J. Vallgårda, L. Arvidsson, B. Svensson
1993
Citations
0
Influential Citations
5
Citations
Journal
European Journal of Medicinal Chemistry
Abstract
Abstract Three phenolic derivatives of 1,2-methano- N,N -dipropyl- 1,2,3,4-tetrahydronaphth-2-ylamine 6–8 were synthesized as structural hybrids of the potent 5-HT 1A -receptor agonist 8-OH-DPAT 1 and 2 related phenolic phenylcyclopropylamine 4 and 5 . The new compounds were assayed for 5-HT 1A -receptor affinity and efficacy in vitro . Hybrids 6 and 7 were considered to be inactive but 8 had a K i value of 130 nM for [ 3 H]-8-OH-DPAT labelled 5-HT 1A -receptors and produced an inhibition of the cAMP-production in the VIP-stimulated adenylyl cyclase assay. Thus, 8 is able to bind to and stimulate 5-HT 1A -receptors. The results are discussed in relation to a previously described 3-D model for 5-HT 1A -receptor agonists.