ABSTRACT
[formula: see text] A tight-binding, hydrophobic inhibitor of carbonic anhydrase II has been masked with a water-solubilizing, photolabile group derived from o-nitrophenylglycine. This caged inhibitor represents our first effort at the site-specific delivery of prodrugs that can be activated by light. Via this approach, we have begun to address the problems of water insolubility and systemic side effects on administration of tight-binding inhibitors of carbonic anhydrase.
Subject(s)
Carbonic Anhydrase Inhibitors/chemical synthesis , Carbonic Anhydrases/chemistry , Carbonic Anhydrase Inhibitors/radiation effects , Fluorometry , Kinetics , PhotolysisSubject(s)
Sleep Apnea Syndromes/complications , Adolescent , Adult , Humans , Male , Sleep Apnea Syndromes/physiopathologyABSTRACT
Forty-two patients with chronic obstructive pulmonary disease participated in a comprehensive inpatient rehabilitation program. Criteria for a safe, maximum treadmill exercise regimen were established; all patients pursued this regimen for six weeks, without complications, even though 31 of 39 patients showed a decline in PaO2 with exercise. Postprogram O2 consumption, minute ventilation, heart rate, and respiratory rate were significantly reduced during exercise when compared with preprogram values. Sixteen of 29 patients improved in terms of dyspnea class; an additional 11 of these 29 improved with regard to activities of daily living. Most patients who improved physiologically also improved functionally. Patients able to tolerate higher levels of treadmill exercise initially had the greatest improvement in postcourse exercise performance. The data suggest that precourse functional and exercise classification is useful in selecting candidates who will receive the greatest functional benefits from participation in rehabilitative programs.
