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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
Nomenclature H1 receptor H2 receptor H3 receptor H4 receptor
HGNC, UniProt HRH1, P35367 HRH2, P25021 HRH3, Q9Y5N1 HRH4, Q9H3N8
Selective agonists methylhistaprodifen (pK i 6.4) [1695], histaprodifen (pK i 5.7) [1107] amthamine (pEC50 6.4) [1003] immethridine (pK i 9.1) [963], methimepip (pK i 9) [962], MK‐0249 (Inverse agonist) (pK i 8.8) [1354] clobenpropit (Partial agonist) (pK i 7.4–8.3) [490, 1107, 1122, 1123, 1335], 4‐methylhistamine (pK i 7.3–8.2) [586, 1107], VUF 8430 (pK i 7.5) [1106]
Antagonists cyproheptadine (pK i 10.2) [1298], promethazine (pK i 9.6) [601], pyrilamine (Inverse agonist) (pK i 8.7–9) [184, 1563], hydroxyzine (pK i 8.7) [608], ketotifen (pK i 8.6) [1014], cetirizine (Inverse agonist) (pK i 8.2) [1298], diphenhydramine (pK i 7.9) [184] – iodophenpropit (pK i 8.2–8.7) [2022, 2051], thioperamide (pK i 7.1–7.7) [355, 489, 490, 1104, 1145, 2022, 2051] –
Selective antagonists clemastine (pK i 10.3) [68], desloratadine (pK i 9) [1090], triprolidine (pK i 8.5–9) [184, 1298], azelastine (pK i 8.9) [1535], astemizole (pK i 8.5) [1480], cyclizine (pK i 8.4) [68], chlorpheniramine (pK i 8.1) [1535], fexofenadine (pK i 7.6) [64], loratadine (pK i 7.4) [850], terfenadine (pK i 7.4) [64], tripelennamine (pIC50 7.4) [635] tiotidine (pK i 7.5) [145] – Rat, ranitidine (pK i 7.1) [1086], cimetidine (pK i 6.8) [263] clobenpropit (pK i 8.4–9.4) [355, 490, 1104, 1122, 1145, 2022, 2051], A331440 (pK i 8.5) [688] JNJ 7777120 (pK i 7.8–8.3) [1107, 1771, 1881]
Labelled ligands [3H]pyrilamine (Antagonist, Inverse agonist) (pK d 8.4–9.1) [403, 1298, 1675, 1695], [11C]doxepin (Antagonist) (pK d 9) [830], [11C]pyrilamine (Antagonist, Inverse agonist) [125I]iodoaminopotentidine (Antagonist) (pK d 8.7) [1029] – Rat, [3H]tiotidine (Antagonist) (pK d 7.7–8.7) [1310] [123I]iodoproxyfan (Antagonist) (pK d 10.2) [1104], [125I]iodophenpropit (Antagonist) (pK d 9.2) [849] – Rat, [3H](R)‐α‐methylhistamine (Agonist) (pK d 9.2) [1122], N‐[3H]α‐methylhistamine (Agonist) (pK d 9) [301] – Mouse [3H]JNJ 7777120 (Antagonist) (pK d 8.4) [1881]