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Phencyclidine, a high-affinity ligand of PCP site 2.. PCP site 2 is a binding site that was identified as a high-affinity target for phencyclidine (PCP), an anesthetic and dissociative hallucinogen that acts primarily as an NMDA receptor antagonist. [1]
Phencyclidine (PCP) is believed to be the first arylcyclohexylamine with recognized anesthetic properties, but several arylcyclohexylamines were described before PCP in the scientific literature, beginning with PCA (1-phenylcyclohexan-1-amine) the synthesis of which was first published in 1907. PCP itself was discovered in 1926 but not ...
Phencyclidine or phenylcyclohexyl piperidine (PCP), also known in its use as a street drug as angel dust among other names, is a dissociative anesthetic mainly used recreationally for its significant mind-altering effects. [1] [4] PCP may cause hallucinations, distorted perceptions of sounds, and violent behavior.
Phencyclidine (also known as PCP or "Angel Dust") and ketamine, both of which block glutamate receptors, are known to cause psychosis at least somewhat resembling schizophrenia, further suggesting that psychosis and perhaps schizophrenia cannot fully be explained in terms of dopamine function, but may also involve other neurotransmitters. [57]
This key finding allowed pharmacologists to begin researching if the Na V 1.7 is a substantial molecular target for analgesic (antipain) medications. [ 5 ] Sensitization , in the clinical sense of the word, is a phenomenon in which nociceptors in an area beyond a tissue injury exhibit decreased thresholds for activation.
[3] [4] [5] Methamphetamine psychosis, or long-term effects of stimulant use in the brain (at the molecular level), depend upon genetics and may persist for months or years. [6] Psychosis may also result from withdrawal from stimulants, particularly when psychotic symptoms were present during use. [7]
Ketamine produces more similar symptoms (hallucinations, withdrawal) without observed permanent effects (other than ketamine tolerance). Both arylcyclohexamines have some(uM) affinity to D2 and as triple reuptake inhibitors. PCP is representative symptomatically, but does appear to cause brain structure changes seen in schizophrenia. [22]
The high affinity of 3-HO-PCP for opioid receptors is unique among arylcyclohexylamines and is in contrast to PCP, which has only very low affinity for the MOR (K i = 11,000–26,000 nM; 282- to 433-fold difference) and the other opioid receptors (K i = 4,100 nM for the KOR and 73,000 nM for the DOR).