79574-62-2Relevant articles and documents
Design, synthesis, and activity of a series of arylpyrid-3-ylmethanones as type i positive allosteric modulators of α7 nicotinic acetylcholine receptors
Hogenkamp, Derk J.,Ford-Hutchinson, Thomas A.,Li, Wen-Yen,Whittemore, Edward R.,Yoshimura, Ryan F.,Tran, Minhtam B.,Johnstone, Timothy B. C.,Bascom, Gavin D.,Rollins, Hannah,Lu, Lena,Gee, Kelvin W.
, p. 8352 - 8365 (2013)
A series of novel arylpyrid-3-ylmethanones (7a-aa) were designed as modulators of α7 nicotinic acetylcholine receptors (nAChRs). The methanones were found to be type I positive allosteric modulators (PAMs) of human α7 nAChRs expressed in Xenopus ooctyes. Structure-activity relationship (SAR) studies resulted in the identification of compound 7v as a potent and efficacious type I PAM with maximum modulation of a nicotine EC 5 response of 1200% and EC50 = 0.18 μM. Compound 7z was active in reversing the effect of scopolamine in the novel object recognition (NOR) paradigm with a minimum effective ip dose of 1.0 mg/kg (2.7 μmol/kg). This effect was blocked by the selective α7 nAChR antagonist methyllycaconitine (MLA). These compounds are potent type I positive allosteric modulators of α7 nAChRs that may have therapeutic value in restoring impaired sensory gating and cognitive deficits in schizophrenia and Alzheimer's disease.
PYRIDINYLMORPHOLINE DERIVATIVES
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Page/Page column 43, (2008/06/13)
The invention relates to compounds of formula (I); wherein R, R1, R2 and X are as defined herein, their preparation and their use as pharmaceuticals.
TREATMENT OF HOT FLASHES, IMPULSE CONTROL DISORDERS AND PERSONALITY CHANGE DUE TO A GENERAL MEDICAL CONDITION
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Page/Page column 258-259, (2010/02/12)
Selective norepinephrine reuptake inhibitors are useful for the prevention or treatment of hot flashes, vasomotor symptoms, impulse control disorders or personality change due to a general medical condition.
