General Information of DBT (ID: ET03SPZ)
Name
Opioid receptor kappa (OPRK1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Kappa opioid receptor; Kappa-type opioid receptor; K-OR-1; KOR; KOR-1; OPRK
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name OPRK1 Gene ID
4986
UniProt ID OPRK_HUMAN (click to find more protein-related data of this DBT)
TTD ID T60693 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
Function
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.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Simethicone Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antifoaming agent; Diluent; Water-repelling agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 155 nM (estimated based on the structural similarity with CHEMBL1707 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.942028986
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRK_HUMAN
References
1 From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. J Med Chem. 2001 Oct 11; 44(21):3378-90.

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