Nomenclature |
5-HT4 receptor |
5-ht5a receptor |
5-ht5b receptor |
5-HT6 receptor |
5-HT7 receptor |
HGNC, UniProt |
HTR4, Q13639
|
HTR5A, P47898
|
HTR5BP, P31387
|
HTR6, P50406
|
HTR7, P34969
|
Principal transduction |
Gs
|
Gi/Go
|
None identified |
Gs
|
Gs
|
Selective agonists (pKi) |
ML 10302 (Partial agonist) (7.9 – 9.0) 121,123,179–181, BIMU 8 (7.3) 138, RS67506 (pEC50 8.8 - Rat) 154
|
– |
– |
E-6801 (Partial agonist) (8.7) 157, WAY-181187 (8.7) 202
|
E55888 (8.6) 132
|
Selective antagonists (pKi) |
RS 100235 (8.7 – 12.2) 138,200, SB 204070 (9.8 – 10.4) 120,179,180,210, GR 113808 (9.3 – 10.3) 117,120,123,138,180,200,210
|
SB 699551 (8.2) 139
|
– |
SB399885 (9.0) 156, SB 271046 (8.9) 133, SB357134 (8.5) 134, Ro 63-0563 (7.9 – 8.4) 126,204
|
SB269970 (8.6 – 8.9) 207, SB656104 (8.7) 145, SB 258719 (Inverse agonist) (7.5) 208
|
Radioligands (Kd) |
[123I]SB 207710 (8.6x10-11 M - Pig) 135, [3H]GR 113808 (Antagonist) (5x10-11 – 2x10-10 M) 117,120,181,210, [3H]RS 57639 (Agonist) (2x10-10 M - Guinea pig) 127, [11C]SB207145 (Antagonist) (2.8x10-9 M) 174
|
[125I]LSD (Agonist, Full agonist) (2x10-10 M) 148, [3H]5-CT (Agonist, Full agonist) (2.5x10-9 M) 148
|
[125I]LSD, [3H]5-CT |
[3H]5-CT (Agonist), [125I]SB258585 (Antagonist) (1x10-9 M) 156, [3H]LSD (Agonist, Full agonist) (2x10-9 M) 125, [3H]Ro 63-0563 (Antagonist) (5x10-9 M) 126
|
[3H]5-CT (Agonist) (4x10-10 M) 207, [3H]SB269970 (Antagonist) (1.2x10-9 M) 207, [3H]5-HT (Agonist, Full agonist) (1x10-9 – 7.94x10-9 M) 118,206, [3H]LSD (Agonist, Full agonist) (2.51x10-9 – 3.16x10-9 M) 206
|