Kappa-type opioid receptor
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions.
Database | Links |
---|---|
UniProt | P41145 |
PDB | 2A0D, 2IQN, 4DJH |
BioGrid | 111031 |
BindingDB | P41145 |
DrugBank | DB00921, DB00611, DB00907, DB00318, DB01209, DB00956, DB00327, DB00454, DB00370, DB00295, DB00844, DB00704, DB00497, DB00652, DB00647, DB00193 |
Guide to PHARMACOLOGY | 318 |
PharmGKB | PA31943 |
KEGG | hsa:4986 |
BioCyc | Not available |
Entrez Gene (GeneID) | 4986 |
Metric | Mean Value | Standard Deviation |
---|---|---|
AUC | 0.9528 | 0.0011 |
Accuracy | 0.9067 | 0.002 |
Sensitivity | 0.89 | 0.0021 |
Specificity | 0.9227 | 0.0031 |
BEDROC | 0.9812 | 0.0017 |
MCC Threshold | 0.496 | N/A |
MCC | 0.8119 | N/A |
F-score Threshold | 0.468 | N/A |
F-score | 0.9027 | N/A |