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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
75 Results for "
5-HT Receptor Activators
" in MedChemExpress (MCE) Product Catalog:
Products (75)
75 Results for "5-HT Receptor Activators" in MCE Product Catalog:
Cat. No.: HY-120037
CAS No.: 152148-63-5
Target:
5-HT Receptor Adrenergic Receptor Dopamine Receptor TRP Channel NF-κB PI3K Interleukin Related TNF Receptor
Research Areas:
A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC50 = 13 nM; Ki = 3.8 nM) and α2-Adrenoceptor receptor antagonist (Ki = 2 nM). A 80426 shows weak antagonistic effect to dopamine D1 receptor (Ki = 744 nM) and D2 receptor (Ki = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression .
Cat. No.: HY-107613AR
CAS No.: 93076-98-3
Synonyms: DKGI-I hydrochloride (Standard); Diacylglycerol kinase inhibitor I hydrochloride (Standard)
Target:
Research Areas:
R 59-022 hydrochloride (Standard) is the analytical standard of R 59-022 (hydrochloride) (HY-107613A). This product is intended for research and analytical applications. R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein Kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
Cat. No.: HY-14604R
CAS No.: 90494-79-4
Synonyms: SR57746A (Standard); SR57746 hydrochloride (Standard)
Research Areas:
Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
Cat. No.: HY-182373
CAS No.: 850033-84-0
Target:
Research Areas:
5-HT2C agonist-13 is an orally active, selective and brain-penetrant 5-HT2C receptor agonist with human 5-HT2C receptor EC50 of 16 nM, Ki of 20 nM. 5-HT2C agonist-13 functionally activates 5-HT2C receptors, reduces food intake, reduces body weight gain, and exhibits effects reversible by a selective 5-HT2C antagonist. 5-HT2C agonist-13 can be used for the research of obesity .
Cat. No.: HY-101225A
CAS No.: 159651-91-9
Target:
Research Areas:
8 Hydroxy PIPAT is a 5-HT1A receptor agonist that promotes histamine release. 8 Hydroxy PIPAT selectively activates 5-HT1A receptors, thereby triggering mast cell degranulation and histamine release. 8 Hydroxy PIPAT is applicable to research related to irritable bowel syndrome .
Cat. No.: HY-N20747
CAS No.: 28363-70-4
Synonyms: 4-Hydroxy-N-methyltryptamine; 4-HO-NMT
Target:
Cat. No.: HY-182597
CAS No.: 65248-90-0
Research Areas:
Tracizoline is an orally active I2-imidazoline receptor agonist. Tracizoline functionally modulates I2-imidazoline receptors, regulates hippocampal FADD cell fate adaptor, attenuates mechanical and thermal hyperalgesia, activates α2A-adrenergic receptors with very weak partial agonism, and induces antidepressant-like activity via 5-HT1A receptor activation. Tracizoline can be used for the research of inflammatory pain, neuropathic pain, and depression .
Cat. No.: HY-19682A
CAS No.: 68576-88-5
Target:
Research Areas:
Enciprazine dihydrochloride is an orally active non-benzodiazepine anxiolytic. Enciprazine dihydrochloride acts as an agonist of 5-HT1A receptor (5-HT1AR) and an antagonist of α1-adrenergic receptor (α1-adrenergic receptor) . Enciprazine dihydrochloride induces drug-related electroencephalogram changes by reducing the average power of δ waves and θ waves, and increasing the average power of α waves and fast β waves. Enciprazine dihydrochloride exhibits anti-aggressive activity, with only weak sedative and ataxic effects. Enciprazine dihydrochloride regulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis. Enciprazine dihydrochloride can be used in research related to anxiety disorders, generalized anxiety syndrome and psychosis .
Cat. No.: HY-181984
Target:
Research Areas:
AGH-194 is a 5-HT7 receptor agonist with a Ki value of 2 nM. AGH-194 activates Gs protein-coupled signaling pathways associated with neuroprotection and neurite outgrowth, and stimulates neurite outgrowth in neuronal cells. AGH-194 reduces cell damage in undifferentiated neuronal cells. AGH-194 can be used in the research of neurodegenerative diseases .
