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5-HT6/5-HT2A antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (17) Adenylate Cyclase (1) Adrenergic Receptor (7) Apoptosis (6) Autophagy (5) Dopamine Receptor (8) Histamine Receptor (2) Isotope-Labeled Compounds (2) mAChR (5) Mitophagy (5) Parasite (1) Reactive Oxygen Species (ROS) (1) Reference Standards (3)
By Research Areas:	Cancer (5) Neurological Disease (16)

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14541

Olanzapine Maximum Cited Publications 14 Publications Verification LY170053	5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis	Neurological Disease Cancer
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 .

HY-N0049

Nuciferine 5+ Cited Publications	Parasite 5-HT Receptor Dopamine Receptor	Neurological Disease
Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (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-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-107836

Methiothepin mesylate 2 Publications Verification Metitepine mesylate; Ro 8-6837 mesylate	5-HT Receptor	Neurological Disease
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).

HY-109036

Landipirdine RO5025181; SYN120	5-HT Receptor	Neurological Disease
Landipirdine (RO5025181; SYN120) is an orally active *5-HT6* and 5-HT2A receptors antagonist. Landipirdine can be used for the study of Parkinson disease .

HY-14541R

Olanzapine (Standard) LY170053 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis	Neurological Disease Cancer
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. 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 .

HY-14541S

Olanzapine-d3 LY170053-d₃	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis	Neurological Disease Cancer
Olanzapine-d₃ (LY170053-d₃) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .

HY-101009

Methiothepin maleate Metitepine maleate; Ro-8-6837 maleate	5-HT Receptor	Neurological Disease
Methiothepin maleate 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).

HY-14541A

Olanzapine hydrochloride LY170053 hydrochloride	5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis	Neurological Disease Cancer
Olanzapine hydrochloride 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 hydrochloride is an atypical antipsychotic .

HY-111491

Methiothepin Metitepine; Ro 8-6837	5-HT Receptor	Neurological Disease
Methiothepin (Metitepine; Ro 8-6837) 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).

HY-117046

AVN-101	5-HT Receptor Histamine Receptor Adrenergic Receptor	Neurological Disease
AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward *5-HT6, 5-HT2A, and 5HT-2C receptors* (K_i values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (K_i= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .

HY-21995

BGC20-761	5-HT Receptor Dopamine Receptor	Neurological Disease
BGC20-761 is a selecvtive *5-HT6* and dopamine receptor antagonist (human receptor K_i values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent .

HY-163150

5-HT6R antagonist 3	5-HT Receptor	Neurological Disease
5-HT6R antagonist 3 (compound 15) is a potent, selective and brain-penetrant *5-HT6R* antagonist with K_i values of 14 nM, 3533 nM, 35 nM, 1449 nM for 5-HT6, 5-HT1A, 5-HT2A, 5-HT7, respectively. 5-HT6R antagonist 3 shows anxiolytic-like and properties neuroprotective and procognitive-like effects. 5-HT6R antagonist 3 has the potential for the research of Alzheimer’s Disease .

HY-117046A

AVN-101 hydrochloride	5-HT Receptor Histamine Receptor Adrenergic Receptor	Neurological Disease
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward *5-HT6, 5-HT2A, and 5HT-2C receptors* (K_i values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (K_i= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis .

HY-N0049R

Nuciferine (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (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-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-107836R

Methiothepin mesylate (Standard) Metitepine mesylate (Standard); Ro 8-6837 mesylate (Standard)	5-HT Receptor Reference Standards	Neurological Disease
Methiothepin (mesylate) (Standard) is the analytical standard of Methiothepin (mesylate). This product is intended for research and analytical applications. Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).

HY-14541S2

Olanzapine-d8 LY170053-d₈	Isotope-Labeled Compounds Apoptosis Dopamine Receptor Autophagy mAChR Mitophagy 5-HT Receptor Adrenergic Receptor	Neurological Disease
Olanzapine-d8 is a deuterated labeled Olanzapine . 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 .

HY-W130288

1-(1-Naphthyl)piperazine	5-HT Receptor Adenylate Cyclase Apoptosis Reactive Oxygen Species (ROS)	Cancer
1-(1-Naphthyl)piperazine is a 5-HT receptor modulator that acts as both a *5-HT2A* receptor antagonist and 5-HT1A receptor agonist, and binds to human *5-HT6* receptor with a K_i of 120 nM. 1-(1-Naphthyl)piperazine partially inhibits forskolin-stimulated adenylate cyclase activity in calf substantia nigra. 1-(1-Naphthyl)piperazine inhibits UV-induced immunosuppression. 1-(1-Naphthyl)piperazine induces S-phase cell cycle delay, apoptosis and increases ROS levels, leading to inhibit MNT-1 cell proliferation. 1-(1-Naphthyl)piperazine can be used for melanoma research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0049

Nuciferine 5+ Cited Publications	Alkaloids Aporphine Alkaloids other families Plants Isoquinoline Alkaloids Source Classification	Parasite 5-HT Receptor Dopamine Receptor
Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (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-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-N0049R

Nuciferine (Standard)	Alkaloids other families Plants Source Classification	Reference Standards 5-HT Receptor Dopamine Receptor
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (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-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

Cat. No.	Product Name	Chemical Structure

HY-14541S

Olanzapine-d3
Olanzapine-d₃ (LY170053-d₃) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .

HY-14541S2

Olanzapine-d8
Olanzapine-d8 is a deuterated labeled Olanzapine . 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 .

Olanzapine-d8

Olanzapine-d8 is a deuterated labeled Olanzapine . 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 .

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