5-HT1 Selective Inhibitors | Agonists | Antagonists
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
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|
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|
Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
|Selective||5-HT1A, Ki: 4.2 nM|
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|
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.
Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.
Rizatriptan Benzoate is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
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|
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|
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|
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|
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.
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