Table 3

Antagonist dissociation constants at histamine receptors

KBvalues
H1H3H2
Doxepin0.06 nM3-a n.d.n.d.
Triprolidine (trans)0.1 nM3-b n.d.n.d.
Temelastine0.3 nM3-c >10 μM3-c n.d.
Mepyramine (pyrilamine)0.4 nM3-d 5.2 μM3-e >1 μM3-f
(+)-Chlorpheniramine0.4 nM3-g 1.2 μM3-h >58 nM3-i
(−)-Chlorpheniramine204 nM3-g 1.2 μM3-h >58 nM3-i
Diphenhydramine1.0 nM3-j n.d.n.d.
Promethazine1.2 nM3-k 3.0 μM3-l n.d.
Chlorpromazine1.2 nM3-k 5.9 μM3-l n.d.
Tripelenamine3.2 nM3-d n.d.n.d.
Arpromidine20 nM3-m agonist3-ah
Cimetidine450 μM3-n 800 nM3-n 33 μM3-i
Metiamiden.d.920 nM3-o 2.5 μM3-j
Ranitidine>100 μM3-p 200 nM3-p >1.2 μM3-i
Famotidinen.d.17 nM3-q n.d.
Zolantidine6.2 μM3-r 25 nM3-r >10 μM3-s
Mifentidine>24 μM3-t 24 nM3-t 100 nM3-s
Tiotidine>30 μM3-u 15 nM3-v >12 μM3-i
Iodoaminopotentidine1.1 μM3-w 2.5 nM3-w n.d.
Impromidine3.4 μM3-x agonist3-x 65 nM3-i
Burimamide320 μM3-y 7.8 μM3-z 70 nM3-i
Thioperamide>100 μM3-aa >10 μM3-aa 4 nM3-aa
Iodophenpropitn.d.n.d.0.25 nM3-ab
Clobenpropit>10 μM3-ac >10 μM3-ac 0.13 nM3-ac
Iodoproxyfan1.4 μM3-ad 5.3 μM3-ad 5 nMad, ag
Impentamine126 μM3-ae 250 μM3-ae 4 nM3-ae
GR174737>10 μM3-af >10 μM3-af 8 nM3-af
  • Values determined in functional assays from guinea pig ileum contraction (H1), biochemical determinations in guinea pig cerebral cortical slices (H1), chronotropic responses in guinea pig atria (H2), cyclic AMP accumulation in guinea pig hippocampal slices (H2), inhibition of histamine release in rat cerebral cortical slices (H3), and inhibition of transmurally stimulated guinea pig ileum (H3). n.d., not determined.

  • 3-a Figge et al. (1979)

  • 3-b Ison et al. (1973)

  • 3-c Brown et al. (1986)

  • 3-d Marshall (1955)

  • 3-e Trendelenburg (1960)

  • 3-f Hew et al. (1990)

  • 3-g Hill et al. (1981)

  • 3-h Hill (1990)

  • 3-i Arrang et al. (1983)

  • 3-j Ganellin (1982)

  • 3-k Hill and Young (1981)

  • 3-l Tuong et al. (1980)

  • 3-m Sellier et al. (1992)

  • 3-n Brimblecombe et al. (1975)

  • 3-o Black et al. (1974)

  • 3-p Cavanagh et al. (1983)

  • 3-q Takeda et al. (1982)

  • 3-r Calcutt et al. (1988)

  • 3-s Schwartz et al. (1990)

  • 3-t Donetti et al. (1984)

  • 3-u Donaldson et al. (1988)

  • 3-v Yellin et al. (1979)

  • 3-w Hirschfeld et al. (1992)

  • 3-x Durant et al. (1978)

  • 3-y Buschauer et al. (1992)

  • 3-z Black et al. (1972)

  • 3-aa Arrang et al. (1987)

  • 3-ab Jansen et al. (1992)

  • 3-ac Van der Goot et al. (1992)

  • 3-ad Ligneau et al. (1994)

  • 3-ae Vollinga et al. (1995)

  • 3-af Clitherow et al. (1996)

  • 3-ag Stark et al. (1996a)

  • 3-ah Buschauer (1989)