Talipexole HCl | B-HT 920 | CAS#36085-73-1 | CAS#101626-70-4 | Dopamine Agonist

MedKoo Cat#: 326699 | Name: Talipexole HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Talipexole, also known as B-HT920 and Domnin, is a dopamine agonist that is marketed as a treatment for Parkinson's Disease in Japan by Boehringer Ingelheim; it was introduced in 1996. 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. It also is an α2-adrenergic agonist. The main side effects are drowsiness, dizziness, hallucinations and minor gastrointestinal complaints. In 2008 the Japanese Ministry of Health, Labour, and Welfare mandated that Boehringer add a warning to the label concerning the risk of sudden onset of sleep.

Chemical Structure

Talipexole HCl

CAS#36085-73-1 (2HCl)

Theoretical Analysis

MedKoo Cat#: 326699

Name: Talipexole HCl

CAS#: 36085-73-1 (2HCl)

Chemical Formula: C10H17Cl2N3S

Exact Mass:

Molecular Weight: 282.23

Elemental Analysis: C, 42.56; H, 6.07; Cl, 25.12; N, 14.89; S, 11.36

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 Weeks
50mg	USD 1,250.00	2 Weeks

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Related CAS #

36085-73-1 (2HCl) 101626-70-4 (free base)

Synonym

B-HT 920, B-HT-920, B-HT920, Talipexole HCl, Talipexole dihydrochloride, Domnin

IUPAC/Chemical Name

6-Allyl-2-amino-5,6,7,8-tetrahydro-4H-thiazolo(4,5-d)azepine dihydrochloride

InChi Key

DPQAXNSOFFYKDS-UHFFFAOYSA-N

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

SMILES Code

NC(S1)=NC2=C1CCN(CC=C)CC2.[H]Cl.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 282.23 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Gómez-Sánchez R, Bravo-San Pedro JM, Niso-Santano M, Soler G, Fuentes JM, González-Polo RA. The neuroprotective effect of talipexole from paraquat-induced cell death in dopaminergic neuronal cells. Neurotoxicology. 2010 Dec;31(6):701-8. doi: 10.1016/j.neuro.2010.07.005. Epub 2010 Jul 29. PubMed PMID: 20673835. 2: Zhang TT, Song M, Hang TJ, Xu XF, Wen AD, Yang L, Jia L. Pharmacokinetic profile of talipexole in healthy volunteers is not altered when it is co-administered with Madopar (co-beneldopa). J Clin Pharm Ther. 2009 Jun;34(3):345-54. doi: 10.1111/j.1365-2710.2008.01008.x. PubMed PMID: 19646081. 3: Gobert A, Di Cara B, Cistarelli L, Millan MJ. Piribedil enhances frontocortical and hippocampal release of acetylcholine in freely moving rats by blockade of alpha 2A-adrenoceptors: a dialysis comparison to talipexole and quinelorane in the absence of acetylcholinesterase inhibitors. J Pharmacol Exp Ther. 2003 Apr;305(1):338-46. PubMed PMID: 12649387. 4: Kakimura J, Kitamura Y, Takata K, Kohno Y, Nomura Y, Taniguchi T. Release and aggregation of cytochrome c and alpha-synuclein are inhibited by the antiparkinsonian drugs, talipexole and pramipexole. Eur J Pharmacol. 2001 Apr 6;417(1-2):59-67. PubMed PMID: 11301060. 5: Osumi E, Imai T. [Increase in serum creatine phosphokinase following administration of talipexole hydrochloride]. Rinsho Shinkeigaku. 2000 Oct;40(10):1041-3. Japanese. PubMed PMID: 11296371. 6: Takata K, Kitamura Y, Kakimura J, Kohno Y, Taniguchi T. Increase of bcl-2 protein in neuronal dendritic processes of cerebral cortex and hippocampus by the antiparkinsonian drugs, talipexole and pramipexole. Brain Res. 2000 Jul 28;872(1-2):236-41. PubMed PMID: 10924701. 