5-HT₂ Receptor Antagonist

Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT_2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNa_v1.7 channels (IC₅₀=25.9 μM; concentration-dependent) and HERG potassium channels (IC₅₀=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis.

Puerarin is an isoflavone extracted from Pueraria root and is a 5-HT2C receptor antagonist. Puerarin inhibits the dorsal motor nucleus of the vagus (DMV)-vagus nerve pathway, which in turn leads to decreased fat absorption.

Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT_2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNa_v1.7 channels (IC₅₀=25.9 μM; concentration-dependent) and HERG potassium channels (IC₅₀=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis.

Puerarin (Standard) is the analytical standard of Puerarin. This product is intended for research and analytical applications. Puerarin, an isoflavone extracted from Radix puerariae, is a 5-HT2C receptor antagonist.

Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic.

SB 242084 is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

GR 113808 is a potent and highly selective 5-HT₄ receptor antagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors.

SB 204741 is a selective and high affinity 5-HT_2B antagonist with a pK_i value of 7.1.

Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.

Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

Sertindole (Lu 23-174) is an orally active 5-HT_2A, 5-HT_2C, dopamine D₂, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells.

Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT_1A, and serotonin 5-HT_2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases.

Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.

RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT₂R antagonist, with pK_is of 8.52, 6.57, and 7.43 for 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT₁, 5-HT₃, 5-HT₄, α₁-, α₂- and β-adrenoreceptor, histamine H₁, H₂ and muscarinic M₃ receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.

Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes.

Blonanserin (AD-5423) is a potent and orally active 5-HT_2A (K_i=0.812 nM) and dopamine D2 receptor (K_i =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pK_is of 8.64, 8.75 and 8.75 for 5-HT_2A, 5-HT_2B and 5-HT_2C, respectively. Metergoline is a high-affinity ligand for the h5-HT₇ receptor, with a K_i of 16 nM. Metergoline is also a reversible neural Na⁺ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.