1. Dear Drugs-Forum readers: We are a small non-profit that runs one of the most read drug information & addiction help websites in the world. We serve over 4 million readers per month, and have costs like all popular websites: servers, hosting, licenses and software. To protect our independence we do not run ads. We take no government funds. We run on donations which average $25. If everyone reading this would donate $5 then this fund raiser would be done in an hour. If Drugs-Forum is useful to you, take one minute to keep it online another year by donating whatever you can today. Donations are currently not sufficient to pay our bills and keep the site up. Your help is most welcome. Thank you.
    PLEASE HELP

Enantiospecific Synthesis and Pharmacological Evaluation of a Series of Super-Potent, Conformational

Enantiospecific Synthesis and Pharmacological Evaluation of a Series of Super-Potent, Conformational

  1. Guigz
    Heterocyclic nucleus 7 with N-trifluoroacetyl-protected D- or L-alanyl chloride, followed by ketone reduction and Ndeprotection.
    The enantiomers demonstrated modest stereoselectivity at the two receptors.
    Several general trends within these classes of new compounds were observed during their
    pharmacological investigation. For most pairs of optical isomers tested, the R-enantiomers of
    the compounds containing heterocycle 7 bound with only slightly higher affinity than their
    S-antipodes at the 5-HT2A and 5-HT2C receptors. Likewise, functional studies indicated that
    the R-enantiomers generally displayed increased potency compared to the S-enantiomers.
    Aromatization of the dihydrofuran rings of these arylalkylamines further increased affinity
    and potency. Only a few compounds were full agonists with most of them possessing intrinsic
    activities in the range of 60-80%. These compounds with a fully aromatic linear tricyclic nucleus are some of the highest-affinity ligands for the 5-HT2A receptor reported to date.