B-HT 920 DIHYDROCHLORIDE
B-HT 920 DIHYDROCHLORIDE Basic information
- Product Name:
- B-HT 920 DIHYDROCHLORIDE
- Synonyms:
-
- 5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azepin-2-amineDihydrochloride,6-Allyl-2-amino-5,6,7,8-tetrahydro-4
- B-HT920dihydrochlorideTalipexole
- 5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azepin-2-amine Dihydrochloride, 6-Allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine Dihydrochloride
- Talipexole, 5,6,7,8-Tetrahydro-6-(2-propenyl)-4H-thiazolo[4,5-d]azepine-2-amine dihydrochloride
- 5,6,7,8-Tetrahydro-6-(2-propen-1-yl)-4H-thiazolo[4,5-d] azepin-2-amine dihydrochloride
- talipexole hydrochloride
- 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine-2-amine dihydrochloride
- 2-Amino-6-allyl-4,5,7,8-tetrahydro-6H-thiazolo(5,4-D)azepin-dihydrochlorid [german]
- CAS:
- 36085-73-1
- MF:
- C10H17Cl2N3S
- MW:
- 282.23
- Product Categories:
-
- Adrenoceptor
- All Inhibitors
- Inhibitors
- Intermediates & Fine Chemicals
- Neurochemicals
- Pharmaceuticals
- Mol File:
- 36085-73-1.mol
B-HT 920 DIHYDROCHLORIDE Chemical Properties
- Melting point:
- 245°C dec.
- storage temp.
- Desiccate at RT
- solubility
- H2O: >20 mg/mL
- form
- solid
- color
- off-white
MSDS
- Language:English Provider:SigmaAldrich
B-HT 920 DIHYDROCHLORIDE Usage And Synthesis
Description
B-HT 920 is a potent agonist of dopamine 2 (D2) receptors (Ki = 5.8 nM) that shows selectivity for D2 over D3 and D4 receptors. It has neuroprotective and regenerative effects in animal models of Parkinson’s disease. B-HT 920 is also an agonist of α2-adrenergic receptors and an antagonist of serotonin-3 (5-HT3; Ki = 0.35 μM) receptors.
Chemical Properties
B-HT 920 DIHYDROCHLORIDE is Light Yellow Solid
Uses
B-HT 920 DIHYDROCHLORIDE is an alpha 2-Adrenoceptor and dopamine D2-receptor agonist. Used as an antiparkinson reagent
Definition
ChEBI: Talipexole dihydrochloride is an azepine.
Biological Activity
Dopamine D 2 receptor agonist, α 2 -adrenoceptor agonist and 5-HT 3 receptor antagonist. Displays antiParkinsonian activity.
References
[1] FRANCIS K. MAINA Tiffany A M. Functional Fast Scan Cyclic Voltammetry Assay to Characterize Dopamine D2 and D3 Autoreceptors in the Mouse Striatum[J]. ACS Chemical Neuroscience, 2010, 1 6: 450-462. DOI: 10.1021/cn100003u
[2] RICHARD E. MEWSHAW. New Generation Dopaminergic Agents. 1. Discovery of a Novel Scaffold Which Embraces the D2 Agonist Pharmacophore. Structure?Activity Relationships of a Series of 2-(Aminomethyl)chromans[J]. Journal of Medicinal Chemistry, 1997, 40 26: 4235-4256. DOI: 10.1021/jm9703653
[3] G S ROBERTSON. In vivo comparisons of the effects of quinpirole and the putative presynaptic dopaminergic agonists B-HT 920 and SND 919 on striatal dopamine and acetylcholine release.[J]. Journal of Pharmacology and Experimental Therapeutics, 1993, 264 3: 1344-1351.
[4] KITAMURA Y. [Dopaminergic neuroprotection and reconstruction of neural network tiara].[J]. Yakugaku zasshi?: Journal of the Pharmaceutical Society of Japan, 2010, 130 10: 1263-1272. DOI: 10.1248/yakushi.130.1263
[5] HIROAKI NISHIO . 5-HT3 receptor blocking properties of the antiparkinsonian agent, talipexole[J]. General Pharmacology-the Vascular System, 1996, 27 5: Pages 779-785. DOI: 10.1016/0306-3623(95)02125-6
[6] DANIEL RICCI Carlos A T. Adrenoceptor Involvement in the Cardiovascular Responses to B-HT 920 in Sinoaortic Denervated Rats[J]. General Pharmacology-the Vascular System, 1999, 32 1: Pages 29-34. DOI: 10.1016/s0306-3623(98)00018-4
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