PMID: 9423932Jan 10, 1998Paper

Labelling of CRF1 and CRF2 receptors using the novel radioligand, [3H]-urocortin

Neuropharmacology
J GottowikG J Kilpatrick

Abstract

The binding of the novel radioligand, [3H]-rat urocortin to homogenates of rat cerebellum and homogenates of cells stably transfected with the human CRF1, rat CRF2alpha and rat CRF2beta receptors was examined. In each case, specific reversible high affinity binding was observed (K[d]s between 0.18 and 0.31 nM). The density of sites was relatively low in the cerebellum (9 fmol/mg tissue) but high in the recombinant systems with expression levels of between 1.4 and 6.3 pmol/mg protein. Agents known to interact with CRF receptors potently competed for binding in each case. The pharmacological profile of binding to the recombinant receptors were consistent with data previously published using other radioligands. Thus, for the recombinant CRF1 receptor, binding was inhibited with similar affinity by Urocortin, sauvagine, Urotensin 1 and CRF. The non-peptidic CRF antagonists (e.g. CP 154,526 and SC 241) also potently inhibited binding. The CRF2alpha and CRF2beta receptor recombinant systems had a very similar pharmacological profile with a clear rank order of potency for the peptide ligands (Urocortin > Sauvagine > Urotensin 1 > CRF), whereas the non-peptide CRF receptor antagonists had no measurable affinity. The pharmacological pro...Continue Reading

References

Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Oct 1, 1993·Proceedings of the National Academy of Sciences of the United States of America·R ChenW W Vale
Mar 28, 1995·Proceedings of the National Academy of Sciences of the United States of America·M PerrinW Vale
Jan 31, 1995·Proceedings of the National Academy of Sciences of the United States of America·T W LovenbergT Oltersdorf
Sep 1, 1996·Endocrinology·C J DonaldsonW W Vale
Sep 17, 1996·Proceedings of the National Academy of Sciences of the United States of America·D W SchulzJ Heym
Apr 1, 1996·Trends in Pharmacological Sciences·D T ChalmersE B De Souza

❮ Previous
Next ❯

Citations

Oct 18, 2000·European Journal of Pharmacology·G N Smagin, A J Dunn
May 30, 1998·Journal of Neuroscience Methods·A ArdatiG J Kilpatrick
May 5, 2001·Peptides·F M DautzenbergJ Moreau
Jan 12, 2000·Molecular and Cellular Endocrinology·B K BrarD S Latchman
Oct 13, 2001·Trends in Cardiovascular Medicine·D S Latchman
Oct 30, 2016·Trends in Neurosciences·Indira NederpeltLaura H Heitman
Apr 13, 1999·The Journal of Clinical Endocrinology and Metabolism·F PetragliaW Vale
Feb 22, 2003·CNS Drug Reviews·Patricia A SeymourDavid W Schulz
Jun 22, 2007·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Ariadne LegendreRuth B S Harris
Dec 23, 1998·Proceedings of the National Academy of Sciences of the United States of America·A RühmannJ Spiess
Jun 18, 2002·American Journal of Physiology. Endocrinology and Metabolism·Alison C HollowayJohn R G Challis
Mar 18, 2000·The Journal of Biological Chemistry·B K BrarD S Latchman
Oct 18, 2000·Regulatory Peptides·K H SkeltonC B Nemeroff

❮ 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.