Table 5

Affinity values of G protein-coupled 5-HT receptors for different 5-HT drugs5-a

5-HT1A5-HT1B5-b5-HT1D5-b5-HT1E5-HT1F5-HT2A5-HT2C5-HT45-HT5A/B5-HT65-HT7
0.7 nM19
7 nM17 0.37 nM13 1,000 nM8 16–40 nM4 774 nM6 0.12 nM5
5-CT0.2 nM31 0.35 nM13 1.5 nM29 7,875 nM3 717 nM3 2,000 nM31 600 nM31 3,160 nM44 12–235 nM9 253 nM8 0.93 nM8
5 nM14
79 nM35 11 nM13 0.6 nM13 >10,000 nM8 16–100 nM4
Methiothepin89 nM36 50 nM35 50 nM35 194 nM3 652 nM3 1.58 nM35 25 nM35 23–145 nM9 0.39 nM6 3.7 nM8
120 nM19
8-OH-DPAT1.2 nM24 >10,000 nM13,14 99 nM13 >10,000 nM43 >10,000 nM44 400–1,200 nM4
0.4 nM36 975 nM15 3,333 nM3 1,772 nM3 700 nM24 52 nM5
>10,000 nM31 >10,000 nM31
WAY 10013523 nM32 6,000 nM31
52 nM32 >10,000 nM35
S-UH-301126 nM34 7,200 nM35 7,150 nM35
8 nM12 1,100 nM18
CP 931291,500 nM12 55 nM16 954 nM40 7,200 nM12 2,900 nM12
55 nM35 1,509 nM15
5 nM13 1,300 nM13 >10,000 nM18 >10,000 nM18 2,987 nM33 6,000–20,000 nM4
(−)-Propranolol52.5 nM35 50 nM40 57 nM16 158 nM42 200 nM33
465 nM16
320 nM29 45 nM13 9.5 nM13 >10,000 nM22 >10,000 nM22 8,000–15,000 nM4 506 nM5
Sumatriptan239 nM38 100 nM14 8.9 nM15 2,520 nM3 23 nM3 951 nM8
GR 127935125 nM31 3 nM30 3 nM30 3,000–4,000 nM30 40 nM30 630 nM30 >10,000 nM30 6,000–20,000 nM30
500 nM13
1,000 nM35 6,000– 10,000 nM13,35 30 nM13 10 nM35
Mianserin1,150 nM39 398 nM35 7.9 nM35 1.9 nM41 38 nM6 67 nM5
200 nM35
300 nM23 3.3 nM13 59 nM13 32 nM24 13 nM35 3,000–4,000 nM4
TFMPP170 nM24 27 nM24 690 nM35 6,293 nM3 1,002 nM3 780 nM35 50 nM23 482 nM6 466 nM8
1.22 nM14
7.9 nM35 0.36 nM13 65.6 nM15 316 nM35 >10,000 nM44 3,000–4,000 nM4
RU 249692.5 nM37 2 nM15 47 nM13 42 nM35 47.8 nM38
Renzapride
8-OH-DPATCP93129L69424727 KetanserinMesulergineBUIM8
Selective ligandWAY 10063528 SDZ2100928 GR17293528 MDL 10090728 SB20064628 GR11380828
YesYesYesNo2 YesYesYes5
mRNA in DRNVery high7 High2,20 Moderate2 Low2 5-HT5B 4
No21 Yes/low26 No1
Binding sites in DRNYesYes/moderate26 Yes/moderate11
Very high7
  • Superscript numbers represent sources: 1, Mengod et al., 1996; 2,Bruinvels et al., 1992; 3, Adham et al., 1993a; 4, Matthes et al., 1993; 5, Ruat et al., 1993; 6, Monsma et al., 1993; 7, Lucas and Hen, 1995; 8, Bard et al., 1993; 9, Erlander et al., 1993; 10, Adham et al., 1993b; 11, To et al., 1995; 12, Kow et al., 1992; 13, Hamblin et al., 1992a; 14, Cerutis et al., 1994; 15, Maenhault et al., 1991; 16,Parker et al., 1993; 17, Oksenberg et al., 1992; 18, Adham et al., 1994; 19, Weinshank et al., 1992; 20, Doucet et al., 1995; 21,Vergé et al., 1986; 22, Glennon et al., 1994; 23, Waeber et al., 1988a; 24, Herrick-Davis and Titeler, 1988; 25, Zgombick et al., 1993; 26, Bruinvels et al., 1993; 27, Heald et al., 1994; 28, Langlois et al., 1993; 29, Koe et al., 1994; 30, Starkey and Skingle, 1994; 31,Skingle et al., 1994; 32, Fletcher et al., 1993; 33, Prisco et al., 1993; 34, Cornfield et al., 1991; 35, Griebel et al., 1995; 36, Gozlan et al., 1983; 37, Peroutka, 1986; 38, Van Winjgaarden, 1990; 39, Hoyer, 1985; 40, Bruinvels et al., 1991; 41, Yagaloff and Hartig, 1985; 42,Alexander and Wood, 1987; 43, Sanders-Bush, 1988; 44, Dumuis et al., 1988.

  • 5-a Affinity values are given as K D orK i values for binding studies performed in brain membranes or heterologous expression systems.

  • 5-b Old nomenclature as it appears in original reference.