serotonin 3 receptor

Granisetron hydrochloride (Granisetron HCl) is a serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.

Tropisetron hydrochloride (Tropisetron HCl) is the hydrochloride salt form of tropisetron, a selective, competitive serotonin 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist, with antinauseant and antiemetic activities.

RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole) is a selective agonist of 5-HT1A and 5-HT1B receptors.

(2-methylpropyl)({[3-(trifluoromethyl)phenyl]methyl})amine is a selective serotonin receptor agonist that specifically targets 5-HT2A and 5-HT2C receptors. It has been used to study the role of serotonin in a variety of physiologic and pathologic conditions.

3-(2-aminopropyl)phenol hydrochloride is a phenethylamine analog used as a molecular structural unit. It is a psychoactive drug that is a partial agonist at several serotonin receptors, including 5-HT1A, 5-HT1B, and 5-HT2C, as well as an antagonist at the 5-HT2A receptor.

2-(5,7-dichloro-1H-indol-3-yl)ethan-1-amine is an indoleamine compound that is structurally similar to serotonin. It is a selective agonist at the 5-HT2A receptor and has potential applications in neuroscience.

AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. It inhibits twitch contraction of the ileum and colon with IC50 values of 45.71 nM and 0.076 nM, respectively. AM9405 significantly slowed mouse intestinal motility under physiological conditions and reversed hypermotility, reducing pain in mouse models that mimic symptoms of functional GI disorders, such as stress-induced diarrhea and writhing test.

Ondansetron hydrochloride dihydrate (GR 38032) is a competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

HDAC6-IN-49 (Compound 3) is an inhibitor of HDAC, with IC50 values of 0.012 and 0.735 µM against HDAC6 and HDAC1, respectively. Additionally, it inhibits MAO-B, cholinesterase (ChE), histamine receptor (H3R), and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective effects in SH-SY5Y cells and enhances cognitive functions and motor abilities in fruit fly models of Parkinson's disease and C. elegans models of Alzheimer's disease.

25CN-NBMD is a highly selective serotonin 5-HT2A receptor (5-HT2AR) agonist developed to investigate the expression and function of 5-HT2AR. Structural modifications were made at the 2' and 3' positions of 25CN-NBMD, and studies revealed these changes are crucial for 5-HT2AR activity. This compound effectively induces characteristic responses associated with 5-HT2AR activation.

Triazolomethylindole-3-acetic acid is a metabolite of Rizatriptan, which acts as an agonist for the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D.

Granisetron, a serotonin receptor (5HT-3 selective) antagonist, is used as an antinauseant and antiemetic for cancer chemotherapy.

Indisetron Dihydrochloride is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.

JNJ-28583867 is an inhibitor of histamine H(3) receptor antagonist and serotonin reuptake.

Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM). Facinicline hydrochloride improves cognition and sensorimotor gating in rodents.

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2 1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3antagonist palonosetron .1It is also a potential impurity in palonosetron preparations.2Palonosetron N-oxide is a degradation product formed by exposure to oxidative stress. 1.Stoltz, R.A., Cyong, J.-C., Shah, A., et al.Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjectsJ. Clin. Pharmacol.44(5)520-531(2004) 2.Vishnu Murthy, M., Srinivas, K., Kumar, R., et al.Development and validation of a stability-indicating LC method for determining palonosetron hydrochloride, its related compounds and degradation products using naphthalethyl stationary phaseJ. Pharm. Biomed. Anal.56(2)429-435(2011)

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) , a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine hydrochloride also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].

Izuforant (JW1601) (Compound 24) exhibits potent anti-inflammatory and anti-pruritic activities, with a binding affinity for human serotonin 3 receptor (h5-HT3R) and an IC50 value of 9.1 μM. It is also an orally active antagonist of histamine H4 receptor (H4R), showing an IC50 value of 36 nM against human H4R [1] [2].

1. 8-Gingerol has antioxidant activity. 2. 8-Gingerol has antimycobacterial activity. 3. 8-Gingerol could be used as an effective skin-whitening agent. 4. 8-Gingerol shows antipyretic and anti-inflammation characteristics. 5. 8-Gingerol seems to be effect

Indisetron is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.

Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in rat brain and peripheral tissues. It reduces isolation-induced aggressive behavior and inhibits electrical foot-shock stimulation-induced belligerence in mice when administered at doses ranging from 3 to 10 mg kg. Maprotiline also reduces aggressive behavior in rhesus monkeys housed in groups. Formulations containing maprotiline have been used in the treatment of depression and anxiety.

FK-1052 HCl is a serotonin 3 & 4 dual receptor antagonist.