A pharmacologic activator of endothelial KCa channels increases systemic conductance and reduces arterial pressure in an anesthetized pig model was written by Mishra, Ramesh C.;Mitchell, Jamie R.;Gibbons-Kroeker, Carol;Wulff, Heike;Belenkie, Israel;Tyberg, John V.;Braun, Andrew P.. And the article was included in Vascular Pharmacology in 2016.Safety of Naphtho[1,2-d]thiazol-2-amine This article mentions the following:
SKA-31, an activator of endothelial KCa2.3 and KCa3.1 channels, reduces systemic blood pressure in mice and dogs, however, its effects in larger mammals are not well known. We therefore examined the hemodynamic effects of SKA-31, along with sodium nitroprusside (SNP), in anesthetized, juvenile male domestic pigs. Exptl., continuous measurements of left ventricular (LV), aortic and inferior vena cava (IVC) pressures, along with flows in the ascending aorta, carotid artery, left anterior descending coronary artery and renal artery, were performed during acute administration of SKA-31 (0.1, 0.3, 1.0, 3.0 and 5.0 mg/mL/kg) and a single dose of SNP (5.0 μg/mL/kg). SKA-31 dose-dependently reduced mean aortic pressure (mPAO), with the highest dose decreasing mPAO to a similar extent as SNP (- 23 ± 3 and – 28 ± 4 mm Hg, resp.). IVC pressure did not change. Systemic conductance and conductance in coronary and carotid arteries increased in response to SKA-31 and SNP, but renal artery conductance was unaffected. There was no change in either LV stroke volume (SV) or heart rate (vs. the preceding control) for any infusion. With no change in SV, drug-evoked decreases in LV stroke work (SW) were attributed to reductions in mPAO (SW vs. mPAO, r2 = 0.82, P < 0.001). In summary, SKA-31 dose-dependently reduced mPAO by increasing systemic and arterial conductances. Primary reductions in mPAO by SKA-31 largely account for associated decreases in SW, implying that SKA-31 does not directly impair cardiac contractility. In the experiment, the researchers used many compounds, for example, Naphtho[1,2-d]thiazol-2-amine (cas: 40172-65-4Safety of Naphtho[1,2-d]thiazol-2-amine).
Naphtho[1,2-d]thiazol-2-amine (cas: 40172-65-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Safety of Naphtho[1,2-d]thiazol-2-amine
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica