In vivo Schild regression analyses using nonselective 5-HT2C receptor antagonists in a rat operant behavioral assay

Ellen A WalkerSteven N Sterious


Although competitive antagonism experiments are critical tools in the classification of potential pharmacotherapies, no studies have quantitatively compared the potencies of 5-HT(2C) receptor antagonists using the Schild regression analysis in vivo. To evaluate the behavioral effects of 5-HT(2C) receptor agonists and antagonists, a series of nonselective 5-HT(2C) receptor antagonists, the 5-HT(2A/2C) receptor antagonist ketanserin, the 5-HT(2B) receptor antagonist SB 204,741, the 5-HT(2B/2C) receptor antagonist SB 200,646, and the peripherally acting 5-HT(2C) receptor antagonist RS102,221 were evaluated for their capacity to competitively antagonize the agonists MK212, mCPP, or BW723C86 in rats. Male Sprague-Dawley rats (N = 28) were trained to respond under a fixed ratio 10 schedule of food reinforcement. A multiple-trial, cumulative-dosing procedure was used to evaluate the capacity of the compounds to suppress response rates. MK212, mCPP, and the 5-HT(2B) receptor agonist BW723C86 dose-dependently decreased response rates. Only metergoline, mianserin, and methysergide produced a dose-dependent antagonism of the rate-decreasing effects of both mCPP and MK212. Apparent pA(2) analysis indicated that metergoline, mianserin, and ...Continue Reading


Jan 1, 1992·Life Sciences·R J Tallarida, R B Raffa
Jan 1, 1992·Life Sciences·D W RobertsonM L Cohen
Mar 1, 1988·Trends in Pharmacological Sciences·D Hoyer
Jan 1, 1986·Psychopharmacology·Kathryn A CunninghamJ B Appel
Jan 1, 1988·Journal of Receptor Research·D Hoyer
May 1, 1988·British Journal of Pharmacology·G A Kennett, G Curzon
Nov 1, 1980·Pharmacology, Biochemistry, and Behavior·G R Wenger
Mar 1, 1994·British Journal of Pharmacology·G A KennettT P Blackburn
Jan 1, 1996·Behavioural Brain Research·G S Baxter
Apr 23, 1997·European Journal of Pharmacology·Mark John MillanS Perrin-Monneyron
Apr 1, 1997·Neuropharmacology·D W BonhausR M Eglen
Aug 18, 2001·Pharmacology, Biochemistry, and Behavior·S P VickersG A Kennett
Dec 20, 2002·The Journal of Pharmacology and Experimental Therapeutics·Steven N Sterious, Ellen A Walker
Apr 24, 2003·Behavioral Neuroscience·Andrew C McCrearyKathryn A Cunningham
Sep 6, 2003·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·J De VryK R Jentzsch
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD
Apr 29, 2004·The Journal of Pharmacology and Experimental Therapeutics·Brian D SchlagJohn Dunlop

Related Concepts

Operant Conditioning
Dose-Response Relationship, Drug
Regression Analysis
Reinforcement Schedule
Serotonin Antagonists
Rats, Holtzman
Serotonin Agonists
Serotonin 5-HT2A Receptor Agonists
Serotonin 5-HT2A Receptor Antagonists

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.

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.

Pediculosis pubis

Pediculosis pubis is a disease caused by a parasitic insect known as Pthirus pubis, which infests human pubic hair, as well as other areas with hair including eye lashes. Here is the latest research.

Rh Isoimmunization

Rh isoimmunization is a potentially preventable condition that occasionally is associated with significant perinatal morbidity or mortality. Discover the latest research on Rh Isoimmunization 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. It also follows CRISPR-Cas9 approaches to generating genetic mutants as a means of understanding the effect of genetics on phenotype.

Enzyme Evolution

This feed focuses on molecular models of enzyme evolution and new approaches (such as adaptive laboratory evolution) to metabolic engineering of microorganisms. Here is the latest research.

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.

Pharmacology of Proteinopathies

This feed focuses on the pharmacology of proteinopathies - diseases in which proteins abnormally aggregate (i.e. Alzheimer’s, Parkinson’s, etc.). Discover the latest research in this field with this feed.

Alignment-free Sequence Analysis Tools

Alignment-free sequence analyses have been applied to problems ranging from whole-genome phylogeny to the classification of protein families, identification of horizontally transferred genes, and detection of recombined sequences. Here is the latest research.