Drug intelligence / Profile preview

R-30490

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
01

Overview

R-30490 is a synthetic opioid analgesic structurally related to carfentanil and fentanyl. It was first synthesized by Janssen Pharmaceutica during structure–activity relationship studies of fentanyl analogues. R-30490 is notable for being the most selective agonist for the mu-opioid receptor among tested fentanyl derivatives, exhibiting extremely high potency—only slightly less than carfentanil. Despite its pharmacological activity, it has never been introduced for medical use in humans; its primary application has been as an animal tranquilizer and in research settings. Like other potent opioids in this class, side effects include itching, nausea, and potentially life-threatening respiratory depression[1][2][3][8].

Other names
4-methoxymethylfentanylN-(4-(methoxymethyl)-1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide
02

Targets

MOR (Mu opioid receptor)

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