Overview
- Eglen, R.M. et al. (1993) Br. J. Pharmacol. 108, 376.
Alomone Labs SDZ 205-557 hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells.Currents were elicited by 10 µM 5-HT, delivered every 3 minutes. SDZ 205-557 hydrochloride (#S-145) was applied 30 seconds before stimulation at 1 and 10 µM, as indicated and inhibited the 5-HT induced current in a dose-dependent and reversible manner.
- Eglen, R.M. et al. (1993) Br. J. Pharmacol. 108, 376.
- Fayyaz, M. and Lackner, J.M. (2008) Ther. Clin. Risk Manag. 4, 41.
- McMahon, L.R. and Cunningham, K.A. (1999) J. Pharmacol. Exp. Ther. 291, 300.
SDZ 205-557 is a potent 5-HT3 and 5-HT4 receptor antagonist with a greater affinity for 5-HT4 receptor with a Ki value of 10.6 nM3. It lacks affinity for other 5-HT receptors. SDZ 205-557 is thus suggested to be used as a useful ligand to characterize and define the 5HT-4 receptor. SDZ 205-557 has the ability to cross the blood brain barrier and has a short duration of action that may complicate its use in vivo1,3.
5-HT3 and 5HT4 are members of the serotonin-gated and G protein coupled receptor superfamily respectively. 5-HT3 receptors are expressed throughout the central and peripheral nervous systems. High levels of 5-HT4 receptors can be found in the olfactory system, striatum, hippocampus, and substantia nigra2,3.
SDZ 205-557 hydrochloride (#S-145) is a highly pure, synthetic, and biologically active compound.
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