PMID: 12183652Aug 17, 2002Paper

Rapid desensitization of the serotonin(2C) receptor system: effector pathway and agonist dependence

The Journal of Pharmacology and Experimental Therapeutics
Brian D StoutKelly A Berg


The serotonin(2C) (5-HT(2C)) receptor couples to multiple effector mechanisms, including phospholipase A(2)-mediated arachidonic acid (AA) release and phospholipase C-mediated production of inositol phosphates (IP). Agonist relative efficacy differs depending upon which response (AA release or IP accumulation) is measured. In this study, we investigated the characteristics and agonist dependence of rapid desensitization of 5-HT(2C) receptor-mediated AA release and IP accumulation measured simultaneously from the same cell population. Pretreatment with 5-HT reduced the ability of a maximal concentration of 5-HT to elicit AA release and IP accumulation by about 60%; however, the AA response desensitized more rapidly (t(1/2) = 1.3 min) than the IP response (t(1/2) = 6.9 min). In addition, desensitization of the IP response was more sensitive (occurred at lower receptor occupancy levels) than the AA response. Moreover, in response to submaximal 5-HT concentrations, after an initial transient desensitization, the AA response was enhanced by up to approximately 250%. After maximal desensitization, both responses recovered, but recovery of the AA response was complete and faster than that for IP. Desensitization of both responses was ...Continue Reading


Feb 1, 1992·Pharmacology, Biochemistry, and Behavior·J L Mueller, R M Quock
May 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·J L BenovicRobert J Lefkowitz
Jul 1, 1995·Trends in Pharmacological Sciences·T Kenakin
Mar 1, 1994·Neuropharmacology·F G Boess, I L Martin
Nov 1, 1996·Trends in Pharmacological Sciences·T T ChuangA De Blasi
Nov 20, 1997·The Journal of Biological Chemistry·Y YuJ B Wang
Aug 15, 1998·Trends in Pharmacological Sciences·William P Clarke, R A Bond
Aug 12, 1999·European Journal of Pharmacology·H Zhong, K P Minneman
Sep 21, 2001·British Journal of Pharmacology·Kelly A BergWilliam P Clarke


Feb 19, 2005·Psychopharmacology·Aska HayashiKeiji Miyata
Oct 19, 2004·Journal of Affective Disorders·Brian M RossIain Glen
Aug 21, 2003·Progress in Neurobiology·Mark J Millan
Nov 14, 2003·Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology·Cornelia WagnerJohn A Oaks
Jul 27, 2007·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Paul J FletcherGuy A Higgins
Apr 5, 2005·The Journal of Pharmacology and Experimental Therapeutics·Stuart MaudsleyLouis M Luttrell
Jun 12, 2010·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Stephen A SchepelKlaus W Beyenbach
Jan 25, 2013·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Noelle C AnastasioKathryn A Cunningham
Jun 2, 2012·Expert Opinion on Drug Discovery·Wayne StallaertMichel Bouvier
Dec 25, 2010·Trends in Molecular Medicine·Erin J WhalenRobert J Lefkowitz
Jul 17, 2007·Trends in Pharmacological Sciences·Barbara Bosier, Emmanuel Hermans
Dec 7, 2007·British Journal of Pharmacology·E KellyG Henderson
Jun 29, 2006·The Journal of Pharmacology and Experimental Therapeutics·Jonathan D UrbanRichard B Mailman
Mar 24, 2005·Molecular Pharmacology·William P Clarke
Sep 21, 2020·Reviews in the Neurosciences·Sumaira KhanDivya Vohora
Aug 8, 2018·The International Journal of Neuropsychopharmacology·Kelly A Berg, William P Clarke
Jan 29, 2019·European Journal of Pharmacology·Daniel E FelsingRaymond G Booth

Related Concepts

Type C Phospholipases
Phospholipases A
Receptors, Tryptamine
Serotonin Antagonists
Signal Transduction
Chinese Hamster Ovary Cell
Serotonin Agonists

Trending Feeds


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.

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.

Lipidomics & Rhinovirus Infection

Lipidomics can be used to examine the lipid species involved with pathogenic conditions, such as viral associated inflammation. Discovered the latest research on Lipidomics & Rhinovirus Infection.

Alzheimer's Disease: MS4A

Variants within the membrane-spanning 4-domains subfamily A (MS4A) gene cluster have recently been implicated in Alzheimer's disease in genome-wide association studies. Here is the latest research on Alzheimer's disease and MS4A.

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.

Torsion Dystonia

Torsion dystonia is a movement disorder characterized by loss of control of voluntary movements appearing as sustained muscle contractions and/or abnormal postures. Here is the latest research.

Generating Insulin-Secreting Cells

Reprogramming cells or using induced pluripotent stem cells to generate insulin-secreting cells has significant therapeutic implications for diabetics. Here is the latest research on generation of insulin-secreting cells.

Central Pontine Myelinolysis

Central Pontine Myelinolysis is a neurologic disorder caused most frequently by rapid correction of hyponatremia and is characterized by demyelination that affects the central portion of the base of the pons. Here is the latest research on this disease.

Epigenome Editing

Epigenome editing is the directed modification of epigenetic marks on chromatin at specified loci. This tool has many applications in research as well as in the clinic. Find the latest research on epigenome editing here.