Table 3:
Affinities of melatonin and a few selected melatonergic drugs towards human MT1 and MT2 receptors.
Compound | pKi at MT1 | pKi at MT2 | References |
---|---|---|---|
Melatonin* | 10.09 | 9.42 | [310] |
Ramelteon | 10.85 | 9.95 | [310] |
Agomelatine | 10.21 | 9.57 | [311] |
GR 196429 | 9.85 | 9.79 | [312,313] |
Tasimelteon | 9.45 | 9.80 | [314] |
TIK-301 | 10.09 | 10.38 | [315,316] |
AH-017 | 8.27 | 9.16 | [313] |
UCM765 | 8.38 | 10.17 | [316,317] |
UCM924 | 6.75 | 9.27 | [317] |
Other, moderately deviating values from different laboratories are summarized in ref. [19]. pKi values were either directly obtained from respective publications or calculated from published Ki values.