ObjectiveEndothelins (ET) can be considered stress-responsive regulators working in paracrine and autocrine fashion. It has been suggested that elevated levels of ET may be responsible for the low coronary re-flow phenomena. Ischemia–reperfusion (I/R) was shown to stimulate ET release in rat he...
We determined the antihypertensive effects of BQ-123 (cyclo(-d-Trp-d-Asp-l-Pro-d-Val-l-Leu-), sodium salt), a selective endothelin ETA receptor antagonist, in spontaneously hypertensive rats treated with deoxycorticosterone acetate-salt (DOCA-salt SHR). BQ-123 (1–30 mg/kg/h) decreased blood pre...
The effects of the endothelin ETA, (BQ-123) and endothelin ETA/B (PD161721) receptor antagonists were investigated on ischaemia-induced arrhythmias and on the maximum following frequency. The study was carried out in Langendorff perfused rat hearts subjected to coronary artery occlusion in which...
PurposeEndothelin-1 (ET-1), a peptide produced by the vascular endothelium, causes profound renal vasoconstriction by binding to ET-A receptors. The present study examined the renal actions of ET-1 after ET-A receptors were blocked by BE-18257B to unmask the functions of ET-B receptors.
A robust and practical synthesis of each enantiomer of 2-methyl-azetidine-2-carboxylic acid, based on the use of (S)-phenylglycinol as resolving agent, is described. This synthesis affords practical quantities of this quaternary amino acid suitably N- and C-protected for use in further peptide c...
The key intermediate 3-aminopyrazolo[4,3-c]pyridine-4,6-dione (2) is considered as a precursor for some novel pyrazolo[4,3-c]pyridines 4a-c, arylhydrazopyrazolo[4,3-c]pyridines 8a-e, pyrazolo[4,5,1-ij][1,6]naphthyridines 11a-e and pyrido[4′,3′:3,4]pyrazolo[1,5-a]-pyrimidines 15a-d through Knov...
We previously identified KCA-1490 [(−)-6-(7-methoxy-2-trifluoromethyl-pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone], a dual PDE3/4 inhibitor. In the present study, we found highly potent selective PDE4 inhibitors derived from the structure of KCA-1490. Among them, N-(3,5...
Endopeptidase-24.11 (‘enkephalinase’, EC 3.4.24.11) from pig kidney hydrolysed neurokinin B at 4 sites:The major site of hydrolysis was the Gly8-Leu9 bond. Angiotensin converting enzyme (peptidyl dipeptidase A, EC 3.4.15.1) from pig kidney hydrolysed substance P releasing the C-tenninal tripep...
Using antisera specific for NH2-terminal and COOH-terminal regions of substance P and for the COOH-terminal region of neurokinin A, peptides with tachykinin-like immunoreactivity were isolated from extracts of chicken small intestine. The peptide Arg-Pro-Arg-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2 d...
A potentiometric, spectroscopic (UV-visible, CD and EPR) and electrospray ionization mass spectrometric (ESI-MS) study of Cu(II) binding to the neurokinin A with point mutation (S5A) (ANKA), His-Lys-Thr-Asp-Ala5-Phe-Val-Gly-Leu-Met-NH2 and its N-acethyl derivative (Ac-ANKA), Ac-His-Lys-Thr-Asp-A...
A novel 3-trifluoromethyl phenylhydroquinone epoxy monomer (3-TFMEP) and a novel 4-trifluoromethyl phenylbenzimidazole (4-TFMBI) curing agent both with trifluoromethyl moieties were synthesized via a multi-step procedure. Their chemical structures were confirmed by FT-IR and 1H NMR spectra. Here...
The stable conformer of 4–hydroxy–6–(trifluoromethyl)pyrimidine (HFMP) has been determined. The conformer (a) has 5.30 kcal mol–1 less energy than the conformer (b). The pyrimidine ring is characterised by alternating of bond angle distortions: the bond angles at N1, N3 and C5 atoms (115.6˚,...
The Kd value of [3H]YM-09151-2, a potent and highly selective dopamine D-2 antagonist, for binding to rat striatum was about 20 pM (half of that for [3H]spiperone and one-fiftieth of that for [3H]raclopride). The Bmax of [3H]YM-09151-2 binding was about 30% higher than that of [3H]raclopride or ...
In order to study the interaction between an IgM cold agglutinin and the erythrocyte I antigen, the former antibody was labelled with 125I using the Chloramine-T, IODOGEN and Bolton-Hunter methods. High incorporation and adequate stability of the labelled IgM were obtained with all procedures. H...
The regulatory light chain (RLC) from chicken gizzard myosin was covalently modified on cysteine 108 with either the 5- or 6-isomer of iodoacetamidotetramethylrhodamine (IATR). Labeled RLCs were purified by fast protein liquid chromatography and characterized by reverse-phase high-performance li...
The femtosecond dynamics of 4-(N,N-dimethylamino)-4′-cyanostilbene (DCS) in acetonitrile and methanol solvent was studied by fluorescence upconversion and pump-probe absorption spectroscopy. The spectral evolution observed provides strong evidence for a fast internal charge-transfer (CT) proces...
The quantum yields of fluorescence φf, cis→trans photoisomerization φc→t and trans→cis photoisomerization φt→c, and photostationary trans/cis ratios of 4-cyanostilbene, 4,4′-dicyanostilbene, 4-cyano-4′-methoxystilbene and 4-cyano-4′-dimethylaminostilbene were measured in several solven...
The S1 state of jet-cooled 4-(N,N-dimethylamino)-4′-cyanostilbene (DCS) was studied by picosecond fluorescence spectroscopy. The line structure of the S0 → S1-excitation spectrum is a superposition of transitions characteristic of isolated trans-stilbene and the dimethylamino group. Rotational...
4-dimethylammo-4'-cyanostilbene and selectively bridged model compounds are investigated using ps-time-resolved absorption and fluorescence measurements. The formation kinetics of a bicimer species are compared in homologous alcohol solvents at ambient pressure and as a function of high pre...
Ab initio complete active space self-consistent field calculations and the second-order Möller–Plesset calculations have been performed to examine the photoisomerization from trans-4-dimethylamino, 4′-cyanostilbene (DCS). Firstly, the conical intersection (CIX), where the radiationless relaxat...
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