Comparison of PNU-69176E analogs for their ability to enhance [3H]5-HT binding to 5-HT2C receptors in membranes from HEK293 cells expressing the receptor
Test ligands share the core head group α -d-galacto-octopyranoside, methyl-7-chloro-6,7,8-trideoxy-6-[(2-piperidinyl)carbonyl]amino group, but each has a different alkyl substitutent at the 4 position of the piperidinyl group, or shares the dodecanamide group but with different head groups attached at the amine group.
| Compounds | [3H]5-HT Binding | |
|---|---|---|
| Type of Alkyl Chains | % Change | |
| PNU-61734E | n-Butyl | -1 |
| PNU-62344E | n-Hexyl | +1 |
| PNU-62804E | t-Butyl | +1 |
| PNU-63502E | n-Propyl | 0 |
| PNU-65287E | Ethyl | +2 |
| PNU-67220E | n-Pentanoyl | -2 |
| PNU-68607E | Methyl | -4 |
| PNU-69176E | n-Undecyl | +393 |
| Type of Head Groups | ||
| PNU-8750 | N-(4-Acetoamido-1-naphthylsulfonyl) | +2 |
| PNU-33078 | N-[2-(Dimethylamino)ethyl]-N-methyl | 0 |
| PNU-43240 | N,N-diethyl | -32 |
| PNU-170158 | N-Phenyl | -8 |