TABLE 2

Binding affinities for selected histamine receptor ligands

Compound #LigandhH1R pKiahH2R pKibhH3R pKichH4R pKid
1Histamine4.65.18.28.1
22-(2-Thiazolyl)-ethylamine5.3<5
4Histaprodifen5.70<5
6Diphenhydramine7.895.804.604.37
8Mepyramine8.804.63<5<5
10Mizolastine9.10<5
11Levocetirizine8.15<6<6<4
12Terfenadine7.92<5<5
13Fexofenadine7.54<5
14Loratadine7.21<54.74
15Desloratadine8.406.45e<55.10
174(5)-Methylhistamine<55.104.727.73
18Amthamine6.825.30
19Dimaprit<54.606.086.42
20Arpromidine6.56.3-8.0
21Impromidine5.27.646.997.76
23Burimamide4.3f5.417.366.97
24Cimetidine4.755.844.695.03
25Ranitidine4.476.674.89<5
27Famotidine<5e7.56<5
30Aminopotentidine4.607.407.10<5
31Tiotidine<47.77<4f<5
32-Methylhistamine4.204.309.007.13
33(R)-α-Methylhistamine<5<48.66.76
34Imetit4.305.109.298.48
35Immepip4.79<3.59.447.79
36Methimmepip9.005.70
38Proxyfan8.27.30
40Thioperamide3.884.277.67.04
41Clobenpropit5.455.479.07.98
42Ciproxifan<5<57.15.73
45Pitolisant5.784.968.06<4
48Conessine<5<58.3<5
55MK-0249<5<58.2<5
56Clozapine8.656.82<46.26
58JNJ-7777120<5<65.308.09
67ZPL-3893786.738.31
72JNJ-39758979<6<66.07.9
74INCB-38579<5<5.36.398.3
75ST-1006<6<66.297.9
  • a Data from Tran et al. (1978); Chang et al. (1979); Kanba and Richelson (1984); De Backer et al. (1993); Leurs et al. (1994a); Vollinga et al. (1994). Sharif et al. (1996); Merlos et al. (1997); Bakker et al. (2001); Gillard et al. (2002a); Esbenshade et al. (2003); Govoni et al. (2003); Thurmond et al. (2004, 2014a,b); Bielory et al. (2005); Xie et al. (2006); Ligneau et al.(2007); Nagase et al. (2008); Zhao et al. (2008); Sander et al. (2009); Rossbach et al. (2011); Appl et al. (2012); Shin et al. (2012); Savall et al. (2014); Where multiple values are reported, they have mostly been averaged.

  • b Data from Harada et al. (1983); Gantz et al. (1991b); Leurs et al. (1994a, 1995b); Sharif et al. (1996); Kreutner et al. (2000); Saitoh et al. (2002); Esbenshade et al. (2003); Thurmond et al. (2004, 2014a,b); Bielory et al. (2005); Lim et al. (2005); Xie et al. (2006); Preuss et al. (2007); Nagase et al. (2008); Zhao et al. (2008); Sander et al. (2009); Rossbach et al. (2011); Shin et al. (2012); Savall et al. (2014); and Levocetirizine New Drug Application #22-064; Loratadine New Drug Application #21-165. Where multiple values are reported, they have mostly been averaged.

  • c Data from West et al. (1990); Vollinga et al. (1994); Sharif et al. (1996); Kato et al. (1997); Lovenberg et al. (1999); Ligneau et al. (2000, 2007); Coge et al. (2001b); Liu et al. (2001a); Wieland et al. (2001); O'Reilly et al. (2002); Wellendorph et al. (2002); Wulff et al. (2002); Esbenshade et al. (2003); Thurmond et al. (2004, 2014a,b); Bielory et al. (2005); Lim et al. (2005); Gbahou et al. (2006); Nagase et al. (2008); Zhao et al. (2008);Sander et al. (2009); Mowbray et al. (2011); Rossbach et al. (2011); Appl et al. (2012); Shin et al. (2012); Andaloussi et al. (2013); Savall et al. (2014); and Levocetirizine New Drug Application #22-064. Where multiple values are reported, they have mostly been averaged.

  • d Data from Ligneau et al., 2000; Liu et al., 2001b; Morse et al., 2001; Zhu et al., 2001; O'Reilly et al., 2002; Esbenshade et al., 2003; Thurmond et al., 2004, 2014a,b; Lim et al., 2005; Gbahou et al., 2006; Ligneau et al., 2007; Nagase et al., 2008; Zhao et al., 2008; Deml et al., 2009; Sander et al., 2009; Mowbray et al., 2011; Rossbach et al., 2011; Appl et al., 2012; Shin et al., 2012; Andaloussi et al., 2013; Savall et al., 2014. Where multiple values are reported, they have mostly been averaged.

  • e Guinea pig.

  • f Rat.