cannabinoid receptor activity’, Journal of Medicinal Chemistry 53 (1): 295-314.

    A796,260: Binding affinity (Ki) at CB1 is 945 nM; Binding affinity (Ki) at CB2 is 4.6 nM

    A834,735: Binding affinity (Ki) at CB1 is 12 nM; Binding affinity (Ki) at CB2 is 0.21 nM

    AM1241: Binding affinity (Ki) at CB1 is 11.5 nM; Binding affinity (Ki) at CB2 is 1269 nM

    UR-144: Binding affinity (Ki) at CB1 is 150 nM; Binding affinity (Ki) at CB2 is 1.8 nM

    McGaraughty, S et al. (2009), ‘A CB2 receptor agonist, A836339, modulates wide dynamic range neuronal activity in neuropathic rats: contributions of spinal and peripheral CB2 receptors’, Neuroscience 158 (4): 1652-1661.

    A836,339: Binding affinity (Ki) at CB1 is 270 nM; Binding affinity (Ki) at CB2 is 0.64 nM

    Dziadulewicz EK, et al. (2007), 'Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration. Journal of Medicinal Chemistry 50 (16): 3851-3856.

    CB13: Binding affinity (Ki) at CB1 is 15 nM; Binding affinity (Ki) at CB2 is 98 nM.

    As far as I know, the following newer compounds have not had binding affinity determined through in-vitro assay:

    AB-001, AKB48, 5F-AKB48, 2NE1, EAM-2201, MAM-2201, STS-135, UR-144-chloropentyl, UR-144-bromopentyl, XLR-11

    Last edited by a moderator: Apr 30, 2017
  7. happy thoughts1

    happy thoughts1 Newbie

    Reputation Points:
    Feb 21, 2011
    from U.K.
    Now I apologise in advance if this post should not be here or lacks info but I stumbled across a fair few cannabinoids not listed

    These are as below:

    Arvanil: CB1/VR1 agonist

    DEA: Endogenous CB1 agonist

    Leelamine hydrochloride: CB1 agonist

    (R)-(+)-Methanandamide: Potent and selective CB1 agonist

    NADA: Endogenous CB1 agonist. Also vanilloid agonist and inhibitor of FAAH and AMT

    Noladin ether: Endogenous agonist for both CB1 and GPR55

    Oleamide: CB1 agonist

    RVD-Hpa: Selective CB1 agonist

    CB 65: High affinity, selective CB2 agonist

    GP 1a: Highly selective CB2 agonist

    GP 2a: Selective CB2 agonist

    GW 405833: Selective, high affinity partial CB2 agonist

    MDA 19: CB2 agonist

    SER 601: Potent, selective CB2 agonist

    AM 1172: CB receptor partial agonist

    Anandamide: Endogenous CB receptor agonist

    2-Arachidonylglycerol: Endogenous cannabinoid agonist

    WIN 55,212-2 mesylate: Highly potent cannabinoid agonist

    O-2545 hydrochloride: High affinity, water-soluble CB1/CB2 agonist
    CB 13: Potent CB1/CB2 agonist

    2-Palmitoylglycerol: Endogenous lipid, enhances activity of 2-Arachidonylglycerol

    N-ArachidonylGABA: Inhibits pain

    N-Arachidonylglycine: Novel endocannabinoid. Suppresses pain

    So all in all, some pretty interesting cannabinoids there, I myself have taken a particular liking to O-2545 hydrochloride for it's water-solubility (seems promising for future in-vivo research)
  8. someguy04

    someguy04 Newbie

    Reputation Points:
    Apr 25, 2016
    34 y/o from U.S.A.
    Can anyone tell me what the affinity is for ORG-28611? Also I am guessing since it is water-soluble that it has a high affinity like O-2545 and would be measured lower than grams for dosing when making a blend unlike a lipid soluble compound?
  9. Shampoo

    Shampoo entity of sorts Staff Member

    Reputation Points:
    Nov 10, 2007
    from france
    CB1 pKi: 8.9, CB2 pKi: 8.8. So, it has a predicted (and in animals, confirmed) potency slightly above that of CP 55,940.
    The water-solubility has nothing to do with the affinity. The dosage should be in µg or mg, not grams.