5-HT1 Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S2852 BRL-54443

BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.

Selective 5-HT1D, pKi: 7.2; 5-HT1B, pKi: 6.9; 5-HT1A, pKi: 7.2; 5-HT1F, pKi: 9.25; 5-HT1E, pKi: 8.7
S3180 Eletriptan HBr

Eletriptan is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

Selective 5-HT1D, Ki: 3.14 nM; 5-HT1B, Ki: 0.92 nM
S1975 Aripiprazole

Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.

Selective 5-HT1A, Ki: 4.2 nM
S2669 LY310762

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.

Selective 5-HT1D, Ki: 249 nM
S2025 Urapidil HCl

Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively.

S2096 Almotriptan Malate

Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.

S1607 Rizatriptan Benzoate

Rizatriptan Benzoate is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.

S4256 Buspirone HCl

Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.

S1283 Asenapine

Asenapine is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.

Pan 5-HT1B, pKi: 8.4; 5-HT1A, pKi: 8.6
S2691 BMY 7378

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.

Pan 5-HT1D, pIC50: 5.9; 5-HT1C, pIC50: 6.4; 5-HT1A, pIC50: 8.3
S2677 BRL-15572

BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

Pan 5-HT1F, pKi: 6; 5-HT1E, pKi: 5.2; 5-HT1B, pKi: 6.1; 5-HT1A, pKi: 7.7; 5-HT1D, pKi: 7.9
S1615 Risperidone

Risperidone is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.

Pan 5-HT1A, Ki: 423 nM; 5-HT1B, Ki: 14.9 nM; 5-HT1D, Ki: 84.6 nM
S8021 Vortioxetine (Lu AA21004) HBr

Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

Pan 5-HT1B, Ki: 33 nM; 5-HT1A, Ki: 15 nM
S4259 Vilazodone HCl

Vilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.