A 5-HT3 receptor antagonist
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MDL 72222

Item No. 43507

Technical Information
Formal Name
3,5-dichloro-benzoic acid, (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
CAS Number
40796-97-2
Synonyms
  • Bemesetron
Molecular Formula
C15H17Cl2NO2
Formula Weight
Purity
≥98%
Formulation
A solid
Ethanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(C1=CC(Cl)=CC(Cl)=C1)O[C@H]2C[C@]3([H])N([C@](CC3)([H])C2)C
InChi Code
InChI=1S/C15H17Cl2NO2/c1-18-12-2-3-13(18)8-14(7-12)20-15(19)9-4-10(16)6-11(17)5-9/h4-6,12-14H,2-3,7-8H2,1H3/t12-,13+,14+
InChi Key
MNJNPLVXBISNSX-WDNDVIMCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MDL 72222 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (IC50 = 0.82 nM).1 It is selective for 5-HT3 over 5-HT1 and 5-HT2 receptors and α1-, α2-, and β-adrenergic receptors (IC50s = >10,000 nM for all), as well as the histamine H1 receptor (IC50 = 3,800 nM). Intraplantar administration of MDL 72222 (10 and 100 µg/animal) inhibits formalin-induced paw licking and complete Freund’s adjuvant-induced decreases in paw withdrawal latency in mice.2 It inhibits emesis induced by cisplatin (Item No. 13119) in dogs when administered at a dose of 0.5 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fozard, J.R. MDL 72222: A potent and highly selective antagonist at neuronal 5-hydroxytryptamine receptors. Naunyn Schmiedebergs Arch. Pharmacol. 326(1), 36-44 (1984).

    2. Giordano, J., and Rogers, L.V. Peripherally administered serotonin 5-HT3 receptor antagonists reduce inflammatory pain in rats. Eur. J. Pharmacol. 170(1-2), 83-86 (1989).

    3. Fukui, H., Yamamoto, M., and Sato, S. Vagal afferent fibers and peripheral 5-HT3 receptors mediate cisplatin-induced emesis in dogs. Jpn. J. Pharmacol. 59(2), 221-226 (1992).