Brain circuits for pain and its treatment
Pain is a multidimensional experience with sensory-discriminative, affective-motivational,
and cognitive-evaluative components. Pain aversiveness is one principal cause of suffering …
and cognitive-evaluative components. Pain aversiveness is one principal cause of suffering …
Neurobiology of addiction: a neurocircuitry analysis
GF Koob, ND Volkow - The Lancet Psychiatry, 2016 - thelancet.com
Drug addiction represents a dramatic dysregulation of motivational circuits that is caused by
a combination of exaggerated incentive salience and habit formation, reward deficits and …
a combination of exaggerated incentive salience and habit formation, reward deficits and …
Molecular recognition of morphine and fentanyl by the human μ-opioid receptor
Morphine and fentanyl are among the most used opioid drugs that confer analgesia and
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
unwanted side effects through both G protein and arrestin signaling pathways of μ-opioid …
Structure of the µ-opioid receptor–Gi protein complex
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most
clinically and recreationally used opioids. The induced positive effects of analgesia and …
clinically and recreationally used opioids. The induced positive effects of analgesia and …
Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists
Biased agonism at G protein–coupled receptors describes the phenomenon whereby some
drugs can activate some downstream signaling activities to the relative exclusion of others …
drugs can activate some downstream signaling activities to the relative exclusion of others …
[PDF][PDF] Bias factor and therapeutic window correlate to predict safer opioid analgesics
Biased agonism has been proposed as a means to separate desirable and adverse drug
responses downstream of G protein-coupled receptor (GPCR) targets. Herein, we describe …
responses downstream of G protein-coupled receptor (GPCR) targets. Herein, we describe …
Opioid analgesia and opioid-induced adverse effects: A review
AK Paul, CM Smith, M Rahmatullah, V Nissapatorn… - Pharmaceuticals, 2021 - mdpi.com
Opioids are widely used as therapeutic agents against moderate to severe acute and
chronic pain. Still, these classes of analgesic drugs have many potential limitations as they …
chronic pain. Still, these classes of analgesic drugs have many potential limitations as they …
Structural insights into µ-opioid receptor activation
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …
An endogenous opioid circuit determines state-dependent reward consumption
DC Castro, CS Oswell, ET Zhang, CE Pedersen… - Nature, 2021 - nature.com
Abstract µ-Opioid peptide receptor (MOPR) stimulation alters respiration, analgesia and
reward behaviour, and can induce substance abuse and overdose,–. Despite its evident …
reward behaviour, and can induce substance abuse and overdose,–. Despite its evident …
Opioid-induced hyperalgesia: cellular and molecular mechanisms
LA Roeckel, GM Le Coz, C Gavériaux-Ruff, F Simonin - Neuroscience, 2016 - Elsevier
Opioids produce strong analgesia but their use is limited by a paradoxical hypersensitivity
named opioid-induced hyperalgesia (OIH) that may be associated to analgesic tolerance. In …
named opioid-induced hyperalgesia (OIH) that may be associated to analgesic tolerance. In …