PMID: 9225298Apr 1, 1997

Functional and radioligand binding characterization of rat 5-HT6 receptors stably expressed in HEK293 cells

Neuropharmacology
Frank G BoessA J Sleight

Abstract

We have stably expressed the rat 5-HT6 receptor in HEK293 cells at a density of > 2 pmol/mg protein, as determined in equilibrium binding studies with [3H]-LSD and [3H]-5-HT and compared the affinity of a range of compounds in competition binding experiments with either [3H]-LSD or [3H]-5-HT as radioligand. A variety of tryptamine derivatives were tested and showed a significantly higher affinity when the 5-HT6 receptor was labelled with [3H]-5-HT, whereas ergoline compounds and several antagonists had higher affinities when [3H]-LSD was used as radioligand. Subsequently we examined the ability of LSD, 5-HT and a number of tryptamine derivatives to stimulate cAMP accumulation in order to determine their agonist potency and efficacy. We observed the following rank order of potency: LSD > omega-N-methyl-5-HT approximately bufotenine approximately 5- methoxytryptamine > 5-HT > 2-methyl-5-HT approximately 5-benzyloxytryptamine approximately tryptamine > 5-carboxamidotryptamine > > 5-HTQ. LSD, lisuride, 2-methyl-5-HT, tryptamine and 5-benzyloxytryptamine behaved as partial agonists relative to 5-HT. The rank order of potency of the tryptamine compounds correlated well with their affinities determined in binding assays. In addition, ...Continue Reading

References

Nov 17, 2001·European Journal of Pharmacology·F P BymasterM L Cohen
Jul 16, 2003·European Journal of Pharmacology·Jean Y ZhangJohn Dunlop
Aug 26, 1999·Neuropharmacology·N M Barnes, T Sharp
Aug 21, 2003·Progress in Neurobiology·Mark J Millan
Jul 13, 2000·Neuroscience Letters·N L Zhukovskaya, John F Neumaier
Apr 6, 1999·Schizophrenia Research·J H KrystalI L Petrakis
Jan 12, 1999·British Journal of Pharmacology·A BoursonA J Sleight
Aug 6, 2000·British Journal of Pharmacology·C RoutledgeD N Middlemiss
Dec 29, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Ellen S MitchellJohn F Neumaier
Jul 10, 2007·Schizophrenia Bulletin·John A Gray, Bryan L Roth
Aug 3, 2000·Alcoholism, Clinical and Experimental Research·F Chen, A J Lawrence
Feb 3, 1999·Annals of the New York Academy of Sciences·A J SleightA Bourson
Feb 3, 1999·Annals of the New York Academy of Sciences·Frank G BoessA J Sleight
Jun 3, 2000·Annual Review of Pharmacology and Toxicology·T A Branchek, T P Blackburn
Oct 29, 2010·Journal of Neurophysiology·Katherine C MurrayDavid J Bennett
Mar 3, 2007·Biological & Pharmaceutical Bulletin·Tohru Komada, Shingo Yano
Jan 1, 2012·Journal of Experimental Stroke & Translational Medicine·Shimin Liu, Jiang-Fan Chen
Jul 9, 2004·Drug Metabolism Reviews·Ai-Ming YuFrank J Gonzalez
Oct 23, 2013·Pharmacological Reports : PR·Magdalena Jastrzębska-WięsekAnna Wesołowska
Oct 23, 2010·Bioorganic & Medicinal Chemistry Letters·Jeff DeFalcoMatthew A J Duncton
Feb 1, 2008·European Journal of Pharmacology·Anna Wesołowska, Agnieszka Nikiforuk
Dec 26, 2006·Journal of Pharmacological and Toxicological Methods·Stanley P NawoschikXavier Khawaja
Jun 14, 2006·Journal of Pharmacological and Toxicological Methods·Gonzalo RomeroPetrus J Pauwels
Jan 5, 2011·Pharmacology, Biochemistry, and Behavior·Franco BorsiniTeresa Riccioni
Jul 21, 2016·Journal of Medicinal Chemistry·M Jesús Pérez de VegaRosario González-Muñiz
Mar 26, 2016·Progress in Neurobiology·Alexander WirthEvgeni Ponimaskin

Citations

Oct 1, 1992·European Journal of Pharmacology·A MansourH Akil
Jun 12, 1990·European Journal of Pharmacology·I van WijngaardenW Soudijn
Nov 1, 1988·Trends in Pharmacological Sciences·R Hitzemann
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Aug 1, 1983·Computer Programs in Biomedicine·G A McPherson
Nov 1, 1994·Synapse·S J Peroutka
Mar 1, 1993·Trends in Pharmacological Sciences·D A Craig

Related Concepts

Transfection
Tissue Membrane
Htr6
Receptors, Tryptamine
Triptans
Serotonin Agonists
Radioligand Assay
Serotonin Antagonists
HTR6
Poly(A) Tail

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.

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.

Synapse Loss as Therapeutic Target in MS

As we age, the number of synapses present in the human brain starts to decline, but in neurodegenerative diseases this occurs at an accelerated rate. In MS, it has been shown that there is a reduction in synaptic density, which presents a potential target for treatment. Here is the latest research on synapse loss as a therapeutic target in MS.

Artificial Intelligence in Cardiac Imaging

Artificial intelligence (ai) techniques are increasingly applied to cardiovascular (cv) medicine in cardiac imaging analysis. 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.

Social Learning

Social learning involves learning new behaviors through observation, imitation and modeling. Follow this feed to stay up to date on the latest research.

Cell Atlas of the Human Eye

Constructing a cell atlas of the human eye will require transcriptomic and histologic analysis over the lifespan. This understanding will aid in the study of development and disease. Find the latest research pertaining to the Cell Atlas of the Human Eye here.

Single Cell Chromatin Profiling

Techniques like ATAC-seq and CUT&Tag have the potential to allow single cell profiling of chromatin accessibility, histones, and TFs. This will provide novel insight into cellular heterogeneity and cell states. Discover the latest research on single cell chromatin profiling here.

Genetic Screens in iPSC-derived Brain Cells

Genetic screening is a critical tool that can be employed to define and understand gene function and interaction. This feed focuses on genetic screens conducted using induced pluripotent stem cell (iPSC)-derived brain cells.