Drug intelligence / Profile preview

pukateine

Development stage
Preclinical
Modality
Small Molecules
Administration
Topical (traditional Use), Research Use: Not Established For Systemic Human Use
01

Overview

**Pukateine** is a natural aporphine alkaloid found in the bark of the New Zealand tree *Laurelia novae-zelandiae* ("Pukatea"), traditionally used in Māori herbal medicine as an analgesic[3][1]. Its chemical structure is \((R)-11\)-hydroxy-1,2-methylenedioxyaporphine (C\(_{18}\)H\(_{17}\)NO\(_3\)), a pentacyclic molecule with a benzylisoquinoline backbone and aporphine ring system[2][4][5]. Mechanistically, pukateine acts as a **dopamine receptor agonist** (targeting both D1 and D2 subtypes) with submicromolar IC50 values, increases extracellular dopamine, and demonstrates antioxidant properties by inhibiting lipid peroxidation[1]. It does **not inhibit monoamine oxidase** at pharmacologically relevant concentrations[1]. Its primary indication is analgesia (pain relief), though modern development remains investigational.

Other names
(-)-pukateinepukateine, (-)-(R)-11-hydroxy-1,2-methylenedioxyaporphine(12R)-11-methyl-3,5-dioxa-11-azapentacyclo[10.7.1.0²,⁶.0⁸,²⁰.0¹⁴,¹⁹]icosa-1(20),2(6),7,14(19),15,17-hexaen-18-ol5H-benzo(g)-1,3-benzodioxolo(6,5,4-de)quinolin-12-ol, 6,7,7a,8-tetrahydro-7-methyl-, (7aR)-N-methyl-11-hydroxy-1,2-methylenedioxyaporphineCAS 81-67-4CAS81-67-4CAS-81-67-4
02

Targets

DRD1 (Dopamine D1 Receptor)DAT (Dopamine plasma membrane transport protein)DRD2 (Dopamine D2 Receptor)

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