CROMAKALIM

Description

(±)-Cromakalim is a prototypical activator of the ATP-sensitive potassium channel, SUR2-K_ir6, that displays anti-ischemic (EC₂₅ = 8.9 μM) and cardioprotective (IC₅₀ = 0.03 μM) effects in rat hearts. (±)-Cromakalim has also been shown to relax bladder smooth muscle in vitro. It has been used to investigate potassium channel biology and as a scaffold to develop increasingly selective K⁺ channel openers with clinical relevance.

Chemical properties

White Crystalline Solid

The Uses of CROMAKALIM

Cromakalim causes vasodilation by activation of potassim channels

The Uses of CROMAKALIM

Cromakalim has been used:

• as a potassium channel agonist to study its response to an acute increase in downstream pressure in rat lymphatic vessels.
• as a potassium channel opener to study its effects on the release of transmitters from adrenergic nerves in rat vas deferens.
• as a potassium channel activator to study its effects on the release of transmitters from purinergic and cholinergic nerves in the rat detrusor muscle.

What are the applications of Application

(±)-Cromakalim is a prototypical Kir6 (KATP) channel activator

Definition

ChEBI: Cromakalim is a 1-benzopyran.

Biological Activity

Prototypical K ATP channel opener. Relaxes rabbit isolated portal vein with an IC 50 value of 21 nM . Potent, orally active and hypotensive in vivo .

Biochem/physiol Actions

Cromakalim is an activator of the potassium channel. It is involved in the relaxation of the vascular smooth muscles. Cromakalim exhibits anti-hypertensive activity.

References

1) Sanguinetti?et al. (1988),?BRL 34915 (cromakalim) activates ATP-sensitive K+ current in cardiac muscle; Proc. Natl. Acad. Sci. USA,?85?8360 2) Wu?et al.?(2011),?Reopening of ATP-sensitive potassium channels reduces neuropathic pain and regulates astroglial gap junctions in the rat spinal cord; Pain,?152?2605 3) Roy Chowdhury?et al.?(2017),?ATP sensitive potassium channel openers: A new class of ocular hypotensive agents; Exp. Eye Res.,?158?85 4) Cao?et al.?(2016),?Opening of the Adenosine Triphosphate-sensitive Potassium Channel Attenuates Morphine Tolerance by Inhibiting JNK and Astrocyte Activation in the Spinal Cord; Clin. J. Pain,?32?617