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Papers of the Week
TRV130 partial agonism and capacity to induce antinociceptive tolerance revealed through reducing available μ opioid receptor number.
Abstract
β-arrestin2 recruitment to μ receptors may contribute to the development opioid analgesics side effects. This possibility led to the development of TRV130 and PZM21, opioids reportedly biased against β-arrestin2 recruitment in favour of G protein signalling. However, low efficacy for β-arrestin2 recruitment by TRV130 and PZM21 may simply reflect partial agonism overlooked due to the overexpression of μ receptors.