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25I-NBOMe: Difference between revisions
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25I-NBOMe has efficacy at the [[serotonin#The 5-HT system|5-HT<sub>2A</sub> receptor]] where it acts as a potent [[Agonist#Agonists|partial agonist]]. However, the role of these interactions and how they result in the [[psychedelic]] experience continues to remain elusive. | 25I-NBOMe has efficacy at the [[serotonin#The 5-HT system|5-HT<sub>2A</sub> receptor]] where it acts as a potent [[Agonist#Agonists|partial agonist]]. However, the role of these interactions and how they result in the [[psychedelic]] experience continues to remain elusive. | ||
This compound is pharmacologically unique when compared to other psychedelics through its action on [[serotonin]] receptors. It is one of the only [[Agonist#Agonists|full agonists]] for the human [[Serotonin#The 5-HT system|5-HT<sub>2A</sub> receptor]] receptor in existence.<ref name="pmid21174090">Ettrup, A. E. A. ; Hansen, M.; Santini, M. A.; Paine, J.; Gillings, N.; Palner, M.; Lehel, S.; Herth, M. M.; Madsen, J. (2010). "Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers". European Journal of Nuclear Medicine and Molecular Imaging 38 (4): 681–693. | http://www.ncbi.nlm.nih.gov/pubmed/21174090</ref> In comparison, classical psychedelics such as [[LSD]], [[DMT]] and [[psilocin]] can only be considered [[Agonist#Agonists|partial agonists]]. | This compound is pharmacologically unique when compared to other psychedelics through its action on [[serotonin]] receptors. It is one of the only [[Agonist#Agonists|full agonists]] for the human [[Serotonin#The 5-HT system|5-HT<sub>2A</sub> receptor]] receptor in existence.<ref name="pmid21174090">Ettrup, A. E. A. ; Hansen, M.; Santini, M. A.; Paine, J.; Gillings, N.; Palner, M.; Lehel, S.; Herth, M. M.; Madsen, J. (2010). "Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers". European Journal of Nuclear Medicine and Molecular Imaging 38 (4): 681–693. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21174090</ref> In comparison, classical psychedelics such as [[LSD]], [[DMT]] and [[psilocin]] can only be considered [[Agonist#Agonists|partial agonists]]. | ||
The [[Ki values]] of the following targets were greater than 500 Ki: [[5-HT1A]], [[D3]], [[H2]], [[5-HT1D]], [[α1A adrenergic]], [[δ opioid]], [[serotonin uptake transporter]], [[5-HT5A]], [[5-HT1B]], [[D2]], [[5-HT7]], [[D1]], [[5-HT3]], [[5-HT1E]], [[D5]], [[muscarinic M1-M5]], [[H3]], and the [[dopamine uptake transporter]].<ref name="high specific">High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand | https://www.ncbi.nlm.nih.gov/pubmed/18468904</ref> | The [[Ki values]] of the following targets were greater than 500 Ki: [[5-HT1A]], [[D3]], [[H2]], [[5-HT1D]], [[α1A adrenergic]], [[δ opioid]], [[serotonin uptake transporter]], [[5-HT5A]], [[5-HT1B]], [[D2]], [[5-HT7]], [[D1]], [[5-HT3]], [[5-HT1E]], [[D5]], [[muscarinic M1-M5]], [[H3]], and the [[dopamine uptake transporter]].<ref name="high specific">High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand | https://www.ncbi.nlm.nih.gov/pubmed/18468904</ref> | ||