| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Other Sizes |
Purity: ≥98%
Talipexole dihydrochloride (also known as B-HT920, Domnin, B-HT-920 dihydrochloride) is a novel and potent dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays anti-parkinsonian activity. Boehringer Ingelheim first brought talipexole to the Japanese market in 1996 with the goal of treating Parkinson's disease. As of December 2014 it was not approved for marketing in the US nor in Europe. Talipexole is a D2 dopamine receptor agonist and interacts both pre- and post-synaptic receptors. A α2-adrenergic agonist, it is as well. The most common adverse effects include lightheadedness, sleepiness, hallucinations, and mild gastrointestinal issues. The Japanese Ministry of Health, Labour, and Welfare ordered Boehringer to include a warning on the label about the possibility of sudden onset of sleep in 2008.
| Targets |
Dopamine D2-like receptor agonist (Ki = 144 nM for displacement of [³H]spiperone binding in rat striatal membranes)
α2-adrenoceptor agonist 5-HT3 receptor antagonist Dopamine D1-like receptor agonist (when combined with chloro-APB, SKF 82958) [2] |
|---|---|
| ln Vitro |
Displacement activity on [³H]spiperone binding to rat striatal membranes with a Ki of 144 nM, indicating dopamine D2-like receptor affinity. [2]
Electrophysiological studies in cats and rats show that talipexole acts on caudate neurons as a dopamine D2-like receptor agonist. [2] Induces yawning behavior in rats, mediated through dopamine D2 receptors. [2] |
| ln Vivo |
Intravenous administration of 30 mcg/kg of talixol hydrochloride (B-HT 920) to cats initially causes an increase in blood pressure, followed by a long-lasting decrease in blood pressure and heart rate. Intracisternal injection of 10 μg/kg talixol dihydrochloride (B-HT 920) promotes vagus nerve-mediated reflex bradycardia in dogs with beta-adrenoceptor blockade and angiotensin injection.
In MPTP-induced hemiparkinsonian monkeys, talipexole induced contraversive rotation in a dose-dependent manner up to 32 μg/kg i.m., with significant improvement in motor movements and hand movements of the affected limb. [2] At 56 and 100 μg/kg i.m., talipexole produced sedation, reducing locomotor activity without extrapyramidal side effects. [2] Combination with chloro-APB (SKF 82958) showed synergistic effects (additive or potentiation) on contraversive rotation. [2] Showed antiparkinsonian activity in MPTP-treated marmosets, improving motor movements. [2] |
| Animal Protocol |
Five adult female Macaca nemestrina monkeys with chronic MPTP-induced hemiparkinsonism were used. [2]
MPTP was slowly infused unilaterally into one common carotid artery at a total dose of approximately 0.6 mg/kg. [2] Animals were housed in standard individual cages with a light/dark cycle and enriched environment. [2] Drugs were administered intramuscularly (i.m.) in logarithmic doses, usually on Thursdays. [2] Behavior was recorded via video cameras for 30 min after vehicle and 2+ hours after drug administration. [2] Circling behavior (ipsiversive and contraversive turns) was scored from videotapes by two blinded observers. [2] |
| ADME/Pharmacokinetics |
After oral administration, taribexol is well absorbed and can rapidly cross the blood-brain barrier. [2]
Its pharmacokinetic properties are similar to those of pramipexol. [2] |
| Toxicity/Toxicokinetics |
In hemilateral Parkinson's monkeys, intramuscular injection of talipexole at doses of 56 and 100 μg/kg induced sedation without extrapyramidal side effects. [2] Some animals showed reduced food and water intake after administration of talipexole, but no vomiting was observed. [2] The sedative effect may be related to stimulation of α2-adrenergic receptors and dopamine D2 autoreceptors. [2]
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| References | |
| Additional Infomation |
Talipexole dihydrochloride is an azathenazone drug. Taribexol is a potent dopamine D2-like receptor agonist with the properties of both an α2-adrenergic receptor agonist and a weak 5-HT3 receptor antagonist. [2] It has been used in controlled clinical trials for Parkinson's disease. [2] The combined use of dopamine D1 and D2 receptor agonists has shown synergistic anti-Parkinson's disease effects. [2] The sedative effect of taribexol may be related to brain damage in Parkinson's disease models. [2]
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| Molecular Formula |
C10H17CL2N3S
|
|---|---|
| Molecular Weight |
282.23308
|
| Exact Mass |
281.052
|
| Elemental Analysis |
C, 42.56; H, 6.07; Cl, 25.12; N, 14.89; S, 11.36
|
| CAS # |
36085-73-1
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| Related CAS # |
Talipexole; 101626-70-4
|
| PubChem CID |
104870
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
364.6ºC at 760mmHg
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| Melting Point |
245ºC dec.
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| Flash Point |
174.3ºC
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| LogP |
3.435
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
|
| Heavy Atom Count |
16
|
| Complexity |
210
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
NC1=NC2=C(CCN(CC2)CC=C)S1.Cl.Cl
|
| InChi Key |
DPQAXNSOFFYKDS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15N3S.2ClH/c1-2-5-13-6-3-8-9(4-7-13)14-10(11)12-8;;/h2H,1,3-7H2,(H2,11,12);2*1H
|
| Chemical Name |
6-prop-2-enyl-4,5,7,8-tetrahydro-[1,3]thiazolo[4,5-d]azepin-2-amine;dihydrochloride
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| Synonyms |
Talipexole HCl; Talipexole dihydrochloride; Domnin; B-HT 920; B-HT-920; B-HT920
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~88.58 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5432 mL | 17.7160 mL | 35.4321 mL | |
| 5 mM | 0.7086 mL | 3.5432 mL | 7.0864 mL | |
| 10 mM | 0.3543 mL | 1.7716 mL | 3.5432 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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