2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor
  5. 5-HT1 Receptor Isoform
  6. 5-HT1 Receptor Modulator

5-HT1 Receptor Modulator

5-HT1 Receptor Modulators (53):

Cat. No. Product Name Effect Purity
  • HY-15780
    Brexpiprazole
    		Modulator 99.80%
    Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
  • HY-14763
    Cariprazine
    		Modulator 99.67%
    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).
  • HY-N0049
    Nuciferine
    		Modulator 99.90%
    Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (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-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
  • HY-14763A
    Cariprazine hydrochloride
    		Modulator 99.88%
    Cariprazine hydrochloride 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).
  • HY-B0032A
    Lurasidone
    		Modulator 99.36%
    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-HT1A receptor with an IC50 of 6.75 nM.
  • HY-A0095
    Flibanserin
    		Modulator 99.43%
    Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research-.
  • HY-B0032
    Lurasidone Hydrochloride
    		Modulator 99.96%
    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-HT1A receptor with an IC50 of 6.75 nM.
  • HY-A0095A
    Flibanserin hydrochloride (propan-2-ol) hydrate
    		Modulator 99.04%
    Flibanserin (BIMT-17) hydrochloride (propan-2-ol) hydrate is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride (propan-2-ol) hydrate binds to dopamine D4 receptors with an Ki 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-.
  • HY-136621
    5-HT1A modulator 2 hydrochloride
    		Modulator 99.69%
    5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT (HY-112061), is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding.
  • HY-B0731A
    Perospirone
    		Modulator 99.03%
    Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
  • HY-W052508
    Norquetiapine
    		Modulator 99.95%
    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-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 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.
  • HY-109112
    Brilaroxazine
    		Modulator 98.82%
    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 (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=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.
  • HY-116076
    S-15535
    		Modulator 99.82%
    S-15535 is a highly selective 5-HT1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT1A receptors and an agonist of presynaptic 5-HT1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety.
  • HY-101094
    Ocaperidone
    		Modulator 99.93%
    Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis 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 pKi of 7.60 and 8.08 for h5-HT1A.
  • HY-133152S
    Brexpiprazole S-oxide-d8
    		Modulator 98.72%
    Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM.
  • HY-16687A
    Eltoprazine hydrochloride
    		Modulator 99.25%
    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.
  • HY-B0731
    Perospirone hydrochloride
    		Modulator 99.94%
    Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2A receptor (Ki of 0.6 nM) and dopamine D2 receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1A receptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
  • HY-100656
    Desmethyl cariprazine
    		Modulator 98.08%
    Desmethyl cariprazine is an active metabolite of Cariprazine. Cariprazine, an antipsychotic agent candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).
  • HY-15780S
    Brexpiprazole-d8
    		Modulator ≥99.0%
    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 D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
  • HY-100658
    Didesmethyl cariprazine
    		Modulator 99.79%
    Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic agent candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.