neuropeptide Y receptor activity

Definition

Target type: molecularfunction

Combining with neuropeptide Y to initiate a change in cell activity. [PMID:9315606]

Neuropeptide Y receptors (NPYR) are G protein-coupled receptors (GPCRs) that mediate the biological effects of the neuropeptide Y (NPY) family of peptides. NPY is a highly conserved peptide that plays a wide range of physiological roles, including the regulation of appetite, stress response, anxiety, and blood pressure. NPYRs are expressed in various tissues and organs, including the brain, heart, liver, and adipose tissue. There are five known NPYR subtypes: Y1, Y2, Y4, Y5, and Y6, each exhibiting distinct pharmacological and functional properties. The molecular function of NPYR activity involves the following steps: 1. Binding of NPY to its receptor: NPY binds to the extracellular domain of the NPYR, triggering a conformational change in the receptor. 2. Activation of G protein: The conformational change in the receptor activates a heterotrimeric G protein, typically a Gαi/o protein. 3. Signaling cascade: The activated Gαi/o protein dissociates from the βγ subunits and interacts with downstream signaling molecules, such as adenylyl cyclase or phospholipase C. 4. Production of second messengers: The activated signaling molecules generate second messengers, such as cyclic AMP (cAMP) or inositol trisphosphate (IP3). 5. Cellular response: The second messengers trigger a variety of cellular responses, including changes in gene expression, ion channel activity, and enzyme activity. The specific cellular response depends on the NPYR subtype, cell type, and other factors. For example, activation of Y1 receptors typically inhibits adenylyl cyclase activity, leading to a decrease in cAMP levels and inhibition of neuronal firing. Y2 receptors, on the other hand, are known to couple to Gαi/o proteins and inhibit adenylyl cyclase and activate phospholipase C. This leads to a reduction in cAMP levels and an increase in IP3 levels, respectively. The activation of Y4 receptors, which are primarily expressed in the central nervous system, has been shown to reduce food intake and body weight. Y5 receptors are involved in the regulation of feeding behavior and have been implicated in obesity. Finally, Y6 receptors, which are mainly found in the periphery, play a role in the regulation of smooth muscle contraction. In summary, NPYR activity involves a complex cascade of events that ultimately leads to a wide range of physiological responses. Understanding the molecular function of these receptors is crucial for developing novel therapeutic strategies for a variety of disorders, including obesity, anxiety, and cardiovascular diseases.'
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Proteins (4)

Compounds (19)