abstract |
Described herein are tryptamine analogs that display high binding affinity and selectivity for the 5-HT1Dβ receptor, of formula (I), wherein R1 represents a chain selected from C¿8-11?alkyl, C7-10alkoxy, C8-11alkanoyl and C7-10alkanoyloxy wherein said chain is optionally substituted by hydroxyl, C1-4alkyl or C1-4alkoxy and wherein one of the intervening carbons of said chain is optionally replaced with a heteroatom selected from oxygen, nitrogen and sulfur; R?2 and R3¿ each independently represent H or C¿1-3?alkyl; and R?4¿ represents H, C¿1-4?alkyl, aryl or arylC1-4alkyl. The compounds are useful as reagents for receptor identification and in receptor-based drug screening programs, and can also be used therapeutically to treat conditions for which administration of a 5-HT1D ligand is indicated, for example in the treatment of migraine. |