7: Minami M, Kohno Y, Endo T, Nemoto M, Ogawa T, Ihira E, Hamaue N, Hirafuji M. Differential effects of talipexole and bromocriptine on serotonin release from rat intestinal tissues--an in vitro study of the emetic response of antiparkinsonian dopamine agonists. Res Commun Mol Pathol Pharmacol. 1999;104(1):3-12. PubMed PMID: 10604273. 8: Inoue Y, Mitani H, Nanba K, Kawahara R. Treatment of periodic leg movement disorder and restless leg syndrome with talipexole. Psychiatry Clin Neurosci. 1999 Apr;53(2):283-5. PubMed PMID: 10459713. 9: Sakai T, Ii Y, Kuzuhara S. [Sinus bradycardia induced by talipexole hydrochloride in a patient with Parkinson disease]. Rinsho Shinkeigaku. 1998 Aug;38(8):771-5. Japanese. PubMed PMID: 9916527. 10: Hironaka N, Kohno Y, Yanagita T. [Comparative studies on antiparkinsonian agents, talipexole and bromocriptine, evaluated by contralateral rotational behavior in unilaterally nigral-lesioned rats]. Nihon Yakurigaku Zasshi. 1998 Oct;112(4):257-66. Japanese. PubMed PMID: 9866843. 11: Kitamura Y, Kosaka T, Kakimura JI, Matsuoka Y, Kohno Y, Nomura Y, Taniguchi T. Protective effects of the antiparkinsonian drugs talipexole and pramipexole against 1-methyl-4-phenylpyridinium-induced apoptotic death in human neuroblastoma SH-SY5Y cells. Mol Pharmacol. 1998 Dec;54(6):1046-54. PubMed PMID: 9855633. 12: Kitamura Y, Kakimura J, Taniguchi T. Protective effect of talipexole on MPTP-treated planarian, a unique parkinsonian worm model. Jpn J Pharmacol. 1998 Sep;78(1):23-9. PubMed PMID: 9804058. 13: Domino EF, Ni L, Zhang H, Kohno Y, Sasa M. Effects of talipexole on contraversive rotation and functional impairment in MPTP-induced chronic hemiparkinsonian monkeys. Jpn J Pharmacol. 1998 Jul;77(3):227-33. PubMed PMID: 9717770. 14: Kondo T, Shimada H, Hatori K, Sugita Y, Mizuno Y. Talipexole protects dopaminergic neurons from methamphetamine toxicity in C57BL/6N mouse. Neurosci Lett. 1998 May 15;247(2-3):143-6. PubMed PMID: 9655613. 15: Kitamura Y, Kohno Y, Nakazawa M, Nomura Y. Inhibitory effects of talipexole and pramipexole on MPTP-induced dopamine reduction in the striatum of C57BL/6N mice. Jpn J Pharmacol. 1997 May;74(1):51-7. PubMed PMID: 9195297. 16: Domino EF, Ni L, Zhang H, Kohno Y, Sasa M. Talipexole or pramipexole combinations with chloro-APB (SKF 82958) in MPTP-induced hemiparkinsonian monkeys. Eur J Pharmacol. 1997 May 1;325(2-3):137-44. PubMed PMID: 9163560. 17: 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. PubMed PMID: 9042591. 18: Minami M, Nemoto M, Endo T, Hamaue N, Kohno Y. Effects of talipexole on emesis-related changes in abdominal afferent vagal activity and ileal serotonin metabolism in rats. Res Commun Mol Pathol Pharmacol. 1997 Jan;95(1):67-82. PubMed PMID: 9055350. 19: Nishio H, Kohno Y, Fujii A, Negishi Y, Inoue A, Nakata Y. 5-HT3 receptor blocking properties of the antiparkinsonian agent, talipexole. Gen Pharmacol. 1996 Jul;27(5):779-85. PubMed PMID: 8842679. 20: Matsubayashi H, Amano T, Hongjing Y, Kohno Y, Sasa M. Action of intravenously administered talipexole on the rat striatal neurons receiving excitatory input from nigral dopamine neurons. Psychopharmacology (Berl). 1995 Aug;120(4):369-75. PubMed PMID: 8539316.