Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives

A series of four racemic ring-substituted trans-2-(indol-3-yl)cyclopropylamine derivatives was synthesized and tested for affinity at the 5-HT1A receptor, by competition with [3H]-8-OH-DPAT in rat hippocampal homogenates, and for affinity at the agonist-labeled cloned human 5-HT2A, 5-HT2B, and 5-HT2C receptor subtypes. None of the compounds had high affinity for the 5-HT1A receptor, with the 5-methoxy substitution being most potent (40 nM). At the 5-HT2A and 5-HT2B receptor isoforms, most of the compounds lacked high affinity. At the 5-HT2C receptor, however, affinities were considerably higher. The 5-fluoro-substituted compound was most potent, with a Ki at the 5-HT2C receptor of 1.9 nM. In addition, the 1R,2S-(-) and 1S,2R-(+) enantiomers of the unsubstituted compound were also evaluated at the 5-HT2 isoforms. While the 1R,2S enantiomer had higher affinity at the 5-HT2A and 5-HT2B sites, the 1S,2R isomer had highest affinity at the 5-HT2C receptor. This reversal of stereoselectivity may offer leads to the development of a selective 5-HT2C receptor agonist. The cyclopropylamine moiety therefore appears to be a good strategy for rigidification of the ethylamine side chain only for tryptamines that bind to the 5-HT2C receptor isoform.     

Primary isolation of Mycobacterium avium complex-serotype 6 on blood agar

Mycobacterium avium complex-serotype 6 was isolated in pure culture on blood agar plates from inocula taken from the heart blood, lungs, liver, kidneys, and spleen of a naturally infected captive female opossum (Didelphis marsupialis virginiana). Repeat cultures from stored tissues and transfer of colonies from original blood agar plates revealed that the mycobacterium grew on tryptose, brilliant green, eosin-methylene blue. Sabouraud glucose, and mycobiotic agar plates and in Fletcher leptospira medium. The cultural, biochemical, and serological characteristics of the test isolate were compared with other mycobacteria. This is the first report to describe the primary isolation of a serotype from the M. avium complex from an animal species on blood agar or in Fletcher broth. In addition, this is the second documented report describing the isolation and identification of a mycobacterial species from the American opossum.     

Pseudocysts of the adrenal glands in newborn infants

With diagnostic aims the author used direct laryngeal tomography in patients with median stenosis of the larynx. Tomography made it possible to define the width of the lumen of the sumplica area. Depending on the change of the subplica area the author varied the extent of surgical intervention. He used the extralaryngeal method of vocal plica laterification in all patients. With narrow subglottis he practiced complete mobilization of the elastic cone and its subsequent laterification; with wide subglottis he mobilized only the uper edge of the elastic cone. He succeeded in obtaining good functional results concerning respiration in all patients.