The endothelin antagonist BQ-123, an anionic cyclopentapeptide, is taken up by rat hepatocytes through active transport systems. Here, we have examined the hepatocellular uptake mechanism for several BQ-123 derivatives with anionic charges using isolated rat hepatocytes. BQ-485, a linear peptide, BQ-518, a cyclic peptide, and compound A, a cyclic peptide with a cationic moiety, were taken up by...

UNLABELLED In vivo estimation of β(2)-nicotinic acetylcholine receptor availability with molecular neuroimaging is complicated by competition between the endogenous neurotransmitter acetylcholine and the radioligand (123)I-3-[2(S)-2-azetidinylmethoxy]pyridine ((123)I-5-IA). We examined whether binding of (123)I-5-IA is sensitive to increases in extracellular levels of acetylcholine in humans, a...

1. Swimming performance and oxygen consumption of normoxic (control) and hypoxia-acclimated (P02 — 40mmHg) rainbow trout, Salmo gairdneri Richardson, were monitored at >145, 60 and 40mmHg. 2. Maximum swimming velocity at 40mmHg was reduced from >54-8cms"' to 41-4cms" in controls and to 40-6cms" in hypoxiaacclimated fish. 3. Normoxic oxygen consumption of control fish ranged from Q-T-SmgOzkg-'h(...

The furan ring and the five-membered fluorene unit in the title compound, C(26)H(22)Cl(2)O(4), adopt envelope conformations. Inter-molecular C-H⋯O inter-actions between symmetry-related mol-ecules involving two C-H groups and an O atom as a bifurcated acceptor generate centrosymmetric hydrogen-bonded dimers with cyclic R(2) (2)(16) and R(2) (2)(8) ring motifs. A short C-H⋯Cl intramolecular cont...

UNLABELLED Patients with arrhythmogenic right ventricular cardiomyopathy (ARVC) typically present with ventricular tachyarrhythmias preferentially triggered by an elevated sympathetic tone. Previous studies demonstrated an impairment of the presynaptic catecholamine reuptake as assessed by (123)I-labeled norepinephrine analog on metaiodobenzylguanidine ((123)I-MIBG) SPECT. Mutations in the gene...

The current study was undertaken to define a biological role for the endothelin-A receptor in a clinically relevant model of altered systemic and renal function produced by suprarenal aortic cross-clamping. This model is associated with profound systemic and renal vasoconstriction, acute renal failure, and a significant increase in circulating endothelin. Studies were performed in three groups ...

On 4 March 2021 at 9 UTC a 30-m in diameter near-Earth asteroid DW1 passed the Earth distance of 570000 km, reaching maximum brightness V=14.6 mag. We observed it photometrically from 2 March, when was visible V=16.5 mag, until 7 (V=18.2 mag). During that time swept 170 degrees long arc northern sky, spanning solar phase angles range 36 to 86 degrees. This made an excellent target for physical ...