Agonist and antagonist actions of (-)pindolol at recombinant, human serotonin1A (5-HT1A) receptors

Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology
A Newman-TancrediM J Millan

Abstract

It has been proposed that the arylalkylamine, (-)pindolol, potentiates the therapeutic action of antidepressant drugs in humans by blockade of 5-HT1A autoreceptors. Its interactions at human 5-HT1A receptors have not, however, been directly characterized. Herein, we demonstrate that (-)pindolol exhibits nanomolar affinity at human 5-HT1A receptors expressed in Chinese Hamster Ovary cells (CHO-h5-HT1A; Ki = 6.4 nmol/L). In a functional test of receptor-mediated G-protein activation (stimulation of [35S]-GTP gamma S binding) (-)pindolol displays an efficacy of 20.3% relative to the endogenous agonist, 5-HT (= 100%). (-)Pindolol also antagonizes 5-HT (100 nmol/L)-stimulated [35S]-GTP gamma S binding, reducing it to 19.8% of control binding. These data indicate that (-)pindolol acts as a (weak) partial agonist at CHO-h5-HT1A receptors and that it blocks the action of 5-HT at these sites.

Citations

Nov 25, 2005·Journal of Pharmacokinetics and Pharmacodynamics·Berangere GruwezMichel Tod
May 27, 2005·Life Sciences·Eduarda FernandesJosé L F C Lima
Jan 20, 2004·Neuroscience Letters·Kurt RasmussenElaine A Shanks
Jul 27, 2001·European Journal of Pharmacology·M J MillanD Cussac
Jun 22, 1999·European Journal of Pharmacology·E GurM E Newman
Mar 20, 2002·Pharmacology, Biochemistry, and Behavior·Mariusz PappConnie Sánchez
Jul 26, 2003·Journal of Affective Disorders·Per Plenge, Erling T Mellerup
May 8, 2001·Trends in Pharmacological Sciences·F ArtigasA Adell
Jan 26, 2000·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·H Yan, T Lewander
Oct 3, 2008·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Alain GobertMark J Millan
Feb 3, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Jean-Philippe GuillouxAlain M Gardier
Feb 24, 2001·Journal of Clinical Psychopharmacology·V PérezUNKNOWN Grup de Recerca en Trastorns Afectius
Dec 30, 2003·Human Psychopharmacology·Michael T IsaacAlan Tournoux
Dec 31, 2002·Journal of Receptor and Signal Transduction Research·Eva JerningNina Mohell
May 6, 2004·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Eugenii A RabinerPaul M Grasby
Feb 27, 2004·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·R Alexander BantickPaul M Grasby
Jul 18, 2020·The International Journal of Neuroscience·Burak Yaman, Ramazan Bal
Jun 30, 2005·European Journal of Pharmacology·Shaun JordanTetsuro Kikuchi

❮ 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.