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. 2020 Feb 21;3(3):509–523. doi: 10.1021/acsptsci.9b00101

Table 2. Kinetic Binding Parameters of Radioligands and Unlabeled FPT at 5-HT1ARs, 5-HT2CRs, and 5-HT7Rsa.

receptor compound residence time koff kon Kd
5-HT1A [3H]5-CT 3 0.32 ± 0.06 1.3 × 108 ± 3.3 × 107 2.5
FPT 2 0.50 ± 0.04 2.8 × 107 ± 8.6 × 106 18
5-HT2C [3H]mesulergine 143 0.007 ± 0.001 4.1 × 106 ± 2.2 × 105 1.7
FPT 5 0.186 ± 0.018 2.5 × 105 ± 1.9 × 104 732
5-HT7 [3H]5-CT 143 0.007 ± 0.002 2.3 × 107 ± 2.9 × 106 0.3
FPT 4 0.26 ± 0.12 4.3 × 107 ± 1.8 × 107 6.2
a

koff (min–1) and kon (M–1·min–1) were derived from 3–4 independent experiments. Residence time was calculated as 1/koff and was rounded to the nearest minute, while the kinetically determined Kd was calculated using mean kinetic parameters and the equation Kd = koff/kon, presented in nM.