Results: The radiotracer 1 was readily prepared and purified (from 2: selleck 40+/-4 min including HPLC, 11.9+/-3.2% decay corrected isolated radiochemical yield, >99% radiochemical purity, n = 4) and displayed good stability (1 h: >99%, saline; 94.6%, serum). Strong alpha(v)beta(6)-targeted binding was observed in vitro (DX3puro beta 6 cells, 15 min: 43.2% binding, >6:1 for DX3puro beta 6:DX3puro). In the

mouse model DX3puro beta 6-tumor binding was low (1 h: 0.47+/-0.28% ID/g, 4 h: 0.14+/-0.09% ID/g) and clearing from the bloodstream was via the renal and hepatobiliary routes (urine: 167+/-84% ID/g at 1 h, 10.3+/-4.8% ID/g at 4 h; gall bladder: 95+/-33% ID/g at 1 h, 63+/-11% ID/g at 4 h).

Conclusion: Copper-free, strain-promoted click chemistry is an attractive, straightforward approach to radiolabeling. Although the [F-18]FBA-C-6-ADBIO-based 17DMAG purchase prosthetic group did not interfere with alpha(v)beta(6)-targeted binding in vitro, it did influence the pharmacokinetics, possibly due to its size and lipophilic nature. (C) 2013 Elsevier

Inc. All rights reserved.”
“Purpose: We investigated nitric oxide mediated inhibition of spontaneous activity recorded in young and aging guinea pig prostates.

Materials and Methods: Conventional intracellular microelectrode and tension recording techniques were used.

Results: The nitric oxide donor sodium nitroprusside (10 mu M) abolished spontaneous contractions and slow wave activity in 5 young and 5 aging prostates. Upon adding the nitric oxide synthase inhibitor L-NAME (10 mu M) the frequency of spontaneous contractile and electrical activity was significantly increased in each age group. This increase was significantly D-malate dehydrogenase larger in 4 to 8 preparations of younger vs aging prostates (about 40% to 50% vs about 10% to 20%, 2-way ANOVA

p < 0.01). Other measured parameters, including the duration, amplitude and membrane potential of spontaneous electrical and contractile activity, were not altered from control values. The guanylate cyclase inhibitor ODQ (10 mu M) significantly increased the frequency of spontaneous activity by 10% to 30% in 6 young guinea pig prostates (Student paired t test p < 0.05). However, it had no effect on aging prostates. The cGMP analogue 8-Br-GMP (1 mu M) and the PDE5 inhibitor dipyridamole (1 mu M) significantly decreased the frequency of contractile activity by about 70% in 4 to 9 young and older prostates (Student paired t test p < 0.05).

Conclusions: The decrease in the response to L-NAME in spontaneous contractile and slow wave activity in aging prostate tissue compared to that in young prostates suggests that with age there is a decrease in nitric oxide production. This may further explain the increase in prostatic smooth muscle tone observed in age related prostate specific conditions, such as benign prostatic hyperplasia.