3-MeO-PCP: Difference between revisions

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3-MeO-PCP acts as an [[NMDA receptor antagonist]]. A specific subtype of glutamate receptor, NMDA (N-Methyl-D-Aspartate), modulates the transmission of electrical signals between neurons in the brain and spinal cord; for the signals to pass, the receptor must be open.

Dissociatives inhibit the normal functioning NMDA receptors by binding to and blocking them. This disruption of neural network activity leads to loss of normal cognitive and affective processing, psychomotor functioning, anesthesia and eventually ~~an almost identical~~ equivalent of ~~the famous “[http://en.wikipedia.org/wiki/K-hole~~ k-hole].”

Dissociatives inhibit the normal functioning NMDA receptors by binding to and blocking them. This disruption of neural network activity leads to loss of normal cognitive and affective processing, psychomotor functioning, anesthesia and eventually the equivalent of a "k-hole".

3-MeO-PCP has a Ki of 20 nM for the NMDA receptor, 216 nM for the serotonin transporter (SERT),42 nM for the sigma-1 receptor ~~and 2097 nM for the H1 Receptor~~ <ref name="AMCD">Advisory Council on the Misuse of Drugs (ACMD) Methoxetamine report, 2012 | https://www.gov.uk/government/publications/advisory-council-on-the-misuse-of-drugs-acmd-methoxetamine-report-2012</ref> It binds to the NMDA receptor with higher affinity than PCP and has the highest affinity of the three isomeric anisyl-substitutions, followed by 2-MeO-PCP and 4-MeO-PCP. http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0194984

3-MeO-PCP has a Ki of 20 nM for the NMDA receptor, 216 nM for the serotonin transporter (SERT), and 42 nM for the sigma-1 receptor <ref name="AMCD">Advisory Council on the Misuse of Drugs (ACMD) Methoxetamine report, 2012 | https://www.gov.uk/government/publications/advisory-council-on-the-misuse-of-drugs-acmd-methoxetamine-report-2012</ref> It binds to the NMDA receptor with higher affinity than PCP and has the highest affinity of the three isomeric anisyl-substitutions, followed by 2-MeO-PCP and 4-MeO-PCP.<ref>http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0194984</ref>

Although 3-MeO-PCP was once ~~famously described as possessing~~ opioid or dopaminergic activity,<ref name="chemist">Interview with a ketamine chemist: or to be more precise, an arylcyclohexylamine chemist | http://www.vice.com/read/interview-with-ketamine-chemist-704-v18n2</ref> this supposition is contradicted by data showing 3-MeO-PCP to be a potent and selective ligand for the NMDA receptor without appreciable affinity for the µ-opioid receptor or dopamine transporter.<ref name="AMCD2">The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor | http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0059334</ref> 3-MeO-PCP was preceded by the less potent dissociative 4-MeO-PCP and first became available as a [[research chemical]] in 2011.<ref name="PCP2MXE" />

Although 3-MeO-PCP was once claimed to possess opioid or dopaminergic activity,<ref name="chemist">Interview with a ketamine chemist: or to be more precise, an arylcyclohexylamine chemist | http://www.vice.com/read/interview-with-ketamine-chemist-704-v18n2</ref> this supposition is contradicted by data showing 3-MeO-PCP to be a potent and selective ligand for the NMDA receptor without appreciable affinity for the µ-opioid receptor or dopamine transporter.<ref name="AMCD2">The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor | http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0059334</ref> 3-MeO-PCP was preceded by the less potent dissociative 4-MeO-PCP and first became available as a [[research chemical]] in 2011.<ref name="PCP2MXE" />

==Subjective effects==

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 -MeO-PCP acts as an [[NMDA receptor antagonist]]. A specific subtype of glutamate receptor, NMDA (N-Methyl-D-Aspartate), modulates the transmission of electrical signals between neurons in the brain and spinal cord; for the signals to pass, the receptor must be open.
-Dissociatives inhibit the normal functioning NMDA receptors by binding to and blocking them. This disruption of neural network activity leads to loss of normal cognitive and affective processing, psychomotor functioning, anesthesia and eventually an almost identical equivalent of the famous “[http://en.wikipedia.org/wiki/K-hole k-hole].”
+Dissociatives inhibit the normal functioning NMDA receptors by binding to and blocking them. This disruption of neural network activity leads to loss of normal cognitive and affective processing, psychomotor functioning, anesthesia and eventually the equivalent of a "k-hole".
--MeO-PCP has a Ki of 20 nM for the NMDA receptor, 216 nM for the serotonin transporter (SERT),42 nM for the sigma-1 receptor and 2097 nM for the H1 Receptor <ref name=&quot;AMCD&quot;>Advisory Council on the Misuse of Drugs (ACMD) Methoxetamine report, 2012 | https://www.gov.uk/government/publications/advisory-council-on-the-misuse-of-drugs-acmd-methoxetamine-report-2012</ref> It binds to the NMDA receptor with higher affinity than PCP and has the highest affinity of the three isomeric anisyl-substitutions, followed by 2-MeO-PCP and 4-MeO-PCP. http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0194984
+-MeO-PCP has a Ki of 20 nM for the NMDA receptor, 216 nM for the serotonin transporter (SERT), and 42 nM for the sigma-1 receptor <ref name=&quot;AMCD&quot;>Advisory Council on the Misuse of Drugs (ACMD) Methoxetamine report, 2012 | https://www.gov.uk/government/publications/advisory-council-on-the-misuse-of-drugs-acmd-methoxetamine-report-2012</ref> It binds to the NMDA receptor with higher affinity than PCP and has the highest affinity of the three isomeric anisyl-substitutions, followed by 2-MeO-PCP and 4-MeO-PCP.<ref>http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0194984</ref>
-Although 3-MeO-PCP was once famously described as possessing opioid or dopaminergic activity,<ref name="chemist">Interview with a ketamine chemist: or to be more precise, an arylcyclohexylamine chemist | http://www.vice.com/read/interview-with-ketamine-chemist-704-v18n2</ref> this supposition is contradicted by data showing 3-MeO-PCP to be a potent and selective ligand for the NMDA receptor without appreciable affinity for the µ-opioid receptor or dopamine transporter.<ref name="AMCD2">The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor | http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0059334</ref> 3-MeO-PCP was preceded by the less potent dissociative 4-MeO-PCP and first became available as a [[research chemical]] in 2011.<ref name="PCP2MXE" />
+Although 3-MeO-PCP was once claimed to possess opioid or dopaminergic activity,<ref name="chemist">Interview with a ketamine chemist: or to be more precise, an arylcyclohexylamine chemist | http://www.vice.com/read/interview-with-ketamine-chemist-704-v18n2</ref> this supposition is contradicted by data showing 3-MeO-PCP to be a potent and selective ligand for the NMDA receptor without appreciable affinity for the µ-opioid receptor or dopamine transporter.<ref name="AMCD2">The Ketamine Analogue Methoxetamine and 3- and 4-Methoxy Analogues of Phencyclidine Are High Affinity and Selective Ligands for the Glutamate NMDA Receptor | http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0059334</ref> 3-MeO-PCP was preceded by the less potent dissociative 4-MeO-PCP and first became available as a [[research chemical]] in 2011.<ref name="PCP2MXE" />
 ==Subjective effects==