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8 relations: Agonist, Analgesic, Functional selectivity, G protein, Κ-opioid receptor, U-47700, U-50488, U-69,593.
Agonist
An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response.
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Analgesic
An analgesic or painkiller is any member of the group of drugs used to achieve analgesia, relief from pain.
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Functional selectivity
Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signalling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor.
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G protein
G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior.
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Κ-opioid receptor
The κ-opioid receptor (KOR) is a G protein-coupled receptor that in humans is encoded by the OPRK1 gene.
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U-47700
U-47700 is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of morphine in animal models.
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U-50488
U-50488 is a drug which acts as a highly selective κ-opioid agonist, but without any μ-opioid antagonist effects.
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U-69,593
U-69,593 is a drug which acts as a potent and selective κ1-opioid receptor agonist.
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