Effect of 5‐imino‐2,2,4,4‐tetrakis (trifluoromethyn imidazolidine (EXP 338) on spasticity: A quantitative evaluation

Abstract

In preclinical studies, 5-imino-2,2,4,4-tetrakis (trifluoromethyl) Departments of Neurological Research, Neuropsychiatric Examining Service, and Therapeutics, Veterans Adminiotration Outpatient ClinicThe structure of 5-imino-2,2.,4,4-tetrakis (triRuoromethyl) imidazolidine (EXP 338)" is shown in Fig. l,1 Preclinical studies revealed that this preparation is capable of reducing abnormal neural activity by its effect on polysynaptic reRex arcs and to a lesser degree upon monosynaptic circuits in experimental animals. No evidence of peripheral interference with neuromuscular transmission was found.8 Toxicology studies revealed no toxicity which would preclude clinical trial. Subsequently it was given to about 20 patients with neurologic diseases for 1 to 60 days without any apparent alterations in urine or blood. 2 Studies in mice with 14C-Iabeled drug indicated a half-life of 8 hours and that the drug was rapidly absorbed and uniformly distributed. 9 Adverse effects of drowsiness, disorientation, ataxia, and convulsions had followed single doses of 50 to 100 mg. of the test drug given orally.2Received for publication Dec. 19, 1967. Accepted for publication April 9, 1968. ·IND, DuPont, Wilmington. Del. 448A quantitative, non blind evaluation of oral EXP 338 was carried out on 15 pa-

Bir Florlu Aminoimidazolin Olan Midaflur'un Karşılaştırmalı Kuantum Kimyasal Analizi

“…It was reported that the compound synthesized and its structure was elucidated by Middleton and Krespan in 1970, has apparent pharmacological activity as a muscle relaxant and central nervous system depressant as a result of clinical studies [10]. There are several studies about crystal structure analysis, pharmacological and toxicological effects of midaflur [11][12][13][14].…”