Hydrolysis of Bz-Gly-Ser-Phe-Arg, C-terminal fragment of atriopeptin 2, by human cardiac angiotensin-converting enzyme has been studied. The KM for the reaction was 10−4 M. The effect of concentration of NaCl on activity of cardiac angiotensin-converting enzyme has been determined, which allowed...

Manipulations of salt and water intake influenced the atriopeptin content in the atria and plasma of rats. Plasma levels of atriopeptin varied in proportion with dietary salt intake. In contrast, cardiac levels of atriopeptin varied inversely with the amount of salt in the diet. Acute stimulatio...

Binding studies revealed the presence of a single class of high affinity binding sites for atriopeptin III on rabbit lung membranes. An apparent dissociation constant (Kd) of 0.32 nM and a binding capacity of 166 fmol/mg protein was determined. Binding was time-dependent and saturable. The relat...

SummaryPharmacological strategies have been employed to manipulate the response to atriopeptin (AP-28; ANF 99–126) in rats. These approaches include: heparin infusion which blocks the natriuresis-diuresis produced by exogenous AP infusion or by acute volume expansion; and autoimmune rats with e...

Atriopeptin II and isoproterenol acted synergistically to inhibit the phenylephrine-induced contraction of aortic smooth muscle from Wistar-Kyoto (WKY) rats. Thus, a weakly inhibitory concentration of atriopeptin II (10 nM) caused a 5-fold decrease in the IC50 of isoproterenol from 169 nM to 32 ...

The involvement of atriopeptin in hypertension was investigated in spontaneously hypertensive rats (SHR). It was found that intravenous injection of atriopeptin III (20 – 80 nmol/kg) markedly decreased the mean arterial pressure in anesthetized SHR in a dose dependent manner. The heart rate was...

Atriopeptin II activated particulate guanylate cyclase 5–10-fold in a concentration- and time-dependent fashion in crude membranes obtained from homogenates of rat adrenal cortex or medulla. Similar effects were observed with other atriopeptin analogs. Soluble guanylate cyclase and adenylate cy...

2-Aryl-3-arylamino-4,4,4-trifluoro-2-butenenitriles were obtained as hydrates from 3-oxo-2-aryl-4,4,4-trifluorobutyronitriles and anilines and their structure and heterocyclizations studied. Cyclization with polyphosphoric acid gave poor yields of 3-aryl-2-trifluoromethyl-4-quinolones, but they ...

The effects on the physical properties of [N(CH3)4]2Zn1-xCoxBr4 (x=0, 0.5, 0.7, and 1) crystal due to the partial substitution of Zn2+ ions with paramagnetic Co2+ ions were discussed. The crystal structures and phase transition temperature (287 K) of layered perovskite-type [N(CH3)4]2Zn1-xCoxBr4...

Starting from 4-amino-1-(tert-butoxycarbonyl)piperidine (Boc-PD-NH2), we report the synthesis of three novel meta-tri- and dimeric tetravalent N-substituted melamines with piperidin-4-yl groups. These compounds were used as central building-blocks and successfully incorporated into three new G-2...

:This chapter includes of the Purification of Biochemicals and is made up of seven sections which provide procedures used in the literature for purifying the respective substances, together with their physical properties, molecular weights and empirical formulae, melting and boiling points, dens...

In the present work, a series of conjugates of amino acids with all-trans-retinoic acid (ATRA) and shorter polyene chain analogues were rationally designed, synthesized by coupling the succinimidyl active esters of the acidic retinoids with appropriately protected amino acids or peptides followe...

The key chiral intermediate 3,5-dihydroxy-6-(benzyloxy) hexanoic acid, ethyl ester 2a, was made by the stereoselective microbial reduction of 3,5-dioxo-6-(benzyloxy) hexanoic acid, ethyl ester 1. Among various microbial cultures evaluated, cell suspensions of Acinetobacter calcoaceticus SC 13876...

Eleven new analogues of arginine vasopressin (AVP) modified in position 2 by 3,3-diphenyl-l-alanine or its d-enantiomer (Dip or d-Dip) were synthesized and pharmacologically evaluated for their pressor, antidiuretic and in vitro uterotonic activities. Both the Dip and d-Dip modifications at posi...

A new strategy for the preparation of both enantiomers of two phenylalanine analogues, β,β-diphenylalanine and fluorenylglycine, has been developed. The combination of a high yielding racemic synthesis and a very efficient resolution procedure has provided significant amounts of each amino aci...

The reaction of thymidine 3′-methanephosphonothioic acid with p-nitrophenylsulfenyl chloride provides S1-(3′-O-thymidine-O-methanephosphonyl)-S2-p-nitrophenyl disulfide which, in the presence of an excess of sulfenyl chloride and triphenylphosphine gives, in a stereospecific manner, thymidine ...

The one-pot reaction of nucleosides with MeP(O)Cl2 and thiophenol, providing nucleoside 3′-O-(S-phenyl methanephosphonothioate), potential monomers for the synthesis of oligonucleoside methanephosphonate, is described.

In A549 cells, the addition of D,L-threo-1-phenyl-2-decanoylamino-3-morpholino-1-propanol (DL-PDMP) led to marked autophagy with massive microtubule-associated protein 1 light chain 3B (LC3B)-II protein expression as an indication of autophagy and a steep decrease of p62 protein as a co-indicati...

Gangliosides and extracellular matrix molecules influence neurite outgrowth, but the combinatorial effects of these endogenous agents on outgrowth are unclear. Exogenous gangliosides inhibit neurite outgrowth from SH-SY5Y cells stimulated with platelet-derived growth factor-BB, and different iso...

This study focused on a series of pyrrolidin-2-one derivatives connected via two or four methylene units to arylpiperazine fragment. The compounds obtained for α1- and α2-adrenoceptors were assessed. The compound with highest affinity for the α1-adrenoceptors was 1-{4-[4-(2-chloro-phenyl)-pip...