endothelium dependent relaxation

L-Nabe (H-Arg(NO2)-Obzl) is a effective irreversible endothelium dependent relaxation inhibitor.

CGP48369 is a potent angiotensin II receptor antagonist with antihypertensive effects that enhances endothelium-dependent relaxation of coronary arteries in spontaneously hypertensive rats.

trans-Ned 19 is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist and two-pore channel (TPC) blocker. It binds with high affinity to the NAADP receptor to inhibit NAADP-dependent lysosomal/endolysosomal calcium release without affecting IP3 or cADPR-mediated calcium signaling pathways. Functionally, trans-Ned 19 inhibits glucose-induced calcium oscillations in pancreatic islets and low histamine concentration-induced endothelium-dependent vasodilation, and reduces Ebola virus infection of host cells. In immunomodulation, NAADP signaling blockade by trans-Ned 19 promotes the conversion of mouse Th17 cells to regulatory T cells (Tregs) and shows protective effects in intestinal inflammation models.

ICI 169369, a 5-HT2/5-HT1C antagonist, can evoke endothelium-dependent relaxation in rabbit aorta.

Nolpitantium Free Base is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extrava......

Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside, an orally active phenolic compound derived from the Geranium species, demonstrates anti-inflammatory properties and holds potential for treating edema and aortic endothelium-dependent relaxation injury [1].

Adrenomedullin (porcine) is a vasodilatory peptide that elicits endothelium-dependent relaxation in rat aorta at an IC50 of 2.4 nM and also induces endothelium-independent relaxation in porcine coronary arteries, with an IC50 of 27.6 nM [1].

Cimicifugic acid D (2-Caffeoylpiscidic acid) is a benzyl tartaric acid ester that can induce vasorelaxation and an endothelium-dependent relaxation mechanism in pre-constricted rat aortic strips. During norepinephrine-induced contractions in rat aortic strips, Cimicifugic acid D inhibits extracellular Ca2+ influx through receptor-operated Ca2+ channels (ROC), while it does not affect voltage-dependent Ca2+ channels (VDC) or K+-induced contractions.

IRL-1038 TFA is a selective and potent endothelin B (ETB) receptor antagonist that inhibits endothelin-induced endothelium-dependent relaxation and can be used in the study of cardiovascular disease.