Table 2 Prediction of 5-HT_1B, 5-HT_1D, and 5-HT_1F receptor occupancy levels in the PNS and CNS. The trigeminal ganglion (TG) represents the PNS region, while whole brain (WB) represents the CNS region. Predictions are based on unbound maximal target site concentrations after therapeutic doses of eletriptan and sumatriptan in humans

K_d,5−HT1B [51]

nM

NA

3.14

11.07

K_d,5−HT1D [51]

nM

NA

0.92

6.58

K_i,5−HT1F [51]

nM

NA

10.23

13.18

f_{u, plasma} [50]

0.13

0.66

C_{tot, max} [35, 36]

nM or (ng/mL)

Plasma

246 (94.0)

102 (30.1)

180 (53.2)

C_{u, max}

nM or (ng/mL)

Plasma

32.2 (12.3)

67.3 (19.9)

119 (35.1)

C_{u, max, ROI}

nM

TG

16.6

62.1

109.8

C_{u, max, ROI}

nM

WB

1.86

3.00

5.31

RO_5−HT1B

%

TG

84

85

90

RO_5−HT1B

%

WB

37

21

32

RO_5−HT1D

%

TG

95

90

94

RO_5−HT1D

%

WB

67

31

45

RO_5−HT1F

%

TG

62

82

89

RO_5−HT1F

%

WB

15

19

29