Table 1

MT2 and MT1/MT2 antagonists on efficacy and maximum contractile effect of melatonin

pEC50 (C.I.)Emaxn
MT2-Antagonism g
Melatonin8.6 (9.2–8.0)0.116 ± 0.0136
+ 10 nM 4P-PDOT8.8 (9.2–8.3)0.170 ± 0.0051-150 6
Melatonina 8.8 (9.4–8.2)0.101 ± 0.0036
+ 10 nM 4P-ADOTa 8.7 (9.2–8.2)0.173 ± 0.0041-150 4
MT1/MT2Antagonism
Melatonin9.0 (10.1–7.9)0.098 ± 0.0077
+ 3 μM luzindole7.7 (8.8–6.7)1-150 0.135 ± 0.0121-150 7
Melatoninb 8.4 (9.5–7.2)0.122 ± 0.0087
+ 3 μM 4P-ADOTb 7.4 (8.1–6.6)1-150 0.168 ± 0.0111-150 7

Data from cumulative concentration-response curves for melatonin in precontracted segments of caudal arteries from male Fisher-344 rats. Mean and 95% confidence interval (CI) given for pEC50 and mean ± S.E.M. given for maximum contraction (Emax) in grams of contractile force.

  • a,b pEC50 and Emax values were calculated from data presented graphically in Krause et al., 2000a and Doolen et al., 1998b. The calculated affinity constants (KB) for luzindole and 4P-ADOT to block the melatonin-mediated contraction were 157 and 302 nM, respectively.

  • 1-150p < 0.05 when compared with melatonin alone