TRV734 is a drug developed by
Trevena Inc
Trevena Inc is a clinical stage biopharmaceutical company, headquartered in Chesterbrook, Pennsylvania, USA, and is involved in the discovery and development of G-protein coupled receptors (GPCR) biased ligands. Trevena was founded in 2007 with t ...
which acts as a biased agonist at the
μ-opioid receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical � ...
, selective for activation of the
G-protein
G proteins, also known as guanine nucleotide-binding proteins, are a family of proteins that act as molecular switches inside cells, and are involved in transmitting signals from a variety of stimuli outside a cell to its interior. Their act ...
signalling pathway over
β-arrestin 2
Beta-arrestin-2, also known as arrestin beta-2, is an intracellular protein that in humans is encoded by the ''ARRB2'' gene.
Members of arrestin/beta-arrestin protein family are thought to participate in agonist-mediated desensitization of G prot ...
recruitment. It is closely related to
oliceridine and has a similar pharmacological profile, but unlike oliceridine which has to be injected, TRV734 is suitable to be administered orally.
See also
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PZM21
PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain.
It is claimed to be a functionally selective μ-opioid receptor agonist which produces μ-opioid receptor mediated G protein signaling, with potenc ...
*
SHR9352
SHR9352 is a drug which acts as a potent and selective biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It was structurally derived from oliceridine by replacing ...
*
SR-17018
SR-17018 is a drug which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. In animal studies it produces analgesic effects but with less respiratory de ...
References
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Mu-opioid receptor agonists
Pyridines
Fluoroarenes
Spiro compounds
Oxygen heterocycles
Amines