PMID: 3753738Jan 27, 1986Paper

Elevation of acetylcholine levels in striatum of rat brain by LY163502, trans-(-)-5,5a,6,7,8,9a,10-octahydro-6-propylpyrimido less than 4,5-g greater than quinolin-2-amine dihydrochloride, a potent and stereospecific dopamine (D2) agonist

Life Sciences
F P BymasterD T Wong

Abstract

LY163502, a partial ergoline and a trans-levorotatory enantiomer, does not stimulate adenylate cyclase in striatal membranes but inhibits 50% binding of 3H-apomorphine, 3H-pergolide and 3H-spiperone at 10, 13 and 151 nM (IC50), respectively. The racemic mixture (LY137157) is less effective, with 3, 2.7 and 1.4 times higher IC50 values, respectively, whereas the dextrorotatory isomer (LY175877) is inactive. LY163502 inhibits binding of 3H-clonidine with an IC50 value of 2600 nM, but not the binding of 3H-WB4101, 3H-dihydroalprenolol, 3H-serotonin, 3H-quinuclidinyl benzilate and 3H-pyramilamine or the uptake of serotonin, norepinephrine or dopamine, suggesting selective affinity toward dopamine receptors in vitro. Both LY163502 and LY137157 elevate striatal acetylcholine (Ach) levels. The elevation of Ach levels by LY163502 is reversed by dopamine antagonists haloperidol, cis-flupenthixol and metoclopramide. Therefore, the levorotatory enantiomer exhibits pharmacology of a D2 type of dopamine agonist.

References

Jan 11, 1979·Nature·J W Kebabian, D B Calne
Nov 15, 1974·Brain Research·P L McGeerE G McGeer
Mar 1, 1974·Brain : a Journal of Neurology·M J Aminoff, V Logue

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Citations

Jan 1, 1987·Journal of Neural Transmission·M M Foreman, J L Hall
Nov 21, 1989·European Journal of Pharmacology·C Sánchez
Sep 1, 1991·Neuropharmacology·S A Berry, G A Gudelsky
Mar 1, 1992·Pharmacology, Biochemistry, and Behavior·S M Pomerantz
Mar 9, 1999·Life Sciences·F P BymasterA Fink-Jensen
Feb 28, 2002·The European Journal of Neuroscience·Per Svenningsson, Catherine Le Moine
Jun 15, 2000·Journal of Neurochemistry·P SvenningssonB B Fredholm
Dec 1, 1991·British Journal of Pharmacology·A M Evans, K L Green
Nov 23, 2000·Journal of Medicinal Chemistry·C C FelderN DeLapp
Sep 1, 1991·Neurobiology of Aging·A M Murray, J L Waddington

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