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Galanin in Alzheimer Disease
Table 5.
GALR Subtype Specific Ligands
| GAL liganda | GALR subtype specificity | IC50 |
|---|---|---|
| a References in parentheses b GALNON is presently the only systemically active GALR agonist. | ||
| AR-M1896 | GALR2 agonist | 1.76 nM (rat GALR2) |
| GAL(2–11)-NH2(142) | 879 nM (hGALR1) | |
| AR-M961 | GALR1 agonist | 1.74 nM (hGALR1) |
| [Sar(1), D-Ala12 ]Gal(1–16)-NH2(142) | GALR2 agonist | 403 pM (rat GALR2) |
| Sch202596 | GALR1 antagonist | 1.7 μ M (hGALR1) |
| Spirocoumaranon(153 , 155) | ||
| PS 766257 | hGALR1 agonist | Not reported |
| Structure unknown(154) | ||
| RWJ-57408 | hGALR1 antagonist | |
| dithiepin-1,1,4,4-tetroxide(143) | 170 nM (hGALR1) | |
| GALNON | hGALR agonist (specificity not established) | 4.8 μ M (Ki at hGALR1) |
| Fmoc-cyclohexylalanine-Lys-amidomethylcoumarin,(136) | ||
