3H]N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine ([3H]BTCP): a new phencyclidine analog selective for the dopamine uptake complex

European Journal of Pharmacology
J VignonR Chicheportiche

Abstract

A benzothiophenyl group instead of a phenyl ring on phencyclidine (PCP) yields a molecule N-[1-(2-benzo(b)thiophenyl)cyclohexyl]piperidine (BTCP), which is one of the more potent known dopamine (DA) uptake inhibitors (IC50 = 7 nM). This compound also has low affinity for the PCP receptor (K0.5 = 6 microM). The sodium-dependent [3H]BTCP binding to rat striatal membranes was investigated. [3H]BTCP bound to two different sites: one with very high affinity (Kd1 = 0.9 nM, Bmax1 = 3.5 pmol/mg protein) which paralleled the distribution of dopaminergic nerve endings and a second with lower affinity (Kd2 = 20 nM, Bmax2 = 7.5 pmol/mg protein). There was a good correlation between the abilities of drugs specific for the DA uptake complex and of PCP analogs to inhibit high affinity [3H]BTCP binding and [3H]DA synaptosomal uptake. This study also demonstrated that PCP interacts with the DA uptake site since it is a competitive inhibitor of high affinity [3H]BTCP binding. This site, however, is not the PCP receptor, which has a different pharmacological selectivity.

References

May 1, 1985·Pharmacology, Biochemistry, and Behavior·K M Johnson, L D Snell
Apr 15, 1985·Biochemical Pharmacology·M L Dubocovich, N R Zahniser
Sep 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·E H WongL L Iversen
Jul 30, 1982·European Journal of Pharmacology·J VignonM Lazdunski
Sep 1, 1981·Proceedings of the National Academy of Sciences of the United States of America·R QuirionC B Pert
Nov 28, 1983·Brain Research·J VignonM Lazdunski
Oct 1, 1983·Psychosomatics·G CaracciS Mukherjee
Aug 1, 1981·Neuropharmacology·M S LevineS H Butcher

❮ Previous
Next ❯

Citations

Jul 1, 1990·Journal of Neuroscience Research·T Maurice, J Vignon
Jan 1, 1990·Journal of Neural Transmission. General Section·B NaudinJ Costentin
Aug 3, 1989·European Journal of Pharmacology·P H Andersen
Jul 3, 1990·European Journal of Pharmacology·C RouillardA S Freeman
Mar 1, 1989·Pharmacology, Biochemistry, and Behavior·I ChaudieuR Chicheportiche
Dec 1, 1994·Pharmacology, Biochemistry, and Behavior·T MauriceA Privat
Nov 18, 1994·Brain Research. Developmental Brain Research·A P PatelM J Kuhar
Jan 1, 1990·Progress in Neurobiology·A S Horn
Nov 13, 2003·European Journal of Pharmacology·Jean-Jacques Bonnet
Dec 23, 1999·European Journal of Pharmacology·N S KulaJ L Neumeyer
Jul 19, 2000·Pharmacology, Biochemistry, and Behavior·R Martin-FardonF Weiss
Sep 3, 2002·Neuroscience and Biobehavioral Reviews·Tangui MauriceRae R Matsumoto
Jun 14, 2000·Progress in Neurobiology·I J MitchellM R Griffiths
Mar 19, 1999·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·A M RedmondB E Leonard
Jun 1, 1996·Drug and Alcohol Review·J M White, C F Ryan
Feb 1, 1991·Journal of Neurochemistry·T MauriceR Chicheportiche

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.