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Bicyclic and tricyclic ergoline partial structures. Rigid 3-(2-aminoethyl)pyrroles and 3- and 4-(2-aminoethyl)pyrazoles as dopamine agonists.
It is proposed, based upon comparisons with apomorphine, that the rigid pyrroleethylamine moiety of the ergolines is the portion of the molecule responsible for dopamine agonist activity. In supportExpand
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Elevation of acetylcholine levels in striatum of rat brain by LY163502, trans−(−)−5,5a,6,7,8,9a,10-octahydro-6-propylpyrimido〈4,5−g〉quinolin-2- amine dihydrochloride, a potent and stereospecific
Abstract LY163502, a partial ergoline and a trans-levorotatory enantiomer, does not stimulate adenylate cyclase in striatal membranes but inhibits 50% binding of 3 H-apomorphine, 3 H-pergolide and 3Expand
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Preclinical studies on quinelorane, a potent and highly selective D2-dopaminergic agonist.
Quinelorane (LY163502) has the endocrine, neurochemical and behavioral profile of a potent and highly selective D2-dopaminergic agonist. The administration of quinelorane produced dose-relatedExpand
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Resolution and absolute configuration of an ergoline-related dopamine agonist, trans-4,4a,5,6,7,8,8a,9-Octahydro-5-propyl-1H(or 2H)-pyrazolo[3,4-g]quinoline.
The title compound (+/-)-5 (R = Pro) (LY141865) has been resolved into a (-) isomer and a (+) isomer as the D- and L-tartrate salts, respectively. Biological studies have shown that dopamine agonistExpand
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Effects of (8beta)-8-[methylthio)methyl]-6-propylergoline on dopaminergic function and brain dopamine turnover in rats.
Abstract (8β)-8-[(Methylthio)methyl]-6-propylergoline induced contralateral turning in rats with nigrostriatal lesions, lowered serum prolactin in reserpinized rats, and caused stereotypedExpand
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Inhibition of prolactin secretion by ergolines.
Peptide-containing ergot alkaloids and synthetic ergoline derivatives were administered to reserpine-treated male rats in order to evaluate their prolactin-inhibiting properties. Each compound wasExpand
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Activity of 6-methyl-8-substituted ergolines against the 7,12-dimethylbenz(a)anthracene-induced mammary carcinoma.
The ability of a series of 8-beta-carboxamido ergolines, 8-formamido ergolines, and 8-methyl ergolines to cause regressions of established dimethylbenz[a]anthracene-induced mammary carcinomas wasExpand
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Binding of [3H]pergolide mesylate to dopamine receptors of mammalian brains.
The ergoline dopamine agonist, [3H]pergolide, binds with pharmacological specificity to particulate fractions of rat and calf brains. Dopamine agonists (apomorphine,Expand
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