(±)-PPHT hydrochoride is a 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.
Potent D2 dopamine receptor agonist.
Code de la classe de stockage
13 - Non Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Équipement de protection individuelle
Eyeshields, Gloves, type N95 (US)
Faites votre choix parmi les versions les plus récentes :
We report the synthesis and pharmacological characterization of novel fluorescently labeled ligands with high affinity and specificity for D1 and D2 dopamine receptors. D1-selective antagonist probes have been synthesized using (R,S)-5-(4'-aminophenyl)-8-chloro-2,3,4,5-tetrahydro-3-methyl-[1H]-3- benzazepin-7-ol, the 4'-amino derivative of the high affinity D1-selective
Naunyn-Schmiedeberg's archives of pharmacology, 336(5), 487-493 (1987-11-01)
The affinity of a series of N,N-disubstituted 2-aminotetralins for the rat striatal D2 dopamine receptor labelled by [3H]spiperone has been determined. Displacement data for the more potent 2-aminotetralins were better described by a model where the compounds competed for [3H]spiperone
European journal of pharmacology, 344(2-3), 223-229 (1998-05-26)
Effects of dopamine and (+/-)-2-(N-phenylethyl-N-propyl)amino-5-hydroxy-tetralin hydrochloride (N-0434), a dopamine D2 receptor agonist, in the presence of prazosin on the ATP- and acetylcholine-induced contraction were investigated in the guinea-pig vas deferens in order to test for the existence of postsynaptic dopamine
The Journal of pharmacology and experimental therapeutics, 284(2), 542-548 (1998-03-07)
Dopamine influences the release of neurohypophysial peptides in vivo. However, the extent to which this effect is caused by a direct dopaminergic action within the neurohypophysis remains unclear. With use of the patch-clamp technique on thin slices of rat posterior
In order to develop a model for the putative binding sites between the D2 dopamine receptor and many of its agonists, we obtained the dissociation constants of many dopaminergic agonists at the high affinity state, D2high, as well as at
Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..
