Talk:PCP

Phencyclidine does not have a "hole" and is very different from Ketamine. 3-Hydroxy-PCP is most similar to PCP and it's due to Inverse agonism at PCP-site-2, located as a second orthosteric pocket on the Sigma-1 Receptor (aka. The Dehydroepiandrosterone-Sulphate Binding Site) and the original one that Methamphetamine targets as the Pregnenolone Sulphate Binding Site....

Phencyclidine is noted in pKi, not Ki, indicating a short concentration increase leading to a exponential rise or decrease in Emax achieved. The NMDA (PCPsite1) antagonism is immediate but the PCPsite2 Inverse agonism takes a minute before locking in. This leads to seeing a white light and hearing a smack due to the sudden rise in Norepinephrine in the brain stem within a millisecond being 1,000 - 4,000% and Dopamine at 4,000 - 10,000%. It still retains D2 Agonist activity but as a superagonist. Here's the correct binding Affinity

NMDAR -Ki: 0.09nM -IA: -100%

PCPsite2: -pKi: 0.0015nM -IA: -3,137%

Dopamine D2R: -pKi: 0.091nM -IA: +398%

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