Corpus ID: 26098777

RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane): central effects of a new dopamine receptor agonist.

  title={RDS-127 (2-di-n-propylamino-4,7-dimethoxyindane): central effects of a new dopamine receptor agonist.},
  author={Stephen Arneric and John Paul Long and M. Williams and David B. Goodale and James Mott and Joan M. Lakoski and Gerald F. Gebhart},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={224 1},
Apomorphine (APO), 2-di-n-propylamino-4,7-dimethoxyindane (RDS-127) and 2-di-n-propylamino-5,8-dimethoxytetralin (JMC-181) were examined on a variety of biochemical and pharmacological assays to determine their possible interaction with dopamine (DA) receptors. Nanomolar concentrations of all three compounds displaced [3H]APO from specific high-affinity binding sites in rat striatal membrane preparations, while higher concentrations were required to displace [3H]spiperone or [3H]rauwolscine… Expand
Derivatives of 4-(2-N,N-Di-n-propylaminoethyl)-5-hydroxyindole: Synthesis and Pharmacological Effects
5-Methoxy-l-methyl-4-(2-N,N-di-n-propylaminoethyl)indole (12) was synthesized from 5-hydroxyindole by a multistep synthesis, and all members of this indole-derived series showed a low order of cardiovascular activity, which appeared to be independent of dopamine receptors. Expand
Pharmacological profile of non-hydroxylated and ether derivatives of the potent D2-selective agonist N-0437
Derivatives of the potent dopamine D2-selective agonist 2-(N-propyl-N-2-thienylethylamino)-5-hydroxytetralin were designed, aimed at producing drugs with less sensitivity towards metabolic inactivation, and show the necessity of the 5-OH group for direct dopaminergic activity. Expand
Stimulation of presynaptic dopamine autoreceptors by 4-(2-di-n-propylaminoethyl) indole (DPAI).
The results of this study indicate that DPAI possesses a high degree of selectivity for presynaptic dopamine autoreceptors, and little or no effect on postsynaptic dopamine receptors. Expand
Assessment of the chloroethyl analog of 3-PPP (N-n-propyl-3-(3-hydroxyphenyl)-piperidine), 3-PPP-C1 as an irreversible ligand for central dopaminergic recognition sites.
N-Chloroethylation of 3-PPP reduced the intrinsic affinity of the agonist seven-fold and, consequently, in contrast to NCA, it was found that 3- PPP-C1 was not a good irreversible ligand at dopamine receptors. Expand
Synthesis and Evaluation of 2-(5-Methoxythiophen-3- yl)ethylamines as Potential Dopamine Agonists
Abstract The synthesis of 2-(5-methoxythiophen-3-yl)ethylamine and some derivatives bearing propyl and 2-phenylethyl substituents on the amino group has been described. The affinities for dopamine DExpand
Interaction of the component enantiomers of the putative dopamine autoreceptor agonist, TL-99 (6,7-dihydroxy-2-dimethylamino tetralin) with dopaminergic systems in mammalian brain and teleost retina
It is concluded that the apparent dopamine autoreceptor selectivity of TL-99 as assessed by in vivo animal test systems may be due partially to its α2-agonist activity. Expand
Effects of a novel dopamine-receptor agonist RDS-127 (2-N,N-di-n-propylamino-4,7-dimethoxyindane), on hormone levels and sexual behavior in the male rat
RDS-127 induced mounting in two thirds and intromissive and ejaculatory patterns in one third of the treated animals, 35 days postcastration, and suggests a neurochemical separation of these two components in the intact male rat. Expand
[Novel central dopaminergic agents derived from atypical di-substituted 2-aminoindane-4, 7. Synthesis and central pharmacological profile].
Results of the preliminary pharmacological evaluation show a centrally acting action through dopamine mechanisms, in which the compounds 10, 11, 13d-h and 14a showed responses as agonists, whereas compounds 14b-h, had responses as antagonists. Expand
An alternative approach to developing dopamine‐receptor agonists with central presynaptic actions following oral administration: A comparison between apomorphine, bromocriptine, and the novel compound RDS‐127 (2‐di‐n‐propylamino‐4,7‐dimethoxyindane)
RDS‐127 (2‐di‐n‐propylamino‐4,7‐dimethoxyindane) is a novel dopamine (DA) receptor agonist with potent central actions. RDS‐127, apomorphine (APO), and bromocriptine (BRM) were compared for theirExpand
Evidence that a novel dopamine receptor agonist, RDS‐127 [2−di‐n‐propylamino−4,7−dimethoxyindane] has some centrally mediated cardiovascular actions† †
The results suggest that RDS−127 activates central DA receptors to produce hypotension and bradycardia in rats, and that phentolamine was ineffective. Expand