Disease relevance of 3-[2-(phenethyl-propyl-amino)ethyl]phenol

• Long-lasting D2 receptor stimulation (8 days; 10 nM RU 24213) prevented this selective effect through activation of a pertussis toxin-sensitive G protein [1].

Psychiatry related information on 3-[2-(phenethyl-propyl-amino)ethyl]phenol

• When, for comparison, the D2 agonist, RU 24213 (0.1-20 mg/kg IP), was tested for PE, SY, motor activity and SB, it displayed a behavioural pattern very similar to that obtained with SND 919 [2].

High impact information on 3-[2-(phenethyl-propyl-amino)ethyl]phenol

• Prior incubation of rat anterior pituitary cells with 17beta-estradiol led to an almost complete reversal of the inhibitory effect of two dopamine agonists, dihydroergocornine and RU 24213, on both basal prolactin release and thyrotropin releasing hormone-induced prolactin release [3].
• In contrast, incubation with the D2 agonists [LY 171555, (+)-3-(3-hydroxyphenyl)-N-n-propylpiperidine, RU 24213] increased the soluble and decreased the particulate PKC activity [4].
• Topographical effects of 0.3 to 10.0 mg/kg RU 24213, primarily induction of sniffing and ponderous locomotion with accompanying reductions in rearing, grooming, sifting and chewing, were not altered to any material extent in DARPP-32-null mice [5].
• In contrast, quinpirole (1 mg/kg) and RU 24213 (3 mg/kg) produced more intense stereotypy consisting of rearing, sniffing and repetitive head movement in the two psychostimulant-treated groups than in the saline-treated group [6].
• In both the NAc and CPu, the inhibition of neurons produced by iontophoresis of the D2 receptor agonists quinpirole or RU-24213 was attenuated by acute DA depletion via the tyrosine hydroxylase inhibitor alpha-methyl-p-tyrosine (AMPT) [7].

Biological context of 3-[2-(phenethyl-propyl-amino)ethyl]phenol

• The rank order of potency was quinpirole (IC50 5 nM) greater than lisuride (IC50 8 nM) greater than RU 24213 (IC50 50 nM) greater than dopamine (IC50 200 nM) [8].
• Reduction in food intake were also produced in rats by the less potent, but selective, D-2 agonist RU 24213 (effective at 10.0 mg/kg), and by d-amphetamine (1.0 and 3.0 mg/kg) [9].

References