(R)-baclofen - CAS 69308-37-8
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
GABA Receptor
(R)-baclofen a selective GABAB agonist.
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NSC 334693
1.Efficient Synthesis of β-Aryl-γ-lactams and Their Resolution with (S)-Naproxen: Preparation of (R)- and (S)-Baclofen.
Montoya-Balbás IJ1, Valentín-Guevara B2, López-Mendoza E3, Linzaga-Elizalde I4, Ordoñez M5, Román-Bravo P6. Molecules. 2015 Dec 10;20(12):22028-43. doi: 10.3390/molecules201219830.
An efficient synthesis of enantiomerically-pure β-aryl-γ-lactams is described. The principal feature of this synthesis is the practical resolution of β-aryl-γ-lactams with (S)-Naproxen. The procedure is based on the Michael addition of nitromethane to benzylidenemalonates, which was easily obtained, followed by the reduction of the γ-nitroester in the presence of Raney nickel and the subsequent saponification/decarboxylation reaction. The utility of this methodology was highlighted by the preparation of enantiomerically-pure (R)- and (S)-Baclofen hydrochloride.
2.Epigenetic regulation of dorsal raphe GABA(B1a) associated with isolation-induced abnormal responses to social stimulation in mice.
Araki R1, Hiraki Y2, Nishida S2, Kuramoto N3, Matsumoto K4, Yabe T5. Neuropharmacology. 2016 Feb;101:1-12. doi: 10.1016/j.neuropharm.2015.09.013. Epub 2015 Sep 11.
In isolation-reared mice, social encounter stimulation induces locomotor hyperactivity and activation of the dorsal raphe nucleus (DRN), suggesting that dysregulation of dorsal raphe function may be involved in abnormal behaviors. In this study, we examined the involvement of dorsal raphe GABAergic dysregulation in the abnormal behaviors of isolation-reared mice. We also studied an epigenetic mechanism underlying abnormalities of the dorsal raphe GABAergic system. Both mRNA and protein levels of GABA(B1a), a GABA(B) receptor subunit, were increased in the DRN of isolation-reared mice, compared with these levels in group-reared mice. In contrast, mRNA levels for other GABAergic system-related genes (GABA(A) receptor α1, β2 and γ2 subunits, GABA(B) receptor 1b and 2 subunits, and glutamate decarboxylase 67 and 65) were unchanged. Intra-DRN microinjection of 0.06 nmol baclofen (a GABA(B) receptor agonist) exacerbated encounter-induced hyperactivity and aggressive behavior, while microinjection of 0.
3.[Double blind placebo controlled randomized pilot clinical trial of baclofen (Baclosan®) for alcohol dependence].
Krupitsky EM1, Rybakova KV1, Kiselev AS1, Alexeeva YV1, Berntsev VA1, Chekhlaty EI1, Zubova EY1, Popov YV1, Neznanov NG1. Zh Nevrol Psikhiatr Im S S Korsakova. 2015;115(6):53-62.
in English, RussianЦель исследования — изучение эффективности применения баклофена (препарат «баклосан») для стабилизации ремиссии у больных алкоголизмом. Материал и методы. Обследовали 32 больных алкоголизмом, которые случайным образом распределялись в одну из двух групп. Больным 1-й группы (16 человек) был назначен баклофен (50 мг/сут) в течение 3 месяцев; больные 2-й группы получали идентично выглядящее плацебо. Все больные еженедельно должны были посещать клинику для контроля ремиссии (потребления алкоголя), оценки выраженности влечения к алкоголю (крэйвинга), аффективных расстройств (депрессии и тревоги), активности гамма–глутамилтранспептидазы (ГГТ) и комплайенса приема препаратов (по рибофлавину в моче). Для контроля потребления алкоголя применяли методику ретроспективного анализа и определение активности ГГТ. Для оценки тревоги использовали шкалы Гамильтона и Спилбергера. Для оценки депрессии — шкалу Монтгомери-Ашберг. Влечение к алкоголю оценивали с помощью обсессивно-компульсивной, пенсильванской и визуальной аналоговой шкал.
4.Validated Method for the Quantification of Baclofen in Human Plasma Using Solid-Phase Extraction and Liquid Chromatography-Tandem Mass Spectrometry.
Nahar LK1, Cordero RE2, Nutt D3, Lingford-Hughes A3, Turton S3, Durant C3, Wilson S3, Paterson S2. J Anal Toxicol. 2016 Mar;40(2):117-23. doi: 10.1093/jat/bkv125. Epub 2015 Nov 4.
A highly sensitive and fully validated method was developed for the quantification of baclofen in human plasma. After adjusting the pH of the plasma samples using a phosphate buffer solution (pH 4), baclofen was purified using mixed mode (C8/cation exchange) solid-phase extraction (SPE) cartridges. Endogenous water-soluble compounds and lipids were removed from the cartridges before the samples were eluted and concentrated. The samples were analyzed using triple-quadrupole liquid chromatography-tandem mass spectrometry (LC-MS-MS) with triggered dynamic multiple reaction monitoring mode for simultaneous quantification and confirmation. The assay was linear from 25 to 1,000 ng/mL (r(2) > 0.999; n = 6). Intraday (n = 6) and interday (n = 15) imprecisions (% relative standard deviation) were <5%, and the average recovery was 30%. The limit of detection of the method was 5 ng/mL, and the limit of quantification was 25 ng/mL. Plasma samples from healthy male volunteers (n = 9, median age: 22) given two single oral doses of baclofen (10 and 60 mg) on nonconsecutive days were analyzed to demonstrate method applicability.
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CAS 69308-37-8 (R)-baclofen

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