Lowering temperature increases cardiac muscarinic receptor site affinity towards agonists and antagonists

General Pharmacology
J W Wei, P V Sulakhe

Abstract

1. The effect of temperature on the binding of agonists and antagonists to cardiac muscarinic receptor sites was investigated. 2. Compared to 37 degrees C, carbachol-[3H]QNB and atropine-[3H]QNB competition curves were shifted to the left at lower temperatures. This was also observed with other agonists and antagonists. 3. Such an effect of temperature persisted in the N-ethylmaleimide (NEM)-and dithiothreitol (DTT)-treated membranes. 4. Dissociation of the membrane-bound [3H]QNB was higher at 37 degrees C 40% at 60 min) compared to 18 degrees C (approximately 20%). Both carbachol and atropine increased the dissociation at 37 degrees C to a similar maximum (to about 60%). 5. The results show marked temperature-dependent alterations in the cardiac muscarinic receptor sites and suggest that these occur either by direct action of the temperature on receptor conformation or its indirect action via membrane fluidity. The likely significance of these results is discussed.

References

Nov 1, 1979·Naunyn-Schmiedeberg's Archives of Pharmacology·J W Wei, P V Sulakhe
Apr 27, 1979·Biochemical and Biophysical Research Communications·C P BerrieE C Hulme
Jun 1, 1979·European Journal of Pharmacology·L B RosenbergerH I Yamamura
Dec 1, 1979·Naunyn-Schmiedeberg's Archives of Pharmacology·K H JakobsG Schultz
Mar 1, 1971·British Journal of Pharmacology·J D GrahamA Tai
May 30, 1980·Biochemical and Biophysical Research Communications·D Gurwitz, M Sokolovsky
Oct 31, 1980·European Journal of Pharmacology·N T PhanP V Sulakhe

❮ Previous
Next ❯

Citations

Nov 1, 1988·Immunopharmacology·L G CostaS D Murphy
Jan 1, 1987·Comparative Biochemistry and Physiology. C, Comparative Pharmacology and Toxicology·J E O'Shea
Apr 1, 1991·Journal of Autonomic Pharmacology·S A DarrochF Mitchelson

❮ 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.