Add time:08/17/2019         Source:sciencedirect.com

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-HT1A-receptor agonist 8-OH-DPAT 1 and 2 related phenolic phenylcyclopropylamine 4 and 5. The new compounds were assayed for 5-HT1A-receptor affinity and efficacy in vitro. Hybrids 6 and 7 were considered to be inactive but 8 had a Ki value of 130 nM for [3H]-8-OH-DPAT labelled 5-HT1A-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-HT1A-receptors. The results are discussed in relation to a previously described 3-D model for 5-HT1A-receptor agonists.

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