5-HT₂ Receptor Agonist

CP-809101 hydrochloride is a potent and highly selective 5-HT_2C receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human 5HT_2C, 5HT_2B and 5HT_2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.

Remlifanserin (ACP-204) is a highly selective 5-HT2A inverse agonist. Remlifanserin is applicable to research related to Alzheimer's disease psychosis.

5-HT2A receptor agonist-3 ((S,S)-9b) is a 5-HT2A receptor agonist with a K_i of 2.5 nM for human 5-HT2A receptor. 5-HT2A receptor agonist-3 shows 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor.

5-HT2A receptor agonist-1 (Compound 3) is a selective 5-HT2A receptor agonist with the EC₅₀ of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders.

IHCH-7113 is a 5-HT2AR agonist with EC₅₀ values of 58.9 nM (Gq bioluminescence resonance energy transfer assay) and 44.7 nM (β-arrestin 2 bioluminescence resonance energy transfer assay). IHCH-7113 activates both Gαq-mediated signaling pathways and β-arrestin 2 recruitment pathways. IHCH-7113 is applicable for research related to depression.

Ro60-0175 is a potent and selective agonist of 5-HT_2C receptor. Ro60-0175 reduces self-administration.

MK-212 monohydrochloride (CPP monohydrochloride) is an orally active, blood-brain barrier permeable agonist of 5-HT₁C, 5-HT₂ and 5-HT₁A receptors. MK-212 monohydrochloride induces hyperthermia, nausea, arousal, irritability and restlessness, inhibits the elevation of plasma cortisol and prolactin, and reduces feelings of calmness and overall positive affect. MK-212 monohydrochloride mediates anxiety-like behaviors and motor inhibition. MK-212 monohydrochloride is applicable to research related to schizophrenia and anxiety disorders.

Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT₄ receptor (5-HT4R), with a pK_i of 7.7. Velusetrag exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease.

SB 206553 is a 5-HT_2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT_2A), 7.7 nM (5-HT_2B) and 7.8 nM (5-HT_2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders.

α-Methylserotonin maleate is a potent and selective agonist of 5-HT₂ receptor. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis.

Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT₄ receptor (5-HT₄R), with a pK_i of 7.7. Velusetrag hydrochloride exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease.

AL-34662 is a selective 5-HT2A receptoragonist (IC₅₀: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC₅₀:0.4 μM). AL-34662 is an ocular hypotensive agent.

Quetiapine-d₄ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects.

(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT_2C receptor agonist with a K_i of 4 nM and an EC₅₀ of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT_2C than 5-HT_2A and 5-HT_2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects.

YM348 is a potent and orally active 5-HT_2C receptor agonist, which shows a high affinity for cloned human 5-HT_2C receptor (K_i: 0.89 nM).

cis-Urocanic acid-¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19.

(R)-DOI hydrochloride is a selective 5HT2A receptor agonist. (R)-DOI hydrochloride has anti-inflammatory, anti-oxidative stress, and lysosomal function-improving effects. (R)-DOI hydrochloride can be used for the researches of inflammation and neurological disease, such as Alzheimer's disease.

5-HT2A receptor agonist-6 (compound 47) is a selective 5-HT_2A receptor agonist (pEC₅₀=6.58).

Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.