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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
62 Results for "
5-HT responses
" in MedChemExpress (MCE) Product Catalog:
Products (62)
62 Results for "5-HT responses" in MCE Product Catalog:
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Plant Xanthones Guttiferae Extract Metabolic Disease Phenols Polyphenols Disease Research Fields Garcinia mangostana Linn. Extract
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Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .
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Uncaria rhynchophylla (Miq.) Miq. ex Havil. Extract Alkaloids Plant Indole Alkaloids Rubiaceae Extract
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1 Cited Publications
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VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM .
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1 Cited Publications
Cat. No.: HY-P1441A
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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-W010973
CAS No.: 61-47-2
Category:
Natural Products Monophenols Metabolic Disease Phenols Endogenous metabolite Disease Research Fields
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Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .
Synonyms: GR 205171A
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Vofopitant dihydrochloride (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant dihydrochloride blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant dihydrochloride exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant dihydrochloride improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant dihydrochloride can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
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ALD-52 (1-Acetyl-LSD) is a prodrug for LSD. ALD-52 shows an affinity to 5-HT1A, 5-HT2A and 5-HT2C with a sub>D values of 1054, 174 and 10.2 nM, respectively. ALD-52 is converted to LSD and induces a head-twitch response (HTR) in vivo. ALD-52 can be used for hallucinogen research .
Cat. No.: HY-106584
CAS No.: 89419-40-9
Synonyms: Clospipramine
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Mosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia .
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BRL-15572 dihydrochloride is a selective antagonist of h5-HT1D, displays high affinity for h5-HT1D receptors. BRL-15572 dihydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .
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LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration .
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H-9 Dihydrochloride is a PKA (protein kinase) inhibitor. H-9 Dihydrochloride (10 μM) significantly reduces the excitatory response to 5-HT. H-9 Dihydrochloride also has a direct effect on pharyngeal activity. H-9 Dihydrochloride inhibits signal-transduction and cell growth in EGF (epidermal growth factor)-dependent epithelial cell lines .
Cat. No.: HY-W743888
CAS No.: 65527-61-9
Synonyms: 6-Allyl-6-nor-LSD
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AL-LAD is a 5-HT2A receptor ligand with rat Ki values of 8.1 nM and 3.4 nM. AL-LAD mediates behavioral responses characteristic of serotonergic psychedelics. AL-LAD induces the head-twitch response in male C57BL/6J mice in an inverted-U-shaped dose-dependent manner. AL-LAD exhibits LSD-like behavioral effects in male C57BL/6J mice .
Synonyms: GR 205171
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Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
Cat. No.: HY-178760
CAS No.: 3136748-24-5
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TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against human 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression) .
Cat. No.: HY-156807
CAS No.: 210751-39-6
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LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
Cat. No.: HY-135439
CAS No.: 135938-17-9
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SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .
Cat. No.: HY-118835
CAS No.: 56775-88-3
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Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .
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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
