This product is freeze dried. All water molecules have been removed.
Every lot is tried & tested in a relevant biological assay.
- Nakamura, Y. et al. (2013) J. Neurochem. 125, 7.
- Alomone Labs Topotecan hydrochloride blocks 5-HT3A receptors expressed in HEK 293T cells.5-HT3A receptor currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Topotecan hydrochloride (#T-160) was applied 30 seconds before stimulation at 10, 100 and 200 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.
Topotecan (Hycamtin) is a synthetic, potent and selective antagonist of the 5-HT3A channel derived from the plant alkaloid Camptothecin. Topotecan has an effective concentration of 10-200 μM and an IC50 of 114.1 μM for the 5-HT3A receptor.
Interestingly, in addition to its inhibitory effect on 5-HT3 receptors, Topotecan can also potentiate the 5-HT receptor. Topotecan’s dual modulation properties depend on the receptor’s subunit composition. Topotecan causes current enhancement in receptors containing the 5-HT3B subunit through means of increased 5-HT affinity to its receptor or a rise in the receptor associated ion channel’s probability of opening. Thus, Topotecan might be effective in distinguishing between different 5-HT3A and 5-HT3B receptors2.
In addition to its function as a 5-HT3 antagonist Topotecan is used as an anti-cancer drug in various malignancies. Topotecan’s chemotherapeutic effect is achieved through inhibition of Topoisomerase-1, inducing DNA damage at transcriptionally active genomic areas3.
Topotecan hydrochloride (#T-160) is a highly pure, synthetic, and biologically active compound.
- Topotecan (#T-161)
- Anti-5HT3A Receptor (HTR3A) Antibody (#ASR-031)
- Anti-5HT3B Receptor (HTR3B) (extracellular) Antibody (#ASR-032)
- Granisetron hydrochloride (#G-105)
- Tropisetron hydrochloride (#T-125)
- Ondansetron hydrochloride (#O-110)
- Azasetron hydrochloride (#Y-100)
- SDZ 205-557 hydrochloride (#S-145)
- VUF 10166 (#V-115)
- 3-AQC (#A-205)
- m-Chlorophenylbiguanide hydrochloride (#M-160)
- 5-HT3 Receptor Antagonist Explorer Kit (#EK-208)
- 5-HT3 Receptor Modulator Explorer Kit (#EK-209)