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更新于：2025-01-23

Talipexole Hydrochloride

盐酸他利克索

更新于：2025-01-23

概要

基本信息

药物类型

小分子化药

别名

Talipexole、Talipexole hydrochloride (JAN)

+ [3]

靶点

D2 receptor

作用机制

D2 receptor激动剂(多巴胺D2受体激动剂)

治疗领域

神经系统疾病内分泌与代谢疾病

在研适应症

帕金森病

非在研适应症-

原研机构-

在研机构-

非在研机构

Boehringer Ingelheim Pharma GmbH & Co., KG

最高研发阶段批准上市

首次获批日期

(1996-01-01),

帕金森病

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C10H17Cl2N3S

InChIKeyDPQAXNSOFFYKDS-UHFFFAOYSA-N

CAS号36085-73-1

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关联

100 项与盐酸他利克索相关的临床结果

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100 项与盐酸他利克索相关的转化医学

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100 项与盐酸他利克索相关的专利（医药）

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593

项与盐酸他利克索相关的文献（医药）

2015-12-16·NeuroReport4区 · 医学

Duration of drug action of dopamine D2 agonists in mice with 6-hydroxydopamine-induced lesions

4区 · 医学

Article

作者: Yamauchi, Yuji ; Ijiro, Tomoyuki ; Kaidoh, Kouichi ; Suzuki, Takayuki ; Hiratochi, Masahiro ; Oana, Fumiki ; Tsuchioka, Akihiro

Although 6-hydroxydopamine-induced (6-OHDA-induced) rats are a well-known Parkinson's disease model, the effects of dopamine D2 agonists in mice with 6-OHDA-induced lesions are not completely understood. We produced mice with 6-OHDA-induced lesions and measured their total locomotion counts following administration of several dopamine D2 agonists (pramipexole, ropinirole, cabergoline, rotigotine, apomorphine, talipexole, and quinelorane). Cabergoline showed the longest duration of drug action, which was in agreement with its long-lived anti-Parkinson effects in rats and humans. In contrast, pramipexole and ropinirole had notably short durations of drug action. We demonstrated that mice with 6-OHDA-induced lesions accompanied with significant lesions in the striatum may be reasonable models to predict the action duration of anti-Parkinson drug candidates in humans.

2014-11-01·Nihon shinkei seishin yakurigaku zasshi = Japanese journal of psychopharmacology

[The therapeutic plasma concentrations of antiparkinson dopamine agonists and their in vitro pharmacology at dopamine receptors].

Review

作者: Kobayashi, Hiroyuki ; Tadori, Yoshihiro

This review discusses the relationship between therapeutic plasma concentrations of antiparkinson dopamine agonists (rotigotine, pergolide, cabergoline, apomorphine, bromocriptine, ropinirole, pramipexole, and talipexole) and their in vitro pharmacology at dopamine D1, D2 and D3 receptors. A significant correlation was found between therapeutic plasma concentrations of these dopamine agonists and their agonist potencies (EC50) at D2 receptors, although no such correlation existed at D1 or D3 receptors, suggesting that D2 receptors could be the primary and common target for the antiparkinson action of all dopamine agonists. However, D1 receptor stimulation is also important for maintaining swallowing reflex, bladder function and cognition. In particular, continuous D1 and D2 receptor stimulation may be reduced to low levels among Parkinson's disease patients. Our findings revealed therapeutic plasma concentrations of rotigotine were similar to its agonist potencies at both D1 and D2 receptors. Thus, rotigotine may be beneficial for the treatment of Parkinson's disease patients in that this dopamine agonist has the potential of continuous stimulation of both D1 and D2 receptors in the clinical setting.

2014-08-01·Brain Research Bulletin3区 · 医学

Analysis of functional selectivity through G protein-dependent and -independent signaling pathways at the adrenergic α2C receptor

3区 · 医学

Article

作者: Nagy, József ; Kolok, Sándor ; Lendvai, Balázs ; Kurko, Dalma ; Kapui, Zoltán

Although G protein-coupled receptors (GPCRs) are traditionally categorized as Gs-, Gq-, or Gi/o-coupled, their signaling is regulated by multiple mechanisms. GPCRs can couple to several effector pathways, having the capacity to interact not only with more than one G protein subtype but also with alternative signaling or effector proteins such as arrestins. Moreover, GPCR ligands can have different efficacies for activating these signaling pathways, a characteristic referred to as biased agonism or functional selectivity. In this work our aim was to detect differences in the ability of various agonists acting at the α2C type of adrenergic receptors (α2C-ARs) to modulate cAMP accumulation, cytoplasmic Ca(2+) release, β-arrestin recruitment and receptor internalization. A detailed comparative pharmacological characterization of G protein-dependent and -independent signaling pathways was carried out using adrenergic agonists (norepinephrine, phenylephrine, brimonidine, BHT-920, oxymetazoline, clonidine, moxonidine, guanabenz) and antagonists (MK912, yohimbine). As initial analysis of agonist Emax and EC50 values suggested possible functional selectivity, ligand bias was quantified by applying the relative activity scale and was compared to that of the endogenous agonist norepinephrine. Values significantly different from 0 between pathways indicated an agonist that promoted different level of activation of diverse effector pathways most likely due to the stabilization of a subtly different receptor conformation from that induced by norepinephrine. Our results showed that a series of agonists acting at the α2C-AR displayed different degree of functional selectivity (bias factors ranging from 1.6 to 36.7) through four signaling pathways. As signaling via these pathways seems to have distinct functional and physiological outcomes, studying all these stages of receptor activation could have further implications for the development of more selective therapeutics with improved efficacy and/or fewer side effects.

100 项与盐酸他利克索相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01505	盐酸他利克索	N04B	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
帕金森病	-	-	1996-01-01

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
帕金森病	临床1期	德国	Boehringer Ingelheim Pharma GmbH & Co., KG	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


SFN2002	N/A	-	-	Piribedil	夢衊獵蓋範鬱鹹膚艱膚(鏇繭壓廠顧積窪憲壓積) = 廠範醖選壓蓋鬱觸獵蓋顧膚鬱觸簾遞鑰壓餘鬱 (築簾淵壓廠衊繭膚鹽鏇 )	-	2002-11-06
				Talipexole	夢衊獵蓋範鬱鹹膚艱膚(鏇繭壓廠顧積窪憲壓積) = 製選膚窪夢築簾網齋鬱顧膚鬱觸簾遞鑰壓餘鬱 (築簾淵壓廠衊繭膚鹽鏇 )