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An animated view of the human κ-opioid receptor in complex with the antagonist JDTic. Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. [1] [2] [3] The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin ...
Activation of the μ-opioid receptor by an agonist such as morphine causes analgesia, sedation, slightly reduced blood pressure, itching, nausea, euphoria, decreased respiration, miosis (constricted pupils), and decreased bowel motility often leading to constipation. Some of these effects, such as analgesia, sedation, euphoria, itching and ...
Loperamide, sold under the brand name Imodium, among others, [1] is a medication of the opioid receptor agonist class used to decrease the frequency of diarrhea. [5] [4] It is often used for this purpose in irritable bowel syndrome, inflammatory bowel disease, short bowel syndrome, [4] Crohn's disease, and ulcerative colitis. [5]
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP for its ligand ketazocine, is a G protein-coupled receptor that in humans is encoded by the OPRK1 gene. The KOR is coupled to the G protein G i /G 0 and is one of four related receptors that bind opioid -like compounds in the brain and are responsible for mediating the ...
Salvinorin A, found naturally in the Salvia divinorum plant, is a kappa-opioid receptor agonist. [270] Tramadol and tapentadol, which act as monoamine uptake inhibitors also act as mild and potent agonists (respectively) of the μ-opioid receptor. [271] Both drugs produce analgesia even when naloxone, an opioid antagonist, is administered. [272]
Drugs known to be σ-agonists include cocaine, morphine/diacetylmorphine, opipramol, PCP, fluvoxamine, methamphetamine, dextromethorphan, and berberine. [citation needed] However, the exact role of σ-receptors is difficult to establish as many σ-agonists also bind to other targets such as the κ-opioid receptor and the NMDA glutamate receptor.
The endogenous system of opioid receptors is well known for its analgesic potential; however, the exact role of δ-opioid receptor activation in pain modulation is largely up for debate. This also depends on the model at hand since receptor activity is known to change from species to species.
An irreversible agonist is a type of agonist that binds permanently to a receptor through the formation of covalent bonds. [2] [3] A biased agonist is an agent that binds to a receptor without affecting the same signal transduction pathway. Oliceridine is a μ-opioid receptor agonist that has been described to be functionally selective towards ...