Histamine receptors

Nomenclature Selective agonists

2-(3-fluOfophenyl)histamine* 2-[3-(trifluoromethyl)phenyl] histamine

dimaprit impromidine" amthamine

R-a-methylhistamine imetit immepip

Selective antagonists

triprolidine (9.9) mepyramine (9.1)

tiotidine (7.8) ranitidine (7.2)

clobenpropit (9.9) iodophenpropit (9.6) thioperamide (8.4)

Radioligands

[3H]mepyramine (0.8 nM) [3H]tiotidine (15 nM) [125I]iodobolpyramine (0.1 nM) [125I]iodoaminopotentidine (O.3nM)

pH]R-a-methylhistamine [3H]N"-methylhistamine [l25I]iodophenpropit (0.6 nM) [l 25I]iodop ro xyfan (0.06nM)

G protein effector Gene/Chromosomal localization

HRHl/3pl4-p21

HRH2/5

Structure - 7TM

h487 P35367 m488 050095 r486 P31390

h359 P20521 m358 050096 r358 P25102

*partial agonist t also an H 3 receptor antagonist Reviews • Hill, S. J. (1990) Distribution, properties and functional characteristics of three classes of histamine receptor Pharmacal. Rev. 42, 45-83 • Leurs, R. et al. (1995) Molecular pharmacological aspects of histamine receptors Pharmacal. Ther. 66, 413-463 • Hill, S. J. et al. (1997) IUPHAR classification of histamine receptors Pharmacol. Rev. (in press)