Omaha Trade Area Study No. 06: License Plate Survey of Five Major Shopping Points

This is the third of a series of continuing studies in the attempt to ascertain Omaha\u27s retail trade area. The method utilized, as in the past, is that of recording license plate prefix numbers at the three major and two minor shopping points within the Omaha SMSA. Emphasis is placed upon the three major shopping points, Downtown, Crossroads and Westroads, for they are the best indicators of the regional focus of Omaha. The two other points surveyed were Southroads and Downtown Council Bluffs (See Map 13, Page 5). This year the survey eliminated The Center, GEM and Skagway because of their community influence

Mouse brain distribution of a carbon-11 labeled vesamicol derivative: Presynaptic marker of cholinergic neurons

The regional mouse brain distribution of a new carbon-11 labeled derivative of vesamicol, [11C]-5-(N-methylamino)benzovesamicol ([11C]MABV) is reported. Radiotracer concentrations in vivo are in the rank order of striatum>cortex>hippocampus>hypothalamus> cerebellum, consistent with reported distributions of other presynaptic cholinergic neuronal markers. In time course studies, striatum/cerebellum and cortex/cerebellum ratios for (-)-[11C]MABV continue to increase to values of 13 and 5, respectively, 75 min after i.v. injection of [11C]MABV. The specific binding in striatum and cortex is lowered by pretreatment with (+/-)-vesamicol, and shows stereoselectivity with lower uptake and lower ratios for the (+)-enantiomer. (-)-[11C]MABV is proposed as a positron-emitting radioligand for the in vivo study of presynaptic cholinergic neurons.Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/28961/1/0000798.pd

Iodine-125 and fluorine-18 labeled aryl-1,4-dialkylpiperazines: Potential radiopharmaceuticals for in vivo study of the dopamine uptake system

A series of fluorine-18 and iodine-125 labeled aryl-1,4-dialkylpiperazine analogs, derivatives of GBR 12935, were synthesized as radiotracers for positron emission tomography or single photon emission computerized tomography imaging of the brain based on their affinity for the presynaptic dopamine reuptake system. High specific activity fluorine-18 tracers were prepared by nucleophilic aromatic substitution reactions; iodine-125 tracers were prepared by isotopic exchange reactions. In vitro competitive binding studies demonstrated that iodine substitution is tolerated in the 4-position of the phenyl ring of the phenalkylpiperazine group. In vivo regional brain biodistribution studies in mice indicated no selectivity of the radioiodinated ligands for the dopamine reuptake site, with striatum/cerebellum concentration ratios of 1. Similar negative results with the new fluorine-18 derivatives demonstrated that in vivo selectivity for the dopamine reuptake site appears to be critically dependent on the carbon chain length between the piperazine ring and the solitary aromatic ring. These studies suggest that development of new radiopharmaceuticals based on the GBR 12935 structure cannot be based solely on considerations of in vitro binding affinities.Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/30090/1/0000461.pd

NMDA receptor channels: Labeling of MK-801 with iodine-125 and fluorine-18

Methods for labeling the glutamate channel blocking agent MK-801 with iodine-125 (125I) and fluorine-18 (18F) are described. Radioiodine was incorporated in the 1- or 3-positions of the aromatic ring of (+/-)MK-801 by solid-state halogen exchange techniques. Attachment of the [18F]fluoromethyl group to the bridgehead methyl position was achieved by reaction of [18F]fluoride with the triflamide alcohol 8 or the novel cyclic sulfamate 9 recently reported by Merck chemists. Radiochemical yields of (+/-)13-[18F]- fluoromethyl-MK-801 were >72%, EOB; radiochemical purity >99%. In competitive binding studies using rat brain homogenates, (+/-)3-bromo-MK-801 showed greater affinity than (+/-)MK-801 for the glutamate-linked channel. The experimental log P (2.1 +/- 0.1) of MK-801 is optimal for transit of the blood-brain barrier. These preliminary findings support further testing of 3-[123I]iodo-MK-801 and (+/-)13-[18F]fluoromethyl-MK-801 as possible agents for in vivo mapping of the glutamate receptor complex.Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/27605/1/0000649.pd

Synthesis of a nonpeptide carbon-11 labeled substance P antagonist for PET studies

CP 96,345 is a nonpeptide high affinity antagonist of the substance P (NK1) receptor. The radiosynthesis of [11C]CP 96,345 suitable for Positron Emission Tomography (PET) applications is described. [11C]CP 96,345 was prepared by O-methylation of a desmethyl precursor via in situ generation of its phenolate salt. The in vivo tissue distribution of [11C]CP 96,345 in guinea pigs (n = 2) at 5 and 30 min was determined. Uptake was low in brain ([approximate] 0.04% dose/g) and highest ([approximate] 1-2% dose/g) in the spleen and lungs. The present findings indicate that the use of [11C]CP 96,345 in PET might be more applicable to the study of substance P receptors in peripheral tissues involved with inflammatory disease and arthritis.Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/30822/1/0000482.pd

Facile Preparation of Fluorescent Neoglycoproteins Using p-Nitrophenyl Anthranilate as a Heterobifunctional Linker

A facile preparation of neoglycoconjugates has been developed with a commercially available chemical, p-nitrophenyl anthranilate (PNPA), as a heterobifunctional linker. The two functional groups of PNPA, the aromatic amine and the p-nitrophenyl ester, are fully differentiated to selectively conjugate with glycans and other biomolecules containing nucleophiles. PNPA is efficiently conjugated with free reducing glycans via reductive amination. The glycan−PNPA conjugates (GPNPAs) can be easily purified and quantified by UV absorption. The active p-nitrophenyl ester in the GPNPA conjugates readily reacts with amines under mild conditions, and the resulting conjugates acquire strong fluorescence. This approach was used to prepare several fluorescent neoglycoproteins. The neoglycoproteins were covalently printed on activated glass slides and were bound by appropriate lectins recognizing the glycans

No compelling evidence that preferences for facial masculinity track changes in women’s hormonal status

Although widely cited as strong evidence that sexual selection has shaped human facial-attractiveness judgments, findings suggesting that women’s preferences for masculine characteristics in men’s faces are related to women’s hormonal status are equivocal and controversial. Consequently, we conducted the largest-ever longitudinal study of the hormonal correlates of women’s preferences for facial masculinity (N = 584). Analyses showed no compelling evidence that preferences for facial masculinity were related to changes in women’s salivary steroid hormone levels. Furthermore, both within-subjects and between-subjects comparisons showed no evidence that oral contraceptive use decreased masculinity preferences. However, women generally preferred masculinized over feminized versions of men’s faces, particularly when assessing men’s attractiveness for short-term, rather than long-term, relationships. Our results do not support the hypothesized link between women’s preferences for facial masculinity and their hormonal status