A new class of selective, non-basic 5-HT2A receptor antagonists.

Based on an existing series of 5-HT2A receptor ligands containing a basic nitrogen, we designed a non-basic lead that had reduced affinity for both the 5-HT2A receptor and the IKr potassium channel. The present paper describes the development of this lead to a novel series of non-basic piperidine sulfonamides and amides that have high affinity for the 5-HT2A receptor, whilst maintaining excellent selectivity over off target activities such as the IKr channel. This work has shown that the proposed pharmacophore model for the 5-HT2A receptor which suggests that a basic nitrogen is required for the binding of ligands is questionable.

St. John Ophthalmic Hospital. An ancient tradition of service revived in the Holy Land.

In Jerusalem in 1888, the Hospital of St. John was founded to combat the eye diseases prevalent in the Middle East. Since that time, this institution has survived world wars and local ones, and the geographic confusion created by redefinition of national borders.