| Description | This entry represents Neurokinin 1 (NK1) receptor that is involved in inflammation and pain transmission. It binds substance P, the first neuropeptide to be discovered in mammals. Neuropeptide receptors are present in very small quantities in the cell and are embedded tightly in the plasma membrane. The neuropeptides exhibit a high degree of functional diversity through both regulation of peptide production and through peptide-receptor interaction [ ]. The mammalian tachykinin system consists of 3 distinct peptides: substance P, substance K and neuromedin K. All possess a common spectrum of biological activities, including sensory transmission in the nervous system and contraction/ relaxation of peripheral smooth muscles, and each interacts with a specific receptor type.Biological functionality of substance P is mediated by its interaction with NK1 receptor, which is a member of GPCR family. In the brain, high concentrations of the NK1 receptor are found in striatum, olfactory bulb, dendate gyrus, locus coeruleus and spinal chord [ ]. In peripheral tissues NK1 receptors are found in smooth muscle (e.g., ileum and bladder), enteric neurons, secretory glands (e.g. parotid), cells of the immune system and vascular endothelium. NK1 receptors activate the phosphoinositide pathway through a pertussis-toxin-insensitive G-protein [].The rhodopsin-like GPCRs (GPCRA) represent a widespread protein family that includes hormone, neurotransmitter and light receptors, all of which transduce extracellular signals through interaction with guanine nucleotide-binding (G) proteins. Although their activating ligands vary widely in structure and character, the amino acid sequences of the receptors are very similar and are believed to adopt a common structural framework comprising 7 transmembrane (TM) helices [ , , ].G protein-coupled receptors (GPCRs) constitute a vast protein family that encompasses a wide range of functions, including various autocrine, paracrine and endocrine processes. They show considerable diversity at the sequence level, on the basis of which they can be separated into distinct groups [ ]. The term clan can be used to describe the GPCRs, as they embrace a group of families for which there are indications of evolutionary relationship, but between which there is no statistically significant similarity in sequence []. The currently known clan members include rhodopsin-like GPCRs (Class A, GPCRA), secretin-like GPCRs (Class B, GPCRB), metabotropic glutamate receptor family (Class C, GPCRC), fungal mating pheromone receptors (Class D, GPCRD), cAMP receptors (Class E, GPCRE) and frizzled/smoothened (Class F, GPCRF) [, , , , ]. GPCRs are major drug targets, and are consequently the subject of considerable research interest. It has been reported that the repertoire of GPCRs for endogenous ligands consists of approximately 400 receptors in humans and mice []. Most GPCRs are identified on the basis of their DNA sequences, rather than the ligand they bind, those that are unmatched to known natural ligands are designated by as orphan GPCRs, or unclassified GPCRs []. | Name | Neurokinin NK1 receptor |
| Short Name | NK1_rcpt | Type | Family |
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