Piperidines

Publication Title: 
Nature

Adiponectin secreted from adipocytes binds to adiponectin receptors AdipoR1 and AdipoR2, and exerts antidiabetic effects via activation of AMPK and PPAR-? pathways, respectively. Levels of adiponectin in plasma are reduced in obesity, which causes insulin resistance and type 2 diabetes. Thus, orally active small molecules that bind to and activate AdipoR1 and AdipoR2 could ameliorate obesity-related diseases such as type 2 diabetes. Here we report the identification of orally active synthetic small-molecule AdipoR agonists.

Author(s): 
Okada-Iwabu, Miki
Yamauchi, Toshimasa
Iwabu, Masato
Honma, Teruki
Hamagami, Ken-ichi
Matsuda, Koichi
Yamaguchi, Mamiko
Tanabe, Hiroaki
Kimura-Someya, Tomomi
Shirouzu, Mikako
Ogata, Hitomi
Tokuyama, Kumpei
Ueki, Kohjiro
Nagano, Tetsuo
Tanaka, Akiko
Yokoyama, Shigeyuki
Kadowaki, Takashi
Publication Title: 
Neuroscience Letters

Blonanserin is a second-generation antipsychotic drug for schizophrenia. The pharmacological actions of blonanserin are shown to be the antagonism of dopamine receptor 2 and serotonin receptors. However, its molecular mechanisms in brain cells have not been fully characterized. Accumulating evidence suggests that antipsychotic drugs and mood stabilizers show epigenetic effects on a wide range of genes in animal and cellular models. We performed genome-wide DNA methylation analysis targeting 479,814 CpG sites of cultured human neuroblastoma cells administered with blonanserin.

Author(s): 
Murata, Yui
Nishioka, Masaki
Bundo, Miki
Sunaga, Fumiko
Kasai, Kiyoto
Iwamoto, Kazuya
Publication Title: 
Revue De L'infirmiere

This personal account describes the pas de deux performed for four years by a couple living with Alzheimer's. ThÈrËse, a former nurse, is suffering from the disease. Her husband, RenÈ is also a former caregiver who has taken on the mantle of his wife's carer to accompany ThÈrËse on her one-way journey to an unknown land. A journey scattered with obstacles during which the need for assistance, support and love is highlighted.

Author(s): 
Magnon, RenÈ
Publication Title: 
Deutsche Medizinische Wochenschrift (1946)
Author(s): 
Mall, G.
Vosseler, E.
Publication Title: 
Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica

Pharmacological effects of ifenprodil (IP), 4-benzyl-alpha-(p-hydroxyphenyl)-beta-methyl-1-piperidineethanol-L-(+)-tartrate monohydrate (Funai Pharmaceutical), a potential vasodilator, were studied in the dog, rabbit, guinea-pig and mouse. 1) Intravenous administration of IP (0.1 approximately 1 mg/kg) exhibited a continuous fall in blood pressure, an increase in heart rate and an increase in cardiac contractile force in the dog. The depressor and chronotropic effects of IP appeared likewise in the pithed dog, and the depressor responses were slightly more evident in the rabbit.

Author(s): 
Maeda, Y.
Furukawa, T.
Publication Title: 
Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica

Effects of ifenprodil tartrate, a potent vasodilator, on the autonomic, peripheral and central nerve system were studied in experimental animals. In isolated vas deferens of guinea pigs, the contraction in response to noradrenaline and sympathetic nerve stimulation was competetively antagonized by ifenprodil 10(-7)--10(-5) M (pA2: 7.69 against noradrenaline). Ifenprodil (50 approximately 1,000 mug/kg i.v.) inhibited the contraction of cat nictitating membrane and dog urinary bladder induced by sympathetic nerve stimulation.

Author(s): 
Mizusawa, H.
Yamane, M.
Sakai, K.
Publication Title: 
Archives Internationales De Pharmacodynamie Et De Thérapie

The antidiarrheal drugs loperamide and diphenoxylate were tested for their ability to potentiate central nervous system depression induced by ethanol in mice and nethohexital in rats. Oral diphenoxylate potentiated the loss of righting reflex (hypnosis) at 10 mg/kg in mice and at 5 mg/kg in rats, doses which were considerably lower than those required to induce morphine-like behavior in mice and rats. Oral loperamide did not potentiate hypnosis.

Author(s): 
Mcguire, J. L.
Awouters, F.
Niemegeers, C. J.
Publication Title: 
Methods and Findings in Experimental and Clinical Pharmacology

The present study explores pharmacologically on the model spontaneously beating 3H-noradrenaline pretreated guinea-pig atrial preparation the mechanism(s) by which the representative central nervous system (CNS) stimulant drug 3-methyl-3-ethylglutarimide (bemegride, MEG) and its representative CNS depressant homologue 3-methyl-3-n-butylglutarimide (MBG) affect transmitter release and the force and rate of atrial contraction and contracture, as well as the relevance of these atrial mechanism(s) to those involved in the production of drug-evoked convulsions and hypnosis in the mammalian CNS.

Author(s): 
Arblaster, C. I.
Cameron, D. W.
Lavi, Y.
Laycock, G. M.
Shulman, A.
Publication Title: 
Indian Journal of Experimental Biology

Piperine (1-peperoyl piperidine), a major alkaloid isolated from Piper nigrum Linn, potentiated pentobarbitone sleeping time in dose dependant manner, with peak effect at 30 min. Blood and brain pentobarbitone levels were higher in piperine treated animals. Piperine treatment in rats, treated chronically with phenobarbitone, significantly potentiated pentobarbitone sleeping time, as compared to the controls. There was no alteration in barbital sodium sleeping time.

Author(s): 
Mujumdar, A. M.
Dhuley, J. N.
Deshmukh, V. K.
Raman, P. H.
Thorat, S. L.
Naik, S. R.
Publication Title: 
Acta Anaesthesiologica Scandinavica

BACKGROUND: Nitrous oxide (N2O) has been suggested to contribute to bowel distension, resulting in worsened operating conditions for laparoscopic surgery, and to increase incidence of postoperative nausea and vomiting. Therefore, our objective was to assess the feasibility of two remifentanil-based anaesthetic regimens free from N2O with special regard to recovery profile, postoperative analgesic demand and side effects in patients undergoing laparoscopic cholecystectomy.

Author(s): 
Grundmann, U.
Silomon, M.
Bach, F.
Becker, S.
Bauer, M.
Larsen, B.
Kleinschmidt, S.

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