where are cox 2 receptors found?
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The other cyclooxygenase, COX-2, also produces prostaglandins, but the COX-2 enzyme is located specifically in areas of the body that commonly are involved in inflammation but not in the stomach.
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These include meloxicam, nimesulide and etodolac. Nabumetone has also been referred to as a preferential inhibitor of COX-2, primarily on the basis of an invitro study suggesting that nabumetone's active metabolite may display preferential COX-2 inhibition; however, this claim has not been confirmed.
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Nociceptors are sensory receptors that detect signals from damaged tissue or the threat of damage and indirectly also respond to chemicals released from the damaged tissue. Nociceptors are free (bare) nerve endings found in the skin (Figure 6.2), muscle, joints, bone and viscera.
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On the other hand COX-2 is an inducible enzyme as it is produced under certain specific conditions like inflammation. Difference in Locations: COX-1 is commonly found in the kidney, stomach and platelets whereas COX-2 is located in macrophages, leukocytes and fibroblasts.
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By blocking the Cox-1 enzyme and disrupting the production of prostaglandins in the stomach, NSAIDs can cause ulcers and bleeding. Some NSAIDs have less effect on prostaglandins in the stomach than others, and, therefore, may have a lower risk of causing ulcers, but the increased risk of ulcers still exists.
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TRPV1 receptors are found mainly in the nociceptive neurons of the peripheral nervous system, but they have also been described in many other tissues, including the central nervous system. TRPV1 is involved in the transmission and modulation of pain (nociception), as well as the integration of diverse painful stimuli.
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Arachidonic Acid Metabolites (Prostaglandins and Related Compounds) Prostaglandins and related compounds (collectively referred to as prostanoids or eicosanoids) such as prostacyclin (PGI2), leukotrienes (LTs) and thromboxanes (TXs) are produced by many different cells in the body.
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Is Celebrex or Ibuprofen more effective? Celebrex is known as a selective COX-2 inhibitor. While it is still an NSAID like ibuprofen, Celebrex only blocks COX-2, as opposed to ibuprofen, which blocks both COX-1 and COX-2.
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Nonsteroidal anti-inflammatory drugs (NSAIDs). NSAIDs include over-the-counter options such as ibuprofen (Advil, Motrin IB, others) and naproxen sodium (Aleve), as well as more-powerful prescription NSAIDs such as indomethacin (Indocin) or celecoxib (Celebrex).
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Beta-agonists bind to the beta receptors on various tissues throughout the body. Beta-1 receptors are predominantly found in three locations: the heart, the kidney, and the fat cells. The beta-1 adrenergic receptor is a G-protein-coupled receptor communicating through the Gs alpha subunit.
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As the class name suggests, nonsteroidal antiinflammatory drugs (NSAIDs) reduce inflammation but are not related to steroids which also reduce inflammation. NSAIDs work by reducing the production of prostaglandins. Prostaglandins are chemicals that promote inflammation, pain, and fever.
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Alpha 1 receptors are the classic postsynaptic alpha receptors and are found on vascular smooth muscle. They determine both arteriolar resistance and venous capacitance, and thus BP. Alpha 2 receptors are found both in the brain and in the periphery. In the brain stem, they modulate sympathetic outflow.
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In many cases, these receptors are expressed on the target cell surface, but some receptors are intracellular proteins located in the cytosol or the nucleus. These intracellular receptors respond to small hydrophobic signaling molecules that are able to diffuse across the plasma membrane.
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Ulcers and NSAIDs. Peptic ulcer disease is a well-recognised complication of NSAID use. Inhibition of COX-1 in the gastrointestinal tract leads to a reduction of prostaglandin secretion and its cytoprotective effects in gastric mucosa. This therefore increases the susceptibility to mucosal injury.
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The α-2A and -2C subtypes are found mainly in the central nervous system. Stimulation of these receptor subtypes may be responsible for sedation, analgesia, and sympatholytic effects. The α-2B receptors are found more frequently on vascular smooth muscle and have been shown to mediate vasopressor effects.
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Eicosanoids typically are not stored within cells but rather synthesized as required. They derive from the fatty acids that make up the cell membrane and nuclear membrane.
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Receptor tyrosine kinases (RTKs) are enzyme-linked receptors localized at the plasma membrane containing an extracellular ligand-binding domain, a transmembrane domain, and an intracellular protein–tyrosine kinase domain.