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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
Nomenclature 5‐HT2A receptor 5‐HT2B receptor 5‐HT2C receptor 5‐HT4 receptor
HGNC, UniProt HTR2A, P28223 HTR2B, P41595 HTR2C, P28335 HTR4, Q13639
Agonists DOI (pK i 7.4–9.2) [204, 1374, 1755] methysergide (Partial agonist) (pK i 8–9.4) [970, 1605, 1969], DOI (pK i 7.6–7.7) [1025, 1374, 1659] DOI (pK i 7.2–8.6) [465, 1374, 1659], Ro 60‐0175 (pK i 7.7–8.2) [953, 970] cisapride (Partial agonist) (pK i 6.4–7.4) [77, 128, 597, 1266, 1267, 1941]
Selective agonists – BW723C86 (pK i 7.3–8.6) [108, 970, 1659], Ro 60‐0175 (pK i 8.3) [970] WAY‐163909 (pK i 6.7–8) [454], lorcaserin (pK i 7.8) [1878] TD‐8954 (pK i 9.4) [1250], ML 10302 (Partial agonist) (pK i 7.9–9) [136, 160, 1266, 1267, 1268], RS67506 (pEC50 8.8) [731] – Rat, relenopride (Partial agonist) (pK i 8.3) [607], velusetrag (pK i 7.7) [1139, 1763], BIMU 8 (pK i 7.3) [347]
Antagonists risperidone (Inverse agonist) (pK i 9.3–10) [986, 1008, 1675], mianserin (pK i 7.7–9.6) [970, 1001, 1280], ziprasidone (pK i 8.8–9.5) [986, 1008, 1675, 1711], volinanserin (pIC50 6.5–9.3) [970, 1142, 1568], blonanserin (pK i 9.1) [1421], clozapine (Inverse agonist) (pK i 7.6–9) [970, 1008, 1277, 1675, 1943], olanzapine (pK i 8.6–8.9) [986, 1008, 1675, 1711], nefazodone (pK i 8.2) [1698], chlorpromazine (Inverse agonist) (pK i 8.1) [1008], loxapine (Inverse agonist) (pK i 8.1) [1008], trifluoperazine (pK i 7.9) [1008], pimozide (pK i 7.1–7.7) [986, 1008], trazodone (pK i 7.4) [970], haloperidol (pK i 6.7–7.3) [1008, 1277, 1675, 1711, 1943], mesoridazine (pK i 7.3) [326], mirtazapine (pK i 7.2) [513], mirtazapine (pK i 7.2) [513], quetiapine (pK i 6.4–7) [986, 1008], molindone (pK i 6.5) [1008] mianserin (pK i 7.9–8.8) [180, 970, 1969] mianserin (Inverse agonist) (pK i 8.3–9.2) [524, 970, 1280], methysergide (pK i 8.6–9.1) [465, 970], ziprasidone (Inverse agonist) (pK i 7.9–9) [743, 1008, 1711], olanzapine (Inverse agonist) (pK i 8.1–8.4) [743, 1008, 1711], loxapine (Inverse agonist) (pK i 7.8–8) [743, 1008], mirtazapine (pK i 7.4) [513], mirtazapine (pK i 7.4) [513], trazodone (pK i 6.6) [970], trifluoperazine (pK i 6.4) [1008], agomelatine (pK i 6.2) [1276] –
Selective antagonists ketanserin (pK i 8.1–9.7) [234, 970, 1559], pimavanserin (Inverse agonist) (pK i 9.3) [572, 1943] BF‐1 (pK i 10.1) [1671], RS‐127445 (pK i 9–9.5) [180, 970], EGIS‐7625 (pK i 9) [1001] FR260010 (pK i 9) [700], SB 242084 (pK i 8.2–9) [928, 970], RS‐102221 (pK i 8.3–8.4) [181, 970] RS 100235 (pK i 8.7–12.2) [347, 1589], SB 204070 (pK i 9.8–10.4) [128, 1266, 1267, 1941], GR 113808 (pK i 9.3–10.3) [77, 128, 160, 347, 1267, 1589, 1941]
Labelled ligands [3H]fananserin (Antagonist) (pK d 9.9) [1188] – Rat, [3H]ketanserin (Antagonist) (pK d 8.6–9.7) [970, 1559], [11C]volinanserin (Antagonist) [676], [18F]altanserin (Antagonist) [1601] [3H]LSD (Agonist) (pK d 8.7) [1559], [3H]5‐HT (Agonist) (pK d 8.1) [1967] – Rat, [3H]mesulergine (Antagonist, Inverse agonist) (pK d 7.9) [970], [125I]DOI (Agonist) (pK d 7.7–7.6) [125I]DOI (Agonist) (pK d 8.7–9) [524], [3H]mesulergine (Antagonist, Inverse agonist) (pK d 9.3–8.7) [524, 1559], [3H]LSD (Agonist) [123I]SB 207710 (Antagonist) (pK d 10.1) [228] – Pig, [3H]GR 113808 (Antagonist) (pK d 10.3–9.7) [77, 128, 1268, 1941], [3H]RS 57639 (Selective Antagonist) (pK d 9.7) [179] – Guinea pig, [11C]SB207145 (Antagonist) (pK d 8.6) [1169]
Comments – LSD (lysergic acid) and ergotamine show a strong preference for arrestin recruitment over G protein coupling at the 5‐HT2B receptor, with no such preference evident at 5‐HT1B receptors, and they also antagonise 5‐HT7A receptors [1963]. DHE (dihydroergocryptine), pergolide and cabergoline also show significant preference for arrestin recruitment over G protein coupling at 5‐HT2B receptors [1963]. The serotonin antagonist mesulergine was key to the discovery of the 5‐HT2C receptor [1479]. –