5-HT1 Selective Inhibitors | Agonists | Antagonists | Modulators

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

Eletriptan (UK-116044) 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
S3716 Flibanserin

Flibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.

Selective 5-HT1A, Ki: 1 nM
S6489 Lasmiditan succinate

Lasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity.

Selective 5-HT(1F), Ki: 2.21 nM
S1975 Aripiprazole

Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.

Selective 5-HT1A, Ki: 4.2 nM
S8447 8-OH-DPAT (8-Hydroxy-DPAT)

8-OH-DPAT (8-Hydroxy-DPAT) is a kind of classic 5-HT1A agonist with the pIC50 of 8.19. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site; Its biological half-life is 1.5 hous.

Selective 5-HT1A, pIC50: 8.19
S2669 LY310762 HCl

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
S4358 Pimozide

Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.

Selective 5-HT1A, Ki: 310 nM
S7538 RS-102895 Hydrochloride

RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.

Selective 5-HT1a receptor, IC50: 470 nM
S0104 Pardoprunox (SLV-308) hydrochloride

Pardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively.

Selective 5-HT1A receptor, pEC50: 6.3
S5153 Tetrahydroberberine

Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors.

Selective 5-HT1A, pKi: 5.38
S5965 Urapidil

Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.

Selective
S4256 Buspirone HCl

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

Selective
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.

Selective
S1607 Rizatriptan Benzoate

Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.

Selective
S3510 NLX-101

NLX-101 (F-15599) is a highly selective 5-HT1A receptor biased agonist that mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors.

Selective
S2096 Almotriptan Malate

Almotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.

Selective
S5064 Lasmiditan

Lasmiditan (Reyvow) is a highly selective 5-hydroxytryptamine (serotonin) receptor 1F (5-HT1F) agonist that can be used as a promising acute anti-migraine therapy.

Selective
S5843 Cinitapride Hydrogen Tartrate

Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors

Pan
S4639 Brexpiprazole

Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.

Pan 5-HT1A, Ki: 0.12 nM
S1283 Asenapine maleate

Asenapine maleate (Org 5222) 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
S4889 Perospirone hydrochloride

Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

Pan 5HT1A receptor, Ki: 2.9 nM
S5185 Perospirone

Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.

Pan 5-HT1A receptor, Ki: 2.9 nM
S2691 BMY 7378 Dihydrochloride

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-HT1C, pIC50: 6.4; 5-HT1D, pIC50: 5.9; 5-HT1A, pIC50: 8.3
S5714 lurasidone

Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.

Pan 5-HT1A receptor, Ki: 6.4 nM
S2677 BRL-15572 Dihydrochloride

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-HT1D, pKi: 7.9; 5-HT1A, pKi: 7.7; 5-HT1B, pKi: 6.1
S1615 Risperidone

Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.

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

Vortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM.

Pan 5-HT1B, Ki: 33 nM; 5-HT1A, Ki: 15 nM
S3913 Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.

Pan 5-HT1B, pKi: <5; 5-HT1A, pKi: 7.63
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.

Pan