Alosetron ((Z) -2-butenedioate)

Alosetron (GR 68755) (Z) -2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z) -2-butenedioate is used for the research of irritable bowel syndrome (IBS) . Alosetron (Z) -2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z) -2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects[1][2].

Product Specifications

CAS Number

[122852-43-1]

Product Name Alternative

GR 68755 ((Z) -2-butenedioate) ; GR 68755X ((Z) -2-butenedioate)

UNSPSC

12352005

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/alosetron-_z_-2-butenedioate.html

Solubility

10 mM in DMSO

Smiles

O=C(C(C1=C2C=CC=C1)=C(N2C)CC3)N3CC4=C(NC=N4)C.O=C(/C=C\C(O)=O)O

Molecular Formula

C21H22N4O5

Molecular Weight

410.42

References & Citations

[1]Balfour JA, Goa KL, Perry CM. Alosetron. Drugs. 2000;59 (3) :511-520.|[2]Motavallian A, et al. Anti-inflammatory effects of alosetron mediated through 5-HT3 receptors on experimental colitis. Res Pharm Sci. 2019;14 (3) :228-236.