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Submit ReviewBIMU 8 is a potent 5-HT4 receptor full agonist (KD = 77 nM and EC50 = 18 nM for wild type 5-HT4 receptors). Binds to receptors in a mechanism different to that of the endogenous ligand 5-HT.
BIMU 8 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 378.9 |
Formula | C19H26N4O2.HCl |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 134296-40-5 |
PubChem ID | 5311028 |
InChI Key | NQYXXIUVFVOJCX-XZPOUAKSSA-N |
Smiles | [H][C@]12CC[C@](CC(NC(N3C(C=CC=C4)=C4N(C(C)C)C3=O)=O)C2)([H])N1C.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 28.42 | 75 | |
DMSO | 37.89 | 100 |
The following data is based on the product molecular weight 378.9. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.64 mL | 13.2 mL | 26.39 mL |
5 mM | 0.53 mL | 2.64 mL | 5.28 mL |
10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
References are publications that support the biological activity of the product.
Pellissier et al (2009) Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors. Mol.Pharmacol. 75 982 PMID: 19168624
Schaus et al (1998) Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: Indazole and benzimidazoline derivatives. J.Med.Chem. 41 1943 PMID: 9599243
If you know of a relevant reference for BIMU 8, please let us know.
Keywords: BIMU 8, BIMU 8 supplier, BIMU8, 5-hydroxytryptamine, 4, 5HT4, receptors, 5-HT4, agonists, serotonin, serotonergic, Receptors, 4374, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for BIMU 8 include:
House et al (2015) Genetic variation in HTR4 and lung function: GWAS follow-up in mouse. PLoS One 29 323 PMID: 25342126
Daniel et al (2021) Serotonin receptor 4 regulates hippocampal astrocyte morphology and function. Glia 69 872-889 PMID: 33156956
Carolina da Silveira et al (2021) Respiratory depression and analgesia by opioid drugs in freely behaving larval zebrafish. Elife 10 PMID: 33720013
Andre et al (2021) The 5-HT4 receptor interacts with adhesion molecule L1 to modulate morphogenic signaling in neurons. J Cell Sci 134 PMID: 33536244
James L et al (2018) Pharmacologic assessment of bovine ruminal and mesenteric vascular serotonin receptor populations. J Anim Sci 96 1570-1578 PMID: 29471490
Wang et al (2016) 5-HTR3 and 5-HTR4 located on the mitochondrial membrane and functionally regulated mitochondrialfunctions Scientific Reports 6 37336 PMID: 27874067
Lucie P et al (2013) Serotonin type 4 receptor dimers. Methods Cell Biol 117 123-39 PMID: 24143975
Do you know of a great paper that uses BIMU 8 from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.