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For naphtho[2,3-f]indole-5,10-diones 6 9 bearing 3-aminopyrrolidine in the side chains, the ability to bind double-stranded DNA and inhibit topoisomerases 1 and 2 mediated relaxation of supercoiled DNA were demonstrated.
The claim that the vasodilator effect was endothelium-independent is also strengthened from the aforementioned scenario, that when rat aorta was denuded of endothelium and the extract mediated relaxation of PE-induced contractions at similar concentration, as in intact preparations.
Animal experiments have shown that a hot water extract of black tea (Camellia sinensis) promotes gastric emptying in rats, possibly as a result of inhibition of nitric oxide mediated relaxation of the stomach by thearubignins and theaflavins.
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In vitro studies have demonstrated a 5-HT4 receptor-mediated relaxatiof of the pre-contracted rat esophagus.
G4 aptamers designed against STAT3, nucleolin and SP1 inhibit STAT3 transcriptional activity in human breast adenocarcinoma MCF-7 cells, and all the studied aptamers inhibit TOP1-mediated relaxation of supercoiled plasmid DNA.
R. sakuraii bradykinin ([Arg0,Leu1,Thr6,Trp8] BK) was 28-fold less potent than mammalian BK in effecting B2 receptor-mediated relaxation of mouse trachea and the des[Arg0] derivative was only a weak partial agonist.
Nevertheless, ALT-711 improved acetylcholine-mediated relaxation of NF and HF arteries in ZDF rats.
This distension is sensed by mechanoreceptors in the rectal wall, which cause a neurally-mediated relaxation of the IAS muscle.
The constitutively active NOS3 mutant, S1177D enhances NO-mediated relaxation of bradykinin-stimulated porcine coronary arteries (Teupe et al., 2002).
In this way, activation of PARs 1 and 2 in a blood vessel causes an immediate endothelium-dependent, NO-mediated relaxation of the tissue.
Furthermore, a recent investigation using high concentrations of 7-KC (205 μM) found no effect of ex vivo incubation on ACh-mediated relaxation of mouse aorta [36].
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