62033-50-5

Upstream product

• 79412-27-4 (+/-)-3-PPP hydrobromide 
• 62033-61-8 3-(3,4-dimethoxyphenyl)-1-propylpiperidine 
• 89980-69-8 3,4-dimethoxyphenylmagnesium bromide 
• 62033-62-9 N-propionyl-3-(3',4'-dimethoxyphenyl)-piperidine 
• 79445-45-7 3-(3,4-Dimethoxyphenyl)pyridine 
• 62033-58-3 3-(3,4-dimethoxy-phenyl)-piperidine 
• 626-55-1 3-Bromopyridine 

Relevant academic research and scientific papers

In-vitro and in-vivo metabolism of the presynaptic dopamine agonist 3-PPP to a catecholic analogue in rats

The dopamine agonist 3-PPP and its enantiomers are hydroxylated in-vitro by rat liver microsomes to the catecholamine 3-(3,4-dihydroxyphenyl)-N-n-propylpiperidine (4-OH-3-PPP) with K(m) and V(max) values of about 1 μM and 2 nmol (mg protein)-1 min-1 respectively. As the catecholamine formed appears to be a good substrate for catechol-O-methyltransferase, in-vivo catecholamine formation in rats from 3-PPP was only detectable after inhibition of COMT by tropolone. The resulting brain levels of 4-OH-3-PPP, as measured by HPLC with electrochemical detection 45 min after administration, were about 350 pmol g-1 after i.p., and about 100 pmol g-1 after s.c. injection of 45 μol kg-1 3-PPP, with no significant difference between racemic, (+) or (-) 3-PPP. It was estimated that these catecholamine levels represent about 1-5% of the 3-PPP levels after i.p., and about 0.2-0.5% after s.c. administration of 3-PPP. The relevance of this metabolic conversion of 3-PPP for its pharmacological profile is discussed.

3-Phenylpiperidines. Central Dopamine-Autoreceptor Stimulating Activity

Thirty compounds related to the selective dopamine-autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine have been synthesized and tested for central dopamine-autoreceptor stimulating activity.The 3-(3-hydroxyphenyl)piperidine moiety seems indispensable for high potency and selectivity.Introduction of an additional hydroxyl group into the 4-position of the aromatic ring gives a compound with dopaminergic activity but lacking selectivity for autoreceptors. 3-(3-Hydroxyphenyl)-N-n-propylpyrrolidine, 3-(3-hydroxy)-N-n-propylperhydroazepine, and 3-(3-hydroxyphenyl)quinuclidine were all inactive.The most potent compounds were the N-isopropyl-, N-n-butyl-, N-n-pentyl-, and N-phenethyl-substituted 3-(3-hydroxyphenyl)piperidine derivatives.None of the compounds investigated seemed to have central noradrenaline- or serotonin-receptor stimulating activity.

3-(3',4'-Disubstituted) phenyl piperidines

Novel phenyl piperidines of the formula STR1 wherein X is selected from the group consisting of hydrogen and acyl of an aliphatic carboxylic acid of 2 to 6 carbon atoms and R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, alkenyl o