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Talipexole dihydrochloride

B-HT 920
An Antagonist of 5-HT3 Channel, an Agonist of D2 Dopamine Receptor and α2-Adrenoceptor
Cat #: B-140
Alternative Name B-HT 920
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 282.23
    Purity: >98%
    Effective concentration 0.3-300 nM.
    Structure
    Chemical name 6-prop-2-enyl-4,5,7,8-tetrahydro-[1,3]thiazolo[4,5-d]azepin-2-amine;dihydrochloride.
    Molecular formula C10H15N3S•2HCl.
    CAS No.: 36085-73-1.
    Activity B-HT 920 is a blocker of 5-HT3 channels1. It is also an agonist of D2 dopamine receptors and α2-adrenoceptors.
    References-Activity
    1. Nishio, H. et al. (1996) Gen. Pharmacol. 27, 779.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Talipexole dihydrochloride (B-HT 920) blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Alomone Labs Talipexole dihydrochloride (B-HT 920) blocks 5-HT3A receptors expressed in HEK 293T cells. 
      Currents were elicited by 10 µM 5-HT, delivered every 3 minutes. Talipexole dihydrochloride (#B-140) was applied 30 seconds before stimulation at 10 and 100 µM, as indicated and inhibited the 5-HT induced current in a dose-dependent and reversible manner.
    References - Scientific background
    1. Nishio, H. et al. (1996) Gen. Pharmacol. 27, 779.
    2. Clarke, P.B. et al. (1990) Br. J. Pharmacol. 99, 509.
    3. Plosker, G.L. and Benfield, P. (1997) CNS Drugs 7, 410.
    4. Inoue, Y. et al. (1999) Psychiatry Clin. Neurosci. 53, 283.
    Scientific background

    Talipexole is an azepine derivative, and acts as an agonist of D2 dopamine pre- and postsynaptic receptors, as well as an α2-adrenoceptor agonist and 5-HT3 receptor antagonist1.

    The purpose of Talipexole is to increase dopamine activity in the central nervous system. It inhibits electrically evoked release of dopamine through activation of D2 synaptic autoreceptors located on dopaminergic terminals. It also causes release of acetylcholine and noradrenalin2,3.

    Talipexole has been established in a number of clinical trials as an anti-Parkinsonian agent. These trials showed significant improvement in motor activity and in other parkinsonian symptoms including akinesia, rigidity, tremor and gait disturbances. There are several side effects caused by this drug such as drowsiness, dizziness, hallucinations, gastrointestinal discomfort, nausea and loss of appetite3.

    In addition, talipexole is also expected to be beneficial for the treatment of periodic leg movement disorder and restless leg syndrome4.

    Target 5-HT3, D2 dopamine, α2-adrenoceptor receptors
    Last update: 23/08/2020

    Talipexole dihydrochloride (#B-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information