Interactions of phenylalkylamines with human lung membrane and microsome preparation

Lipophilic amines are recognized as important tracers for brain imaging. Their pulmonary accumulation was a drawback for optimal concentration in the brain. We used IMP, HIPDM, IP, amphetamine derivatives to determine the relation between structure and accumulation in the lung. The incubation of phenylalkylamines in competition with 3H-Imipramine, for human lung membrane and microsomes was performed and led to the extraction of a competitive constant (KI). The results showed that the compounds can be classified in order of their decreasing affinity: Iodoamphetamine, iodoisopropylamphetamine, dimethyliodophentermine, hydroxyiodobenzyl propane diamine (HIPDM), isopropylamphetamine and amphetamine. Iodine set in the para position of the ring seemed to increase the affinity of phenylalkylamines for the lung. Adjunction of isopropyl or methyl groups to the lateral chain decreased this affinity.     

Fracture of the patella treated by open reduction and external compressive skeletal fixation

Open reduction combined with external compressive skeletal fixation was used to treat twenty-seven patients who had a separated fracture of the patella. Fixation was obtained by the use of two compressive clamps applied to stainless-steel pins that were inserted just proximal and distal to the proximal and distal poles of the patella. Range-of-motion exercises for the knee were begun at two weeks and the pins were removed at three to four weeks. All of the fractures healed. Twenty-four patients regained a range of motion that was equal to that of the opposite knee. There was no evidence of chronic osteomyelitis. Osteoarthritis was noted in one patient who refused excision of a portion of the patella.     

On the relevance of non-steroidal anti-inflammatory drugs in the prevention of paralytic ileus in rodents

In the mouse, the gastrointestinal transit of a charcoal marker, halved following the intraperitoneal administration of acetic acid, was no longer inhibited after pretreatment with the non-steroidal anti-inflammatory drugs (NSAIDs), indomethacin, ketoprofen, piroxicam or ximoprofen (0.25-2.5 mg kg-1 orally). In the fasted rat, the migrating myoelectric complex pattern of the small intestine which was disrupted for about one hour by acetic acid was unaltered by pretreatment with indomethacin or ximoprofen (0.5 mg kg-1 i.p.). In the anaesthetized rat, the inhibition by about 50% of the gastrointestinal transit due to laparotomy, did not occur following treatment with NSAIDs. It is concluded that NSAIDs prevent the occurrence of chemically-induced and postoperative ileus in rodents, an effect probably related to the analgesic properties of NSAIDs.     

Crystal-matrix interrelations in brushite and uric acid calculi

Brushite and uric acid calculi were studied by means of scanning electron microscopy with the partial dissolution method and transmission electron microscopy. Brushite calculi consist of radially oriented columnar crystals which have sheet-like substructure. The organic matrix is identified chiefly at the outside of the crystals but partly included between the substructure. The concentric matrix bands are often dislocated between the neighbouring crystals. Uric acid calculi also consist of radially oriented columnar crystals, and a fine meshwork of the organic matrix is incorporated within the crystals. The concentric matrix layers of different density are angled according to the crystal lattice. These findings indicate that the organic matrix arose from a mucinous surface coat, at least in the radially striated calculi. The crystals continued to grow in this gel-state milieu, either thrusting the matrix aside or incorporating it within the crystals.