U-37883A

Modify Date: 2024-04-09 12:40:43

U-37883A Structure
U-37883A structure
Common Name U-37883A
CAS Number 57568-80-6 Molecular Weight 381.98300
Density N/A Boiling Point 474.1ºC at 760mmHg
Molecular Formula C21H36ClN3O Melting Point N/A
MSDS N/A Flash Point 240.5ºC

 Use of 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].

 Names

Name N-(1-adamantyl)-N'-cyclohexylmorpholine-4-carboximidamide,hydrochloride
Synonym More Synonyms

 U-37883A Biological Activity

Description 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].
Related Catalog
In Vitro 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].
References

[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.

 Chemical & Physical Properties

Boiling Point 474.1ºC at 760mmHg
Molecular Formula C21H36ClN3O
Molecular Weight 381.98300
Flash Point 240.5ºC
Exact Mass 381.25500
PSA 36.86000
LogP 4.69650

 Safety Information

Safety Phrases 22-24/25

 Synonyms

4-Morpholinecarboximidine-N-1-adamantyl-N'-cyclohexane