Receptors and Second Messengers
Summary :
Table of Contents
- Introduction
- A powerful tools of molecular biology
- Receptor population for peptides
- Neuropeptide and second messenger signal transduction systems
- Peptidases
- Description
- The metabolism of TRH
- Neuroendocrine secretion
- The peptides involved in neuroendocrine regulation
- Regional differences in CRF receptor regulation
- Neuropeptides in psychiatric disorders
- Neuropeptide research
- Alzheimer's disease
- The CRF-containing interneurons of the cortex
- Mood disorders
- Somatostatin
- Thyrotropin releasing hormone
- Conclusion
- References
Abstract
Neuropeptide receptors have undergone the same process of discovery and characterization that receptors for other neurotransmitters have enjoyed. The process begins with the pharmacological characterization of the receptor's physicochemical binding properties by assessing the affinity of various metabolically derived and synthetic peptide fragments, and the native molecule, for the receptor binding site found in membrane preparations. Peptide receptor locations are mapped with radioactive or fluorescent tags that are inserted into peptide molecules, which often contain substituted amino acids at the most vulnerable peptidase cleavage sites. Previously, once the peptide receptor was characterized pharmacologically, it was usually purified from some relatively enriched biological tissue source or brain region by affinity column chromatography. After it had been purified, binding parameters and activity were recharacterized for the reconstituted purified receptor protein and structural information obtained by X-ray crystallography. This process was closely followed in the purification of the neurotensin-neuromedin N receptor.
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