Cat. No.: HY-111193A
CAS No.: 52423-57-1
Synonyms: 3-Chloroprocainamide hydrochloride
Research Areas:
Declopramide (3-Chloroprocainamide) hydrochloride is an orally active, blood-brain barrier-permeable IκBβ/NF-κB inhibitor and chemosensitizer. Declopramide exhibits affinity for rabbit 5-HT3 receptors (5-HT3R) with a Ki value of 3.2 μM. Declopramide inhibits IκBβ degradation, blocks NFκB activation, and induces rapid apoptosis and DNA strand breaks in cancer cells. Declopramide enhances the cytotoxicity induced by Cisplatin (HY-17394) and is also metabolically converted to N-acetyl declopramide. Declopramide can be used in the research of tumors such as brain astrocytoma .
Cat. No.: HY-30234B
CAS No.: 17162-20-8
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Endocrinology
Clemizole sulfate is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC50 value of 1.05-1.34 μM against mouse TRPC5. Clemizole sulfate blocks TRPC1:TRPC5, TRPC3, TRPC4, TRPC6, TRPC7, hERG, hKCNQ1/hKCNE1 and hKv1.5 channels, and activates TRPA1; it modulates 5HT-2B and HTR2A receptors; it inhibits HCV RNA replication, CrtN enzymatic activity, oxidative stress, neuroinflammation, cell apoptosis and bacterial virulence; it maintains blood-brain barrier (BBB) integrity; it enhances DNA repair capacity; it improves cell viability; and it alters cardiac electrophysiological properties. Clemizole sulfate can be used in the research of Dravet syndrome, hepatitis C virus infection, Staphylococcus aureus skin infection, Cisplatin (HY-17394)-induced nephrotoxicity, STXBP1-related diseases, traumatic brain injury and xeroderma pigmentosum type C .
Cat. No.: HY-B0670S
Dihydroergotamine-d3 is the d3-labeled Dihydroergotamine (HY-B0670). Dihydroergotamine (DFN-19) is a blood-brain barrier-permeable semi-synthetic ergot alkaloid, acting as a full agonist of 5-HT1B/1D receptors (Ki values of 0.3 nM and 2.5 nM, respectively; functional IC50 values of 2 nM and 2.2 nM, respectively). Dihydroergotamine inhibits Forskolin (HY-15371)-stimulated cAMP accumulation, possesses α-adrenergic receptor antagonistic activity and weak dopaminergic agonistic activity. It mediates intracranial cerebrovascular contraction, inhibits the release of neuropeptides such as CGRP/substance P, and suppresses neurogenic inflammation by activating 5-HT1B/1D receptors in the trigeminovascular system. Dihydroergotamine binds to the catalytic site of Trypanosoma cruzi trypanothione reductase and exhibits trypanocidal activity in vitro. Dihydroergotamine can be used in studies related to migraine and trypanosome infections .
Cat. No.: HY-59201
CAS No.: 848591-89-9
Research Areas:
A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia .
Cat. No.: HY-46286
CAS No.: 352560-76-0
Synonyms: N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide
Research Areas:
TTFB (N-(4-tert-butyl-1,3-thiazol-2-yl)-3-fluorobenzamide) is a selective, non-competitive zinc-activated channel (ZAC) antagonist. TTFB inhibits Zn 2+- and H +-induced ZAC currents with IC50 values of 3 μM and 8.5 μM, respectively, and has an IC50 of 4.7 μM against spontaneous activity. TTFB shows no significant agonistic, antagonistic or modulatory activity towards representative classical Cys-loop receptors including m5-HT3AR, hα3β4 nAChR, hα1β2γ2S GABAAR and hα1 GlyR. TTFB can be used to investigate the physiological and pathological functions of ZAC.
Cat. No.: HY-180372
CAS No.: 581813-10-7
Research Areas:
CSP-2503 is a potent and selective 5-HT1A receptor agonist , with an EC50 of 0.15 μM and a Ki of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (Ki > 1000 nM), 5-HT4 receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders .
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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
