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Many people are well aware of kratom (mitragyna speciosa), Salvia Divinorum and poppy (papaver somniferum) so for now SWIM will not discuss these given the abundance of information on them on this forum already. Keep in mind that despite being legal, the potency and binding affinities of most of the alkaloids in these plants have not yet been evaluated so if one decides to experiment with these plants, EXERCISE CAUTION.
Nepeta Cataria-Contains alpha,7alpha,7a alpha-nepetalactone (also found in Nepeta Caesarea) which has displayed analgesic effects which have been reversed by naloxone. Believed to act on kappa or delta receptors.
Commiphora Myrrha-Contains furanoeudesma-1,3-diene and a still unidentified terpene which act on opioid receptors. No additional information available online.
Peripentadenia Mearsii- peripentonine A, B, and C, peripentadenine and mearsamine are alkaloids found in the leaves of this tree. Peripentadenine, Peripentonine A/B (isolated as inseparable diastereomers) and Perpentonine C showed IC50 values of 11.4, 69.2, and 30.9 microM for the delta-opioid receptor. Keep in mind that IC50 is NOT the same as binding affinity (Ki), which still has to be determined.
Picralima nitida-The seeds of this plants contain akuammidine, akuammine, akuammicine, akuammigine and pseudoakuammigine. Akuammidine binding most at mu receptors, the Ki values for mu, delta and kappa binding sites were .6, 2.4 and 8.6 microM. Akuammine showed a Ki at mu sites of .5 microM but showed some antagonist activity with a pkB of 5.7 against the mu agonist DAMGO. Akuammicine at the kappa sites has a Ki of .2 microM. Akuammigine and psuedoakuammigine displayed little or no binding at opioid receptors.
Psychotria Umbellata-SWIM made post about this plant a while back. It contains umbellatine, an opioid and NMDA antagonist. This was determined by observation of reversal of effects by naloxone (opioid antagonist) and also an observation of synergy when combined with the NMDA antagonist MK-801. This plant also contais Psychollatine, an indole with anxiolytic and antidepressant effects comparable to the powerful tricyclic antidepressant imipramine. This compound is believed to act at the HT(A/C) receptors.
Psychotria Colorata-Contains Psychotridine, an analgesic with NMDA antagonistic properties. Also contains Hodgkinsine, a mu opioid agonist and NMDA antagonist.
Psychotria Brachypoda-Extracts of leaves have exhibited opioid activity so it might contain some of the same alkaloids from P. Colorata and/or P. Umbellata.
Dalea purpurea-Contains the geranyl stilbenes Pawhuskin A, B and C. Pawhuskin A has displayed the strongest opioid activity with a Ki of .29 +/- 0.11 microM.
Nigella Sativa-Contains thymoquinone which acts on mu and kappa receptors.
Stephania japonica-8 Hasubanan alkaloids and 1 morphinane alkaloid have been isolated from this vine. The hasubanan alkaloids showed affinity for delta-opioid receptors, with equal potency at mu receptors and no activity at kappa receptors. IC50 values at delta opioid receptor ranged from .7 to 46 microM.
Actaea racemosa-Contains a partial mu-opioid agonist.
Elaeocarpus grandis-The leaves of this tree contain grandisine A, B, C, D, E, F, G and isoelaeocarpiline. All these alkaloids show affinity for the delta-opioid receptor. IC50 values at delta-receptors for Grandisines C-G were 14.6, 1.65, 1.55, 75.4, and 9.9 microM.
Elaeocarpus fuscoides- elaeocarpenine, isoelaeocarpicine, isoelaeocarpine and elaeocarpine are found in this tree. IC50 values at the delta-opioid receptor are 2.7, 35.1, 13.6, and 86.4 microM.
List will be updated as SWIM finds more plants.
On a related note, Does anyone have the Ki values for any weaker opiates such as mitragynine or codeine? Please post them if so for comparison with the alkaloids listed above that have the Ki values established.
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“New geranyl stilbenes from Dalea purpurea with in vitro opioid receptor affinity.”
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Working on Myrrh source, having trouble.
“Alkaloids with human delta-opioid receptor binding affinity from the Australian rainforest tree Peripentadenia mearsii.” Katavic PL, Venables DA, Guymer GP, Forster PI, Carroll AR. J Nat Prod. 2007 PMID: 18039010
“Hasubanan alkaloids with delta-opioid binding affinity from the aerial parts of Stephania japonica.” Carroll AR, Arumugan T, Redburn J, Ngo A, Guymer GP, Forster PI, Quinn RJ. J Nat Prod. 2010 PMID: 20426456
“Indolizidine alkaloids with delta-opioid receptor binding affinity from the leaves of Elaeocarpus fuscoides.” Katavic PL, Venables DA, Rali T, Carroll AR. J Nat Prod. 2007 PMID: 17451272
“Grandisine A and B, novel indolizidine alkaloids with human delta-opioid receptor binding affinity from the leaves of the Australian rainforest tree Elaeocarpus grandis.”
Carroll AR, Arumugan G, Quinn RJ, Redburn J, Guymer G, Grimshaw P. J Org Chem. 2005 PMID: 15730315
“Grandisines C-G, indolizidine alkaloids from the Australian rainforest tree Elaeocarpus grandis.” Katavic PL, Venables DA, Forster PI, Guymer G, Carroll AR. J Nat Prod. 2006
“Opioid activity of alkaloids extracted from Picralima nitida (fam. Apocynaceae).”
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“Antinociceptive effects of Nigella sativa oil and its major component, thymoquinone, in mice.”
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