Overview: 5-HT receptors [nomenclature as agreed by NC-IUPHAR Subcommittee on 5-HT receptors (Hoyer et al., 1994) and subsequently revised (Hartig et al., 1996)] are, with the exception of the ionotropic 5-HT3 class, 7TM receptors, where the
endogenous agonist is 5-HT. The diversity of 5-HT receptors is increased by alternative splicing that produces isoforms of the 5-HT2A
(non-functional), 5-HT2C (non-functional), 5-HT4 and 5-HT7 receptors. RNA editing produces 5-HT2C receptor isoforms that differ in
function, such as efficiency and specificity of coupling to Gq/11. The 5-HT3 receptor [nomenclature as agreed by NC-IUPHAR
Subcommittee on 5-hydroxytryptamine (serotonin) receptors (Hoyer et al., 1994)] is a transmitter-gated ion channel of the Cys-loop
family that includes the nicotinic acetylcholine, GABAA and strychnine-sensitive glycine receptors. The receptor exists as a
pentamer of 4TM subunits that form an intrinsic cation selective channel. 5-HT3 receptor subunits have been cloned, only homo-
oligomeric assemblies of 5-HT3A and hetero-oligomeric assemblies of 5-HT3A and 5-HT3B subunits have been characterised in detail. In
brackets: pEC50/pIC50/pKD values followed by Cat. Nos. (Radioligands: see BIOTREND Radiochemicals-Catalogue).
Further reading: Hoyer et al. (1994) Pharmacol Rev 46:157; Hartig et al. (1996) TiPS 17:103; Alexander et al. (2006) Br J Pharmacol 147:S6; Alexander et al. (2006) Br J Pharmacol 147:S94 Table: Serotonin receptor compounds Nomenclature
(9.0) BN0035,
CP 94253 (8.7) BN0158,
Sumatriptan BG0326
NAS-181 (7.3) BN0368
[3H]-GR 125743 (8.6), [3H]-GR 125743 (8.6),
ART-0750, ART-1750, ART-1750, ART-1551 A3-AI-074 ART-1619 ART-1619 Nomenclature
Gq/11, ↑PLC Gq/11, ↑PLC Gq/11, ↑PLC
ART-1429, ART-1551 ART-1675,
[3H]-LSD ART-0890 Nomenclature
SB 258585 (8.6) BN0668
[3H]-5-HT ART-1551 For a complete list of available products, please visit www.biotrend.com 5-HT1 receptor selective
Category
5-HT1A partial agonist, α1D adrenoceptor antagonist
5-HT1 agonist, also high affinity for 5-ht5A and 5-HT7
Selective 5-HT1A agonist, moderate affinity for 5-HT7
1A agonist, also highly potent D2-like antagonist
5-HT1A/1B antagonist, also β adrenoceptor antagonist
5-HT1A/1B antagonist, also β3 adrenoceptor partial agonist
5-HT1A antagonist, also α2 adrenoceptor ligand
5-HT2 receptor selective
Category
5-HT2C agonist, 5-HT2A/2B partial agonist
5-HT2 antagonist, also dopamine D2 antagonist
Potent 5-HT2A antagonist, atypical antipsychotic
5-HT2C antagonist, also D2/D3 partial agonist
Selective 5-HT2A antagonist, also 5-HT1D antagonist
5-HT2 antagonist, also H1 and α2 adrenoceptor antagonist
For a complete list of available products, please visit www.biotrend.com Category
2 antagonist, also dopamine D2 antagonist
2 antagonist, also dopamine D2 antagonist
2A antagonist, also dopamine D2-like antagonist
Potent 5-HT2 antagonist, also 5-HT1 antagonist
5-HT2,3 antagonist, also H1 and α2 adrenoceptor antagonist
5-HT3 receptor selective
Category
5-HT3 antagonist, D2 agonist, α2 agonist
Weak 5-HT3 antagonist, dopamine D2 antagonist
Potent 5-HT3 antagonist, also 5-HT4 agonist
4 agonist, stimulates Ach release in the intestine
4 agonist, also moderate 5-HT3 antagonist
High affinity for 5-ht5A and 5-HT7, also 5-HT1 agonist
High affinity 5-HT7 ligand, also dopamine D2 antagonist
Potent, selective, brain-penetrant 5-HT7 antagonist
For a complete list of available products, please visit www.biotrend.com 5-HT uptake inhibitors
Category
Active enantiomer of Citalopram (Cat. No. BG0143)
Selective, potent 5-HT uptake inhibitor, σ ligand
Potent 5-HT and adrenergic uptake inhibitor
5-HT and adrenergic uptake inhibitor, 5-HT2A antagonist
Potent 5-HT and adrenergic uptake inhibitor
Potentiator of 5-HT reuptake blockers, 5-HT2C agonist
ART-1402
5-HT reuptake inhibitor, photo affinity labeling reagent
ART-1331 ART-0379 5-HT related compounds
Category
5-HT antagonist, D2,4 and muscarinic antagonist
5-HT antagonist, α and D2 partial agonist
5-HT antagonist, α and D2 partial agonist
Potentiator at 5-HT2A/2C receptors, CB1 agonist
5-HT release inhibitor, antiinflammatory agent
5-HT uptake inhibitor with affinity for 5-HT1A, D2 agonist
Selective serotonin reuptake enhancer (SSRE)
5-HT uptake inhibitor, opioid μ agonist
…distributed by: For a complete list of available products, please visit www.biotrend.com
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§ 90-92. Schedule IV controlled substances. This schedule includes the controlled substances listed or to be listed by whatever official name, common or usual name, chemical name, or trade name designated. In determining that a substance comes within this schedule, the Commission shall find: a low potential for abuse relative to the substances listed in Schedule III of this Article; currentl
Overview: 5-HT receptors [nomenclature as agreed by NC-IUPHAR Subcommittee on 5-HT receptors (Hoyer et al., 1994) and subsequently revised (Hartig et al., 1996)] are, with the exception of the ionotropic 5-HT3 class, 7TM receptors, where the
endogenous agonist is 5-HT. The diversity of 5-HT receptors is increased by alternative splicing that produces isoforms of the 5-HT2A
(non-functional), 5-HT2C (non-functional), 5-HT4 and 5-HT7 receptors. RNA editing produces 5-HT2C receptor isoforms that differ in
function, such as efficiency and specificity of coupling to Gq/11. The 5-HT3 receptor [nomenclature as agreed by NC-IUPHAR
Subcommittee on 5-hydroxytryptamine (serotonin) receptors (Hoyer et al., 1994)] is a transmitter-gated ion channel of the Cys-loop
family that includes the nicotinic acetylcholine, GABAA and strychnine-sensitive glycine receptors. The receptor exists as a
pentamer of 4TM subunits that form an intrinsic cation selective channel. 5-HT3 receptor subunits have been cloned, only homo-
oligomeric assemblies of 5-HT3A and hetero-oligomeric assemblies of 5-HT3A and 5-HT3B subunits have been characterised in detail. In
brackets: pEC50/pIC50/pKD values followed by Cat. Nos. (Radioligands: see BIOTREND Radiochemicals-Catalogue).
Further reading: Hoyer et al. (1994) Pharmacol Rev 46:157; Hartig et al. (1996) TiPS 17:103; Alexander et al. (2006) Br J Pharmacol 147:S6; Alexander et al. (2006) Br J Pharmacol 147:S94 Table: Serotonin receptor compounds
Nomenclature 
5-HT uptake inhibitors