(±)-PPHT hydrochloride 

Potent D₂ dopamine receptor agonist.

A series of new dopamine (DA) receptor agonists, of the 2-aminotetralin group, i.e. N-0434, N-0437 and N-0734 were investigated in both in vivo and in vitro pharmacological test systems. In vivo, the reversal of the gamma-butyrolactone-induced increase in rat central DOPA biosynthesis rate was taken as a measure of presynaptic activity. The homovanillic acid (HVA) decrease, after intraperitoneal and after oral administration of the drugs was also taken as a measure of presynaptic activity. Postsynaptic activity was measured in two behavioural models, i.e. reserpine reversal and stereotypy induction. The effects of (±)-PPHT (N-0434) these drugs on noradrenaline and dopamine turnover (alpha-MpT method) were studied in addition. The results indicate that all three compounds N-0434 ((±)-PPHT), N-0437 and N-0734 are potent and selective DA agonists that lack significant alpha 2 activity.

≥98% (HPLC)

solid

off-white

DMSO: ≥10 mg/mL

H₂O: ≥2 mg/mL

human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)

Seeman, P., et al., Dopamine D₂ receptor binding sites for agonists. A tetrahedral model. Mol. Pharmacol. 28, 391, (1985) abstract

Seiler, M.P., et al., Structure-activity relationships of dopaminergic 5-hydroxy-2-amino-tetralin derivatives with functional N-alkyl substituents. J. Med. Chem. 29, 912-917, (1986) abstract

Van der Weide, J. et al., , Pharmacological profiles of three new, potent and selective dopamine receptor agonists: N-0434, N-0437 and N-0734. Eur. J. Pharmacol. 125, 273-2Eur82, (1986)

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