Drug intelligence / Profile preview

PEPAP

Development stage
Unknown
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Intravenous, Inhalation, Intranasal
01

Overview

PEPAP (1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine) is a synthetic opioid analgesic and an analogue of meperidine (pethidine). It was first discovered by Janssen in 1960. Structurally related to desmethylprodine (MPPP), PEPAP features an N-phenethyl group instead of the N-methyl group found in MPPP and has an acetate ester rather than a propionate. It is approximately six to seven times more potent than morphine in animal studies. Like other opioids, it produces effects such as analgesia, sedation, euphoria, and can cause side effects including itching, nausea, and potentially life-threatening respiratory depression. PEPAP acts primarily as a mu-opioid receptor agonist but is also noted to be a CYP2D6 inhibitor with potential for drug interactions. There are no approved medical uses for PEPAP; it has been sold illicitly as "synthetic heroin" and is classified as a Schedule I controlled substance due to its high abuse potential and lack of accepted safety or medical use[1][2][3][4][5].

Other names
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidinephenethylphenylacetoxypiperidine4-piperidinol 1-phenethyl-4-phenyl acetate
02

Targets

MOR (Mu opioid receptor)

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