Synthesis and dopamine receptor affinities of 6-amino-5,6,7,8-tetrahydroquinoline derivatives

Some N,N-dialkyl derivatives of 6-amino-5,6,7,8-tetrahydroquinoline were synthesized. The affinity of new compounds for dopamine binding sites was measured in a test involving displacement of [ 3H]SCH 23390 (D-1 selective) and [ 3H]spiperone (D-2 selective) from homogenized rat striatal tissue. While no compound was effective in displacing [ 3H]SCH 23390, in the binding assays on the D-2 receptor all tetrahydroquinolines displaced [ 3H]spiperone from specific binding sites, the compounds with a N-n-propyl-N-phenylethylamino group or N,N-di n-propylamino group being the most potent

On local Morse theory for p-area functionals, p > 2

This survey article deals with some Morse theoretic aspects for functionals defined in Sobolev Banach spaces, associated with quasilinear elliptic equations or systems, involving the p-Laplace operator, p > 2.We discuss the notion of nondegeneracy in a Banach (not Hilbert) variational framework and we present some developments concerning the critical groups estimates and the interpretation of the multiplicity of a critical point

Synthesis and preliminary pharmacological evaluation of 5-hydroxy-and 5,6-dihydroxy-1,2,3,7,12,12a-hexahydrobenzo [5,6]cycloheptal [1,2,3-ij]isoquinoline derivatives as dopamine receptor ligands

A series of 5-hydroxy- and 5,6-dihydroxy- 1,2,3,7,12,12a-hexahydrobenzo[5,6]cyclohepta[1,2,3-iJ]isoquinoline derivatives (5a-e and 6a-e) were synthesized as conformationally rigid analogues of 1-benzyltetrahydroisoquinoline and evaluated for their affinity at D-1 and D-2 dopamine receptors. All compounds showed lower D1 and D affinities than dopamine. The 5-hydroxy-1-methyl-2,3,12,12a-hexahydrobenzo[5,6]cyclohepta[1,2,3-ij] 5a and the 5,6dihydroxy analogue 6a showed D-2 agonist activity. This was proved by their effects on prolactin release from primary cultures of rat anterior pituitary cells. Molecular modeling studies showed that the geometric parameters (namely the distances from meta and para hydroxyl oxygens to the nitrogen and the height of nitrogen from the hydroxylated phenyl ring plane) of the dopaminergic pharmacophore embedded in our compounds have lower values in comparison with those observed in D-1 and D-2 selective ligands. (C) 2001 Elsevier Science Ltd. All rights reserved

Per una storia dell'Universit\ue0 di Macerata

Sezione monografica del fascicolo n. 13 della rivista "Annali di storia delle universit\ue0 italiane" (CISUI)E 183532 Codice ISI: 1127-825