5-HT₁ Receptor Modulator

Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM).

Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D₃ (K_i=0.085 nM) and D₂ (K_i=0.49 nM) receptors, and moderate affinity for the 5-HT_1A receptor (K_i=2.6 nM).

Lurasidone (SM-13496) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

Cariprazine hydrochloride is a novel antipsychotic agent candidate that exhibits high affinity for the D₃ (K_i=0.085 nM) and D₂ (K_i=0.49 nM) receptors, and moderate affinity for the 5-HT_1A receptor (K_i=2.6 nM).

Flibanserin (BIMT-17) hydrochloride (propan-2-ol) hydrate is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with K_i values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride (propan-2-ol) hydrate binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin hydrochloride (propan-2-ol) hydrate shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research^-.

Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.

Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT_2A receptor (K_i=0.6 nM) and dopamine D₂ receptor (K_i=1.4 nM), and also a partial agonist of 5-HT_1A receptor (K_i=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.

5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT (HY-112061), is a modulator of 5-HT_1A with a K_i of 53 nM for 5-HT_1A binding.

Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT₂ and dopamine D₂ antagonist, and a 5-HT_1A agonist, with K_is of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT₂, a₁-adrenergic receptor, dopamine D₂, histamine H₁ and a₂-adrenergic receptor, respectively, and a pEC₅₀ and pK_i of 7.60 and 8.08 for h5-HT_1A.

Cariprazine-d₈ is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).

Eltoprazine (DU 28853) hydrochloride is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine hydrochloride shows antiaggressive and anxiogenic effects.

Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.

Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

Brexpiprazole-d₈ (OPC-34712-d₈) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM)^.

Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D₂ and D₃ receptors, full agonist at the 5-HT_1A receptor, and antagonist at the human 5-HT_2B receptor (K_i: 1.41 nM (human D_2L), 0.056 nM (human D₃), 1.7 nM (human 5-HT_1A), 0.52 nM (human 5-HT_2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.

Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT_1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT_1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT₂ and the α₁-adrenergic function.

Cariprazine-d₆ is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM).

S-15535 is a highly selective 5-HT_1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT_1A receptors and an agonist of presynaptic 5-HT_1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety.