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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
5-HT2AR agonist
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "5-HT2AR agonist" in MCE Product Catalog:
2
2
2 Cited Publications
Synonyms: Ordenina hydrochloride; Peyocactine hydrochloride
Cat. No.: HY-169841
CAS No.: 2957888-70-7
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IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT2AR with a Ki of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression .
Cat. No.: HY-W077477
CAS No.: 313368-85-3
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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 .
Cat. No.: HY-N0113S
CAS No.: 1346598-66-0
Synonyms: Ordenina-d6; Peyocactine-d6
Target:
Isotope-Labeled Compounds Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Hordenine-d6 (Ordenina-d6; Peyocactine-d6) is the deuterated-labeled Hordenine (HY-N0113). Hordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder .
Cat. No.: HY-172995
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RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression .
Cat. No.: HY-172981
CAS No.: 2913202-87-4
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CTW0404 is a 5-HT2AR positive allosteric modulator that enhances Serotonin (HY-B1473A)-induced intracellular calcium release without intrinsic agonist activity. CTW0404 attenuates head-twitch responses but does not induce head twitches by itself. CTW0404 can be used for research on neuropsychiatric disorders .
Cat. No.: HY-157429
CAS No.: 2865185-31-3
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25N-N1-Nap is a blood-brain barrier-permeable, selective, β-arrestin2-biased 5-HT2A receptor (5-HT2AR) agonist. 25N-N1-Nap reduces Gq efficacy while preserving β-arrestin2 efficacy. 25N-N1-Nap does not induce hallucinogen-like behavioral responses, blocks hyperactivity induced by hallucinogens and psychostimulants, and induces rapid tolerance to hallucinogen-like responses. 25N-N1-Nap can be used for research on schizophrenia-related hyperactivity .
Cat. No.: HY-W728110
CAS No.: 3949-14-2
Synonyms: 5-Methoxy pyrrolidinyltryptamine
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5-MeO-pyr-T (5-Methoxy pyrrolidinyltryptamine) is a 5-HT1AR agonist, with Kis of 0.577 and 373 μM for 5-HT1AR and 5-HT2AR respectively. 5-MeO-pyr-T inhibits 5-HT uptake and elicits 5-HT release. 5-MeO-pyr-T induces hypolocomotion .
Cat. No.: HY-157425
CAS No.: 1216074-15-5
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5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT2CR partial agonist (Emax=71.09%) with an EC50 value of 121.5 nM and no observed activity toward 5-HT2AR or 5-HT2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .
Cat. No.: HY-N0113BR
CAS No.: 6027-23-2
Synonyms: Ordenina hydrochloride (Standard); Peyocactine hydrochloride (Standard)
Category:
Alkaloids Plant Cactaceae Extract Monophenols Other Alkaloids Phenols Coryphantha vivipara var arizonica Extract
Target:
Reference Standards Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Cat. No.: HY-N0113BS
Synonyms: Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride
Target:
Isotope-Labeled Compounds Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Research Areas:
Hordenine-d6 hydrochloride (Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride) is the deuterated-labeled Hordenine hydrochloride (HY-N0113B). Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder .
Cat. No.: HY-N0113A
CAS No.: 62493-39-4
Synonyms: Ordenina sulfate; Peyocactine sulfate
Category:
Cardiovascular Disease Alkaloids Plant Phenols Other Families Extract Disease Research Fields
Target:
Reference Standards Bacterial p38 MAPK JNK ERK Akt Interleukin Related TNF Receptor NO Synthase COX Reactive Oxygen Species (ROS) Microphthalmia Associated Transcription Factor (MITF) Wnt β-catenin Dopamine Receptor Adrenergic Receptor 5-HT Receptor Serotonin Transporter Dopamine Transporter α-synuclein
Cat. No.: HY-187560
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VCU-1012 is a serotonin 2A receptor (5-HT2AR) agonist, with a pEC50 of 5.81 and a pKi of 5.75 against human receptors. VCU-1012 binds to the canonical orthosteric binding pocket of 5-HT2AR, triggers intracellular calcium release and Gαq protein dissociation, and its agonistic activity depends on specific amino acid residues in the receptor binding pocket. VCU-1012 can be used in research related to depression, anxiety disorders, and chemotherapy-induced mood disorders .
Cat. No.: HY-189235
CAS No.: 3078735-55-1
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IHCH-8110 is a peripherally restricted, non-brain-penetrant 5-HT2AR and 5-HT2CR agonist (Ki=47.86 nM) that antagonizes 5-HT2BR. IHCH-8110 induces CXCL10 and IL-18 expression by activating 5-HT2AR on enteric glial cells, thereby promoting CD8 + T cell recruitment and effector polarization, and avoids the risk of cardiac valvulopathy associated with 5-HT2BR activation. IHCH-8110 exhibits a low risk of hERG channel inhibition (IC50=5.96 μM) and is well tolerated, sensitizing immunologically cold colorectal cancer to PD-1 blockade therapy, making it suitable for research related to colorectal cancer .
Cat. No.: HY-183357
CAS No.: 3128970-09-9
Target:
GABA Receptor 5-HT Receptor Reactive Oxygen Species (ROS) TNF Receptor Interleukin Related COX NF-κB IKK NO Synthase
Research Areas:
GABAAR/5-HT2AR modulator-1 is an orally active and brain-penetrant GABAAR agonist and 5-HT2AR antagonist with Kd values of 0.89 and 0.78 μM. GABAAR/5-HT2AR modulator-1 blocks 5-HT-stimulated IP1 accumulation, inducing a chloride current, reduces LPS (HY-D1056)-induced increases of ROS, NO, TNF-α, IL-6, IL-1β, iNOS, and COX-2 levels. Antidepressant agent 11 dihydrochloride inhibits NF-κB pathway activation by reducing IκBα and p65 phosphorylation and blocking p65 nuclear translocation. GABAAR/5-HT2AR modulator-1 alleviates depression-like behaviors in LPS-challenged and chronic restraint stress-challenged mice, and protects hippocampal neurons against inflammation-mediated damage .
Cat. No.: HY-189719
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EA-Ri-153 is a selective D3R agonist. EA-Ri-153 has a Ki = 2.8 nM and pEC50 = 8.9 for D3R, and a Ki = 1.2 μM for D2R, with a D3/D2 selectivity ratio of 435-fold. EA-Ri-153 has a Ki = 2.5 μM for 5-HT1AR and a Ki = 22.8 μM for 5-HT2AR. EA-Ri-153 can be used for research on diseases related to the dopamine D3 receptor subtype .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
