5-HT Receptor Modulator

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.

Azaphen (Azafen) is an orally active tricyclic antidepressant that inhibits the reuptake of serotonin and monoamines, regulates the 5-HT2c receptor, and exerts sedative, antidepressant and anxiolytic effects. Azaphen increases the bioavailability of serotonin in the synaptic cleft, does not block muscarinic receptors or affect monoamine oxidase activity, and binds to the human serotonin transporter via salt bridges, π-stacking, π-cation and hydrophobic interactions. Azaphen can be used in studies related to depression.

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).

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.

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.

Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks.

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