title: Inhibitory effect of DG-5128 on steroid-dependent asthma.
abstract: To study the possible role of alpha-2 receptors in intractable asthmatics, we investigated the ameliorative effects of 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenylthyl]pyridine dihydrochloride sesquihydrate (DG-5128) on 10 steroid-dependent asthmatic patients. The forced expiratory volume in 1 second (FEV1) and the respiratory resistance (Rrs) were measured 1, 2, and 3 hours after oral administration of 200 mg DG-5128 and compared with the premedication measurements. Two hours after DG-5128 administration, the FEV1 rose significantly (p less than 0.01) and the Rrs decreased significantly (p less than 0.05). Asthmatic symptoms (cough, wheezing, dyspnea) also improved in 80% of the patients. This finding raises the possibility that alpha-2 adrenoceptors exist in human airways, that they play an important role in the pathophysiology of asthma, and that the overfunction of these alpha-2 adrenoceptors and/or Gi-protein cause intractable asthma.
authors.affiliation: First Department of Internal Medicine, Gunma University School of Medicine, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Yoshie
authors.forename: K
authors.initials: K
authors.lastname: Iizuka
authors.forename: T
authors.initials: T
authors.lastname: Nakazawa
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism; D000305:Adrenal Cortex Hormones / Q000627:therapeutic use; D000317:Adrenergic alpha-Antagonists / Q000627:therapeutic use*; D000328:Adult; D000368:Aged; D000403:Airway Resistance / Q000187:drug effects; D001249:Asthma / Q000188:drug therapy* / Q000503:physiopathology; D002908:Chronic Disease; D005260:Female; D005541:Forced Expiratory Volume; D019204:GTP-Binding Proteins / Q000378:metabolism; D006801:Humans; D007093:Imidazoles / Q000627:therapeutic use*; D008297:Male; D008875:Middle Aged; D014797:Vital Capacity / Q000187:drug effects
chemical_list: D000305:Adrenal Cortex Hormones; D000317:Adrenergic alpha-Antagonists; D007093:Imidazoles; C032368:midaglizole; D019204:GTP-Binding Proteins; D000262:Adenylyl Cyclases