B-HT 920 |
Catalog No.GC14491
One-Click Copy Product Info
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A potent agonist of D2 receptors
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 36085-73-1
Sample solution is provided at 25 µL, 10mM.
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B-HT 920, marketed as talipexole in Japan, is a full agonist at both pre- and postsynaptic D-2 dopamine receptors agonist and α2-adrenergic receptor agonist. In addition, it is a 5-HT3 receptor antagonist in both rat cortical and intestinal membrane fractions with Ki values of 0.35 μM and 0.22 μM, respectively. [1, 2]
Adrenergic receptor and dopamine receptors are distributed in many cells. α-adrenergic receptor can be divided into two categories, α1 and α2 adrenergic receptors, which involve in functions of smooth muscles and veins. Dopamine receptors are widely distributed in the brain and control neural signaling that modulates many important behaviors
By measuring the DOPA in mice corpus striatum, effect of B-HT 920 on the presynaptic D-2 receptors was studied in mice treated with gamma-butyrolactone (GBL, 750 mg/kg i.p.). B-HT 920 inhibited the synthesis of DA to approximately the same extent from 0.1 to 3mg/kg. Haloperidol (2 mg/kg) completely inhibited the effects of 0.1 to 1 mg/kg B-HT 920. Furthermore, B-HT 920 on postsynaptic DA receptors were studied in mice in which the DA stores had been depleted by reserpine. The motor activity of three groups of mice was recorded by the use of electronic motility meters. The motor activity was enhanced by apomorphine. Combined treatment with B-HT920 (0.1 mg/kg) and SKF38393 produced an even greater increase in the motor activity of the reserpine-treated mice. Moreover, B-HT 920 at a dose 1 mg/ kg had a persistent effect on mice. A study was performed relating the involvement of α-adrenergic receptors in the cardiovascular responses to intracerebroventricular (ICV) injection of B-HT 920. In sham-operated rats, B-HT 920 (10–60 mg) caused cardiovascular activities including increased blood pressure and bradycardia. However, in sinoaortic-denervated rats, after the pressor response, there was a decline in blood pressure observed. The responses to this agent were greater in sinoaortic-denervated rats than in sham-operated subjects. B-HT 920 was assessed in combination of other active agents. Treatment with the α2-adrenergic receptor antagonist yohimbine (30 mg), the imidazoline receptor antagonist idazoxan (15 mg) and the α1A -adrenergic receptor antagonist 5-methylurapidil (15 mg) blocked the revesed effects of B-HT 920 (30 mg). The α1-adrenergic receptor antagonist prazosin (15mg) and the α1B -adrenergic receptor antagonist chloroethylclonidine (100 mg) did not alter the responses to B-HT 920. [1, 3]
References:
[1] Andén, N-E., and M. Grabowska-Andén. "B-HT 920 is a full agonist at both pre-and postsynaptic D-2 dopamine receptors." Journal of Neural Transmission/General Section JNT 79.3 (1990): 209-214.
[2] Nishio, Hiroaki, et al. "5-HT 3 receptor blocking properties of the antiparkinsonian agent, talipexole." General Pharmacology: The Vascular System 27.5 (1996): 779-785.
[3] Ricci, Daniel, and Carlos Alberto Taira. "Adrenoceptor involvement in the cardiovascular responses to B-HT 920 in sinoaortic denervated rats." General Pharmacology: The Vascular System 32.1 (1999): 29-34.
| Cas No. | 36085-73-1 | SDF | |
| Chemical Name | 6-allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride | ||
| Canonical SMILES | C=CCN1CCC2=C(SC(N)=N2)CC1.Cl.Cl | ||
| Formula | C10H17Cl2N3S | M.Wt | 282.23 |
| Solubility | PBS (pH 7.2): 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5432 mL | 17.716 mL | 35.4321 mL |
| 5 mM | 708.6 μL | 3.5432 mL | 7.0864 mL |
| 10 mM | 354.3 μL | 1.7716 mL | 3.5432 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)