[CAS NO. 36085-73-1] Talipexoledihydrochloride
PRODUCTS SPECIFICATIONS [36085-73-1]
DESCRIPTION [36085-73-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 282.23 |
| Molecular Formula | C10H17Cl2N3S |
| SMILES | NC1=NC2=C(CCN(CC2)CC=C)S1.Cl.Cl |
Summary
Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
IC50 & Target
|
α adrenergic receptor
|
α2 25 nM (IC 50 ) |
D 2 Receptor
|
5-HT 3 Receptor
|
In Vivo
Intravenous injection of 30 micrograms/kg of Talipexole dihydrochloride (B-HT 920) into cats lead initially to an increase in blood pressure and then to a long-lasting decrease in blood pressure and heart rate. Vagally mediated reflex bradycardia elicited by angiotensin injection in beta-adrenoceptor-blocked dogs was facilitated by intracisternal injection of 10 micrograms/kg Talipexole dihydrochloride (B-HT 920).
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL ( 88.58 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [1] Ricci and Taira Adrenoceptor involvement in the cardiovascular responses to B-HT 920 in sinoaortic denervated rats. Gen.Pharmacol. (1999)32 29.
- [2] Eur J Pharmacol. 1997 May 1;325(2-3):137-44.
- [3] Kohno Y, Fukuzaki K, Kitahara K, Koja T.Anti-tremor activity of talipexole produced by selective dopamine D2 receptor stimulation in cynomolgus monkeys with unilateral lesions in the ventromedial tegmentum.Eur J Pharmacol. 1997 Jan 29;319(2-3):197-205.
- [4] Momiyama T, Sasa M, Takaori S.Inhibition by talipexole, a thiazolo-azepine derivative, of dopaminergic neurons in the ventral tegmental area.Life Sci. 1991;49(7):535-43.
- [5] Nishikawa T, Yamada S, Tsuda A, Tanaka M, Koga I, Uchida Y.Chronic treatment with talipexole dihydrochloride on abnormal involuntary movement in humans.Clin Neuropharmacol. 1990 Jun;13(3):259-63.
- [6] Robertson, G.S., et al., 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 Pharmacol Exp Ther, 1993. 264(3): p. 1344-51.
Synonyms
