Tricyclic antidepressants: potent blockade of histamine H1 receptors of guinea pig ileum

European Journal of Pharmacology
J FiggeE Richelson

Abstract

Six tricyclic antidepressants were tested for their ability to antagonize histamine actions at histamine H1 receptors in a bioassay for these receptors (histamine-induced contractions of guinea pig ileum). All compounds were competitive antagonists with equilibrium dissociation constants in the range of 5.6 x 10(-11) M to 1.5 x 10(-7) M. Doxepin hydrochloride and amitriptyline hydrochloride were the most potent compounds of the series and may be the most potent antihistamines known. Antagonism at histamine H1 receptors by these compounds may explain their sedative effects.

References

Oct 3, 1980·European Journal of Pharmacology·J E Taylor, E Richelson
Jun 13, 1980·European Journal of Pharmacology·D DiffleyS H Snyder
Mar 26, 1981·European Journal of Pharmacology·H Hall, S O Ogren
Oct 28, 1983·European Journal of Pharmacology·S Kanba, E Richelson
Jan 21, 1986·European Journal of Pharmacology·M KornerJ C Schwartz
Oct 6, 1987·European Journal of Pharmacology·R RubinsteinS Cohen
Jan 1, 1987·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·S A BoschmansS E Terblanche
Dec 1, 1985·Journal of the American Academy of Dermatology·A LedoE Sendagorta
Jan 1, 1982·Progress in Neuro-psychopharmacology & Biological Psychiatry·G Kato, T Ban
Jan 13, 2001·Dermatologic Clinics·M W Greaves
Aug 5, 2000·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·C Ito
Apr 7, 2006·Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology·American College of Allergy, Asthma, & Immunology
Jun 1, 1996·Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology·E N Charlesworth
Sep 1, 1983·Clinical and Experimental Pharmacology & Physiology·J R NielsenL F Gram
Jan 1, 1990·Fundamental & Clinical Pharmacology·A FigueiredoF Teixeira
Feb 6, 1988·British Medical Journal·P C Newbold
Jan 1, 1981·Pharmacology & Therapeutics·M F Sugrue
Jun 18, 1984·Brain Research·S Kanba, E Richelson
Feb 1, 1985·British Journal of Pharmacology·J AcevesJ M Young
Feb 1, 1982·British Journal of Urology·K E Creed, A G Tulloch
Nov 29, 2005·The Medical Clinics of North America·Donald A Dibbern
Jan 1, 1981·Acta Psychiatrica Scandinavica. Supplementum·S O OgrenA L Renyi
Jan 1, 1981·Acta Psychiatrica Scandinavica. Supplementum·S O OgrenH Hall
Jun 30, 2012·Dermatologic Therapy·Christina Lam, Ruth Ann Vleugels
Mar 1, 2018·Pharmacological Reviews·Tobias AtkinGabriella Gobbi
Feb 12, 1998·The British Journal of Dermatology·R A SabroeC B Archer

Citations

Aug 1, 1977·European Journal of Pharmacology·F G van den Brink, E J Lien
Jan 1, 1977·Annual Review of Pharmacology and Toxicology·J C Schwartz
Dec 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·V T TranS H Snyder
Nov 23, 1978·The New England Journal of Medicine·L E Hollister
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

Related Concepts

Histamine Measurement
Receptors, Histamine H1
Cavia
Ileum
Contraction (Finding)
Smooth Muscle
Amitriptyline Hydrochloride
Antihistamines, Classical
Entire Ileum
Inotropism

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.