Every lot is tried & tested in a relevant biological assay.
- Fozard, J.R. (1984) Naunyn Schmiedebergs Arch. Pharmacol. 326, 36.
- Alomone Labs MDL 72222 blocks 5-HT3A receptors expressed in HEK 293T cells.5-HT3A receptor currents elicited with 10 µM 5-HT, delivered every 3 minutes. MDL 72222 (#M-155) was applied 30 seconds before stimulation at 1 µM as indicated and completely inhibited the 5-HT induced current in a dose dependent and reversible manner.
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid tryptophan by the enzyme tryptophan decarboxylase. The 5-HT3 channel is a ligand-gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.
MDL 72222 (Bemesetron) is a synthetic, potent and selective antagonist of the 5-HT3 receptor. MDL 72222 has an effective concentration of 1 nM - 1μM and an ED50 of 9.27 nM. MDL 72222 produces blockade of the Bezold-Jarisch effect of 5-HT in anaesthetized rats. Inhibition of the 5-HT receptor by MDL 72222 is selective since high doses of MDL 72222 fail to alter response to electrical stimulation of efferent vagus nerves. In contrast, MDL 72222 proves only a weak and essentially non-selective antagonist of responses mediated by the 5-HT M-receptor present on the cholinergic nerves of guinea-pig ileum. MDL 72222 does not block smooth muscle contractile responses elicited by oxytocin or mediated through 5-HT D-receptors2. In addition, MDL 72222 also significantly reduces pancreatic enzyme secretion induced by luminal administration of L-trp or melatonin and reverses the effects of 5-HT on amylase secretion3.
MDL 72222 (#M-155) is a highly pure, synthetic, and biologically active compound.
- Anti-5HT1A Receptor (HTR1A) Antibody (#ASR-021)
- Anti-5HT1B Receptor (HTR1B) (extracellular) Antibody (#ASR-022)
- Anti-5HT1D Receptor (HTR1D) (extracellular) Antibody (#ASR-023)
- 2-Methyl-5-hydroxytryptamine hydrochloride (#M-170)
- Mirtazapine (#M-130)
- Mosapride citrate (#M-225)
- PU02 (#P-165)
- Tropanyl-3,5-dimethylbenzoate (#T-135)
- 5-HT3 Receptor Antagonist Explorer Kit (#EK-208)
- 5-HT3 Receptor Modulator Explorer Kit (#EK-209)