5-HT Receptor Modulator

Brexpiprazole S-oxide (DM-3411) 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-HT_1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT_2A receptor antagonist with a K_i of 0.47 nM.

Lurasidone (Hydrochloride) (Standard) is the analytical standard of Lurasidone (Hydrochloride). This product is intended for research and analytical applications. 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.

1-(2-Methoxyphenyl)piperazine hydrochloride is a key agent intermediate of antipsychotics with high affinity to the serotonin receptors and 5-HT, which can be used to synthesize the intestinal worm-repellent agents Piperazine phosphate (HY-B0912C) and Piperazine citrate (HY-17599), as well as Fluphenazine (HY-119980), dihydrochloride, Rifampicin (HY-B0272).

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

RS-30199 is an anxiogenic agent. RS-30199 interacts with the 5-HT_1A receptor. RS-30199 prolongs intromission latency. RS-30199 fully inhibits the facilitation of sexual behaviour caused by Delequamine (HY-106874).

Tegaserod-¹³C,d₃ (maleate) is the ¹³C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract.

Ipsapirone hydrochloride (TVX Q 7821) is an anxiolytic compound and a 5-HT_1A receptor partial agonist. Ipsapirone hydrochloride (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.

LY320135 is a potent and selective antagonist of CB1 receptor, with a K_i of 141 nM. LY320135 also binds to 5-HT₂ and muscarinic receptors with K_is of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.

5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pK_i of 6.33 (5-HT6) and a pIC₅₀ valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC₅₀ = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

(R)-Viloxazine hydrochloride is a less active R-isomer of Viloxazine hydrochloride. Viloxazine hydrochloride is an effective antidepressant agent.

Adatanserin (WY-50324) is a high affinity, selective and partial agonist for the 5-HT_1A receptor with a K_i of 1 nM. Adatanserin is a moderate affinity 5-HT₂ receptor antagonist with a K_i of 73 nM. Adatanserin shows significant anxiolytic and antidepressant activity in an animal conflict model.

Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine dihydrochloride 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 dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation.

CTW0419 is a potent 5-HT Receptor positive allosteric modulators (PAMs). CTW0419 is promising for research of neuropsychiatric disorders.

Brexpiprazole (OPC-34712) hydrochloride, 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 hydrochloride is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM).

5-HT2A receptor activator-1 is an allosteric modulator of the 5-HT2A receptor, with an EC₅₀ of 0.56 μM. 5-HT2A receptor activator-1 exerts allosteric interaction with the 5-HT2A receptor, enhances 5-HT-induced receptor activation by binding to the allosteric site, and shows no obvious agonistic activity on its own. 5-HT2A receptor activator-1 can be used in the research of neurological or psychiatric disorders.

Lurasidone-d₈ is deuterium labeled Lurasidone. 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.

R-MDDMA, 4-methylenedioxymethamphetamine (MDMA) analogue, is a 5-HT2A/5-HT2C receptor modulator. R-MDDMA shows antagonistic activity against 5-HT2A/5-HT2C with IC₅₀ values of 642 and 137 nM, and also shows partial agonist activity with EC₅₀ values of 24.5 and 14.4 nM, but does not activate 5-HT2B receptors. R-MDDMA promotes cortical neuron growth. R-MDDMA facilitates fear extinction learning and produces antidepressant-like effects in preclinical rodent models. R-MDDMA can be used for the researches of post-traumatic stress disorder and depression.

ML10375 is a compound that modulates 5-HT4 and 5-HT2 receptors, affects gap junction coupling in rat atrial myocytes, and regulates intracellular cAMP concentration and L-type calcium current.

1-1-Naphthylpiperazine hydrochloride (1-NP hydrochloride; 1-Naphthylpiperazine hydrochloride) is a serotonergic derivative of quipazine, which is both an agonist for 5-HT1A receptor and an antagonist for 5-HT2A receptor. 1-1-Naphthylpiperazine hydrochloride induces cell apoptosis. 1-1-Naphthylpiperazine hydrochloride prevents the immunosuppression and photocarcinogenesis.

Cinitapride monotartrate is a 5-HT_1A and 5-HT₄ agonist. Cinitapride monotartrate is also a 5-HT_2A and D₂ antagonist. Cinitapride monotartrate can be used for the research of functional dyspepsia.