Role of the aromatic group in the inhibition of phencyclidine binding and dopamine uptake by PCP analogs

  title={Role of the aromatic group in the inhibition of phencyclidine binding and dopamine uptake by PCP analogs},
  author={Isabelle Chaudieu and Jacques Vignon and Mich{\`e}le Chicheportiche and Jean Marc Kamenka and G{\'e}rard Trouiller and Robert Rubin Chicheportiche},
  journal={Pharmacology Biochemistry and Behavior},

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b]thienyl)cyclohexyl]piperidine Homologues at Dopamine-Uptake and Phencyclidine- and a-Binding Sites
The diverse binding properties of these compounds at the DA-uptake site and their spectrum of inhibitory activities for [3H]DA uptake identifies them as a useful base for the development of subtype selective probes at this site.
Synthesis and Analgesic Properties of New Modified Analogs of Phencyclidine with Specific Binding on PCP Receptor or Dopamine Inhibition Reuptake Activities
The obtained results indicated that all new synthesized drugs showed better activity in decreasing acute thermal and chemical pains in tail immersion and formalin tests compared to PCP and ketamine.
Synthesis and antinociception properties of phencyclidine derivatives with modified aromatic or cycloalkyl rings and amino group
New phenyl and thienyl analogues with specific affinity for the phencyclidine sites in NMDA receptors, dopamine uptake blocking, or both of them were synthesized and showed better activities to decrease acute thermal and chemical, but not chronic pains.
Differential Interaction of Phencyclidine‐Like Drugs with the Dopamine Uptake Complex In Vivo
The results imply that the pharmacological effects of PCP are due to its simultaneous interaction with the dopamine uptake complex and the PCP receptor, and TCP and MK‐801, which have the same behavioral properties as PCP, exert their action only through the interaction withThe PCP receptors.


Chemical synthesis and molecular pharmacology of hydroxylated 1-(1-phenylcyclohexyl-piperidine derivatives.
The most characteristic effects of hydroxylation of PCP on the cyclohexyl, piperidine, or phenyl moieties are the following: it generally decreases its activity in inhibiting [3H]PCP binding by a factor of 10 to 80, and it does not produce a large variation in the affinity for the morphine receptor.
A comparison between classes of drugs having phencyclidine-like behavioral properties on dopamine efflux in vitro and dopamine metabolism in vivo.
In vivo it was found that PCP, m-amino-PCP and PCE significantly elevated HAL-induced DA metabolism, whereas ketamine and m-nitro- PCP were without effect, and both levoxadrol and EKC significantly decreased the ratio of HVA/DA after HAL administration.
Effects of phencyclidine (PCP)-like drugs on turning behavior, 3H-dopamine uptake, and 3H-PCP binding
Antagonism of N-methyl-D-aspartate-induced transmitter release in the rat striatum by phencyclidine-like drugs and its relationship to turning behavior.
  • L. Snell, K. Johnson
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1985
It is concluded that turning is the result of nondopaminergic properties of the PCP-like drugs, based on previously reported studies of the dopaminergic Properties of these drugs.
Effects of phencyclidine, amphetamine and related compounds on dopamine release from and uptake into striatal synaptosomes.
PCP is less potent than amphetamine at releasing dopamine and may affect dopamine metabolism in the striatum primarily by inhibiting the reuptake of this catecholamine.
Specific [3H]phencyclidine binding in rat central nervous system.
  • S. Zukin, R. Zukin
  • Biology, Chemistry
    Proceedings of the National Academy of Sciences of the United States of America
  • 1979
[3H]PCP binding was most enriched in crude synaptosomal subcellular fractions, and was about three times higher in hippocampus than in cervical spinal cord, suggesting that PCP may exert its effects on the central nervous system via binding to specific brain receptor sites.
Binding characteristics of the dopamine uptake inhibitor [3H]nomifensine to striatal membranes.