title: 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.
abstract: NCA, the chloro analog of the potent dopamine agonist NPA is an irreversible ligand at dopamine receptors in mammalian brain. The chloroethyl analog of the recently described putative dopamine autoreceptor agonist 3-PPP, 3-PPP-C1, was evaluated for its potential use as an irreversible autoreceptor ligand. 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.
mesh_terms: D000818:Animals; D001060:Aporphines / Q000378:metabolism; D001921:Brain / Q000378:metabolism*; D066298:In Vitro Techniques; D008024:Ligands; D010880:Piperidines / Q000378:metabolism*; D051381:Rats; D011954:Receptors, Dopamine / Q000378:metabolism*
chemical_list: D001060:Aporphines; D008024:Ligands; D010880:Piperidines; D011954:Receptors, Dopamine; C025935:chloroethylnorapomorphine; C026539:preclamol