30341-94-7Relevant articles and documents
Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst1 receptor
Troxler, Thomas,Enz, Albert,Hoyer, Daniel,Langenegger, Daniel,Neumann, Peter,Pfaeffli, Paul,Schoeffter, Philippe,Hurth, Konstanze
, p. 979 - 982 (2008/09/18)
Non-peptidic compounds containing the octahydro-indolo[4,3-fg]quinoline (ergoline) structural element have been optimized into derivatives with high affinity (pKd r sst1 > 9) and selectivity (>1000-fold for h sst1 over h sst2-h sst5) for the somatostatin sst1 receptor. In functional assays, these ergolines act as antagonists at human recombinant sst1 receptors. Pharmacokinetic studies in rodents reveal good oral bioavailability and brain penetration for some of these compounds.
EPIMERIZATION OF ESTERS OF STEREOISOMERIC 8-ERGOLINECARBOXYLIC ACIDS ON CARBON C(8)
Benes, Jan,Cerny, Antonin,Miller, Vladimir,Kudrnac, Stanislav
, p. 1333 - 1340 (2007/10/02)
Esters of 8β-ergolinecarboxylic acids, I-XI, exposed to strong bases, such as lithium diisopropylamide, in polar aprotic solvents gave enolates, which were decomposed by suitable proton donors to a mixture of epimers.This contained, apart from the starting 8β-esters, the corresponding 8α-esters, Ia-IVa and VIa-XIa (65-80percent) and Va (about 16percent).Exposure of 8α-ester XIIa to these conditions produced epimerization on C(8) (about 54percent) and, to a small extent, isomerization on C(10), affording ester I(c. 1percent) and Ia (c. 5percent).