Cebranopadol

Cebranopadol
Clinical data
Other names	GRT-6005; GRT6005; PRK-101; PRK101; TRN-228; TRN228
Routes of; administration	Oral
Drug class	Non-selective opioid receptor agonist; μ-Opioid receptor agonist; Nociceptin receptor agonist; κ-Opioid receptor agonist; Opioid analgesic
Legal status
Legal status	Uncontrolled;
Pharmacokinetic data
Bioavailability	40%
Onset of action	4–6 hours (TmaxTooltip time to peak levels)
Elimination half-life	62–96 hours
Identifiers
	IUPAC name 6-fluoro-N,N-dimethyl-1'-phenylspiro[4,9-dihydro-3H-pyrano[3,4-b]indole-1,4'-cyclohexane]-1'-amine;
CAS Number	863513-91-1;
PubChem CID	11848225;
DrugBank	DB12830;
ChemSpider	29398942;
UNII	7GDW9S3GN3;
KEGG	D10436;
ChEBI	CHEBI:231222;
ChEMBL	ChEMBL2364605;
Chemical and physical data
Formula	C24H27FN2O
Molar mass	378.491 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN(C)C1(CCC2(CC1)C3=C(CCO2)C4=C(N3)C=CC(=C4)F)C5=CC=CC=C5;
	InChI InChI=1S/C24H27FN2O/c1-27(2)23(17-6-4-3-5-7-17)11-13-24(14-12-23)22-19(10-15-28-24)20-16-18(25)8-9-21(20)26-22/h3-9,16,26H,10-15H2,1-2H3; Key:CSMVOZKEWSOFER-UHFFFAOYSA-N;

Cebranopadol, also known by its developmental code names TRN-228 and formerly GRT-6005, is an experimental atypical opioid analgesic which is under development for the treatment of various types of pain as well as for treatment of substance-related disorders. It is taken orally.

Side effects of cebranopadol include nausea, vomiting, constipation, somnolence, euphoria, and respiratory depression, among others. The drug acts as a non-selective opioid receptor agonist, including as a dual μ-opioid receptor and nociceptin receptor full agonist and to a lesser extent as a κ-opioid receptor partial agonist. In relation to its multi-target profile, namely its nociceptin receptor agonism, cebranopadol shows atypical effects and certain potential advantages compared to selective μ-opioid receptor agonists like morphine, such as less misuse potential and respiratory depression. On the other hand, it has a long half-life in humans and still carries risk of misuse similarly to other opioids.

Cebranopadol was first described in the patent literature by 2002 and in the scientific literature by 2013. As of August 2025, it has completed multiple phase 3 clinical trials for treatment of pain. According to its developer, a New Drug Application (NDA) is to be submitted in the near future. As a dual μ-opioid and nociceptin receptor agonist, cebranopadol is a potential first-in-class medication. Cebranopadol is not yet a controlled substance as of 2022. It either has been encountered or could be encountered as a novel opioid recreational designer drug as of 2019.