Reverse intrinsic activity of antagonists on G protein-coupled receptors

Article Abstract:

Studies show that antagonists exhibit binding properties as well as promote conformational alteration in G protein-coupled receptor sites which leads to receptor-G protein separation. The introduction of guanine nucleotides increases the affinity of antagonists to coupled receptors. Moreover, the results have identified antagonists exhibiting null intrinsic and negative intrinsic activities. Additionally, extensive research on the physiological importance of G protein-linked receptors may provide better functional and biological understanding of antagonistic systems.

Guanine, Chemical inhibitors

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Melatonin receptors step into the light: cloning and classification of subtypes

Article Abstract:

Melatonin is a hormone secreted by the pineal gland in response to a variety of biological stimuli. Recent studies using 2-[125]iodomelatonin have identified high-affinity melatonin receptors in several vertebrate species. The G protein-coupled melatonin receptors were the first melatonin receptors identified using expression cloning. The second cloned receptor was designated the Mel1b receptor and Mel1a receptor as the third cloned receptor. Molecular and genetic studies have shown that these three receptor subtypes have a similar gene structure.

Melatonin

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In vivo regulation of intraneuronal trafficking of G protein-coupled receptors for neurotransmitters

Article Abstract:

G-protein-coupled receptors (GPCRs) are known to regulate the activity of neurotransmitters at the plasma membrane of neurones. In the nervous system, these GPCRs are believed to undergo complex changes in their subcellular localization and intracellular trafficking as they interact with the neurotransmitter environment. These events can be directly observed and examined with exquisite cellular and subcellular resolution using confocal microscopy and ultrastructural immunohistochemistry.

Cell membranes, Plasma membranes, Neurotransmitters, Neurotransmitter receptors, Immunohistochemistry

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