Compound | H1 (Ki, nM)a | H2 (Ki, nM)b | H3 (Ki, nM)3-c | H1/H3ratio3-d | H2/H3 ratio3-d |
---|---|---|---|---|---|
GT-2227 | 13,407 ± 540 | 4,469 ± 564 | 3.2 | 4,190 | 1,397 |
a,b The affinity of GT-2227 for the human HA H1and H2 receptors, respectively, was determined using Chinese hamster ovary cells expressing the respective HA receptor subtype (mean ± S.E., n = 4).
↵3-c The affinity of GT-2227 for the human HA H3 receptor was determined using membranes prepared from postmortem human forebrain tissue (n = 1).
↵3-d Ratios were calculated by dividing the HA H1 or H2 K i values by the HA H3 K i value.