| â‰¥98% (HPLC) |
| form || solid |
| color || off-white |
| solubility || DMSO: â‰¥10 mg/mL |
| || H2O: â‰¥2 mg/mL |
| Gene Information || human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816) |
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 (Â±)-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.
Features and Benefits
This compound is also offered as part of Sigmas Library of Pharmacologically Active Compounds (LOPACÂ®1280
), a biologically annotated collection of high-quality, ready-to-screen compounds.