U-37883A

PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, KATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells[1][2].

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

In HEK-293 cells stably expressing Kir6.2/SUR1, Kir6.2/SUR2A, Kir6.2/SUR2B or Kir6.1/SUR2B, PNU-37883A inhibits four types of KATP channels, but to different extents. Inhibition of the putative smooth muscle KATP channel types, Kir6.2/SUR2B (IC50 of 15 μM) and Kir6.1/SUR2B (IC50 of 6 μM). PNU-37883A significantly inhibits currents generated by expressing Kir6.2Δ26 alone, with an IC50 of 5 μM, which was significantly increased to 38 μM when Kir6.2Δ26 is expressed with SUR2B[1]. PNU 37883 (0.1-10 nM) hydrochloride produces a concentration-dependent attenuation of the relaxation of agmatine (100 μM) in phenylephrine- or KCl- precontracted aortic rings. However, treatment with PNU 37883 (10 nM) hydrochloride alone does not modify the vascular tone[3].

[1]. Yi Cui, et al. Different molecular sites of action for the KATP channel inhibitors, PNU-99963 and PNU-37883A. Br J Pharmacol. 2003 May;139(1):122-8.

[2]. Noriyoshi Teramoto. Pharmacological Profile of U-37883A, a Channel Blocker of Smooth Muscle-Type ATP-Sensitive K Channels. Cardiovasc Drug Rev. Spring 2006;24(1):25-32.

[3]. Guang-Yuan Mar, et al. Changes of imidazoline receptors in spontaneously hypertensive rats. Int J Exp Pathol. 2013 Feb;94(1):17-24.