57568-80-6

57568-80-6 structure

Name: U-37883A
Chemical Name: N-(1-adamantyl)-N'-cyclohexylmorpholine-4-carboximidamide,hydrochloride
CAS Number: 57568-80-6
Molecular Formula: C₂₁H₃₆ClN₃O
Molecular Weight: 381.98300
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
Create Date: 2017-11-15 17:53:57
Modify Date: 2024-04-09 12:40:43
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].

Name	N-(1-adamantyl)-N'-cyclohexylmorpholine-4-carboximidamide,hydrochloride
Synonyms	4-Morpholinecarboximidine-N-1-adamantyl-N'-cyclohexane

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	Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
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.

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 Phrases	22-24/25

57568-80-6	178606-66-1
538-28-3	96744-75-1
82668-33-5	87151-85-7
76525-19-4	125173-71-9
118625-40-4	82657-23-6
1158522-08-7	940364-43-2
134104-43-1	131615-57-1
6906-52-1	930439-75-1
1018584-77-4	1375289-11-4
849349-65-1	127437-46-1