The affinity of radioligands for GPCR105 and the human H3receptor
| Radioligand | H3Receptor KD | GPCR105 ReceptorKD |
|---|---|---|
| nM | nM | |
| 3H-Histamine | 11 ± 2 (n = 2) | 5.0 ± 3.5 (n = 3) |
| 3H-R-α-methylhistamine | 0.6 ± 0.3 (n = 3) | 58 ± 9 (n = 2) |
| 3H-N-methylhistamine | 0.8 ± 0.1 (n = 2) | 17 ± 3 (n = 2) |
K D values (average ± S.D.) are derived from a −1/slope of a linear regression of a Scatchard transformation (bound/free versus bound). Saturation binding was performed on membranes from SK-N-MC cells stably transfected with either the human H3 receptor or human GPCR105.