Nomenclature |
H1 receptor |
H2 receptor |
H3 receptor |
H4 receptor |
HGNC, UniProt |
HRH1, P35367
|
HRH2, P25021
|
HRH3, Q9Y5N1
|
HRH4, Q9H3N8
|
Principal transduction |
Gq/11
|
Gs
|
Gi/o
|
Gi/o
|
Selective agonists (pKi) |
methylhistaprodifen (6.4) 1025, histaprodifen (5.7) 1013
|
amthamine (pEC50 6.4) 1008
|
immethridine (9.1) 1007, methimepip (9.0) 1006
|
clobenpropit (Partial agonist) (7.4 – 8.3) 1000,1013–1015,1019, 4-methylhistamine (7.3 – 8.2) 1001,1013, VUF 8430 (7.5) 1012
|
Selective antagonists (pKi) |
pyrilamine (Inverse agonist) (8.7 – 9.0) 995,1023, triprolidine (8.5 – 9.0) 995,1017
|
tiotidine (7.5 - Rat) 994, ranitidine (7.1) 1010
|
clobenpropit (8.4 – 9.4) 997,1000,1011,1014,1016,1028,1029, A331440 (8.5) 1002, iodophenpropit (8.2 – 8.7) 1028,1029, thioperamide (7.1 – 7.7) 997,999,1000,1011,1016,1028,1029
|
JNJ 7777120 (7.8 – 8.3) 1013,1026,1027
|
Radioligands (Kd) |
[11C]pyrilamine, [11C]doxepin (Antagonist) (1x10-9 M) 1004, [3H]pyrilamine (Antagonist, Inverse agonist) (7.9x10-10 – 4x10-9 M) 998,1017,1024,1025
|
[125I]aminopotentidine (Antagonist) (2x10-9 M - Rat) 1009, [3H]tiotidine (Antagonist) (2.2x10-9 – 2x10-8 M) 1018
|
[123I]iodoproxyfan (Antagonist) (6.3x10-11 M) 1011, [125I]iodophenpropit (Antagonist) (6x10-10 M - Rat) 1005, [3H](R)-α-methylhistamine (Agonist, Full agonist) (6x10-10 M) 1014, N-[3H]α-methylhistamine (Agonist, Full agonist) (1x10-9 M - Mouse) 996
|
[3H]JNJ 7777120 (Antagonist) (3.6x10-9 M) 1027
|