Detail of "101626-70-4"

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Antitremor activity of talipexole produced by selective dopamine D2 receptor stimulation in cynomolgus monkeys with unilateral lesions in the ventromedial tegmentum

Antitremor activity of talipexole produced by selective dopamine D2 receptor stimulation in cynomolgus monkeys with unilateral lesions in the ventromedial tegmentum.Some chemicals with cas registry numbers like 186000-16-8 and 101626-70-4 are also used. Kohno, Yasuko; Fukuzaki, Koichiro; Kitahara, Koichi; Koja, Takeshi ( Product Management Department, Marketing Division, Nippon Boehringer Ingelheim Co., Ltd., 3-10-1, Yato, Kawanishi, Japan). European Journal of Pharmacology, 319(2/3), 197-205 (English) 1997 Elsevier. CODEN: EJPHAZ. ISSN: 0014-2999. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The antitremor activity of talipexole, a nonergot dopamine D2 receptor agonist which possesses a2-adrenoceptor agonistic and 5-HT3 receptor antagonistic properties, was examd. in monkeys with a unilateral lesion in the ventromedial tegmentum. Talipexole dose-dependently suppressed the tremor and had ED50 values of 34 mg/kg s.c. and 84 mg/kg orally. The antitremor effect of talipexole occurred at much lower doses than that of an ergot dopamine receptor agonist, bromocriptine (ED50 2.5 mg/kg s.c.), and talipexole acted synergistically in combination with L-dopa. In ventromedial tegmentum-lesioned monkeys, antitremor doses of talipexole did not cause emetic behavior, but had sedative effects. Conversely, monkeys given bromocriptine exhibited oral movement, salivation and vomiting when antitremor effects were obsd., but not marked sedative behavior at any of the doses investigated. During repeated administration of talipexole (50 mg/kg/day s.c. for 21 days), the extent and duration of the antitremor effect did not change, but those of the sedative effect decreased gradually. The antitremor effect of talipexole was suppressed by sulpiride, but not by SCH 23390 or yohimbine, while the sedative effect was inhibited by sulpiride and yohimbine. The main metabolites of talipexole had no antitremor or sedative effects. These results indicate that talipexole exerts its antitremor activity via selective dopamine D2 receptor stimulation. .

Evaluation of antiparkinsonian activities of pramipexole hydrochloride (SND919CL2Y) on animal Parkinson's disease models

Evaluation of antiparkinsonian activities of pramipexole hydrochloride (SND919CL2Y) on animal Parkinson's disease models. Takeuchi, Shougo; Osugi, Takeshi; Satoh, Hisashi; Kohjimoto, Yoshiro; Setoguchi, Harumi (Kawanishi Pharma Research Institute, Nippon Boehringer Ingelheim Co., Ltd., Japan). Igaku to Yakugaku, 49(6), 973-983 (Japanese) 2003 Shizen Kagakusha. CODEN: IGYAEI. ISSN: 0389-3898. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effects of pramipexole, dopamine D3/D3 agonist, were examd. in two types of animal Parkinson's disease models. In MPTP-lesioned monkeys, the effects of pramipexole (0.03, 0.1, 0.3 mg/kg p.o.) were compared with those of talipexole (0.03, 0.1, 0.There are some reagents with their cas registry numbers 104632-25-9 and 101626-70-4 are used in this study.3 mg/kg p.o.) and bromocriptine (1.0, 3.0 10 mg/kg p.o.). Pramipexole ameliorated dose-dependently the MPTP-induced parkinsonism that was assessed with the rating scale on functional motor behavioral changes. Statistical significances were obtained at the dose of 0.1 and 0.3 mg/kg p.o. of pramipexole, and the effects lasted during the observations, at least 6 h after the administrations. The efficacy of pramipexole was similar to that of talipexole, and more potent than that of bromocriptine. In reserpinized mice, the combined effects of pramipexole with L-DOPA were examd. Pramipexole (0.1, 0.3, 1.0 mg/kg p.o.) ameliorated the reserpine-induced akinesia that was assessed on the locomotor activity, and the catalepsy, the failure to correct an externally imposed posture, in a dose-dependent manner. The effects of pramipexole were strengthened by combined treatment with L-DOPA (200 mg/kg s.c. in the presence of benserazide chloride 50 mg/kg i.p.). The combined effect of pramipexole with L-DOPA was additive or synergistic, and no antagonistic effect was obsd. These results indicate that pramipexole could be beneficial for treating Parkinson's disease. .