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Chemical Compound Review:

CHEMBL97196 2,2-dimethyl-4-(1- oxidopyridin-6...

Synonyms: AG-D-44160, SureCN6369348, ACMC-20motq, CTK4B1782, Ro-31-6930, ...

Gater, P.R. et al., Workman, A.J. et al., Paciorek, P.M. et al., Zell, M. et al., Finta, E.P. et al., et al.

Workman, MacKenzie, Northover,

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High impact information on Ro 31-6930

Two openers of ATP-sensitive potassium (K(ATP)) channels, RO 31-6930 (10 microM) and cromakalim (100 microM) decreased the spontaneous discharge of action potentials without altering their amplitude or duration [1].
BRL-38227, EMD 52692, SDZ PCO 400 and Ro 31-6930 were 11-42 times less potent in relaxing contractions to ET-1 than KCl [2].
Glibenclamide and procaine, but not apamin, inhibit the relaxant responses to Ro 31-6930 in guinea-pig taenia caeci [3].
This study compares the effects of two K(+0-channel openers, Ro 31-6930 and BRL 38227, on cholinergically-evoked contraction of guinea-pig airways to examine whether either compound acts through prejunctional inhibition of the release of acetylcholine [4].
In the anaesthetised guinea-pig, Ro 31-6930 inhibited the bronchoconstriction evoked by bilateral vagus nerve stimulation and intravenous acetylcholine with ID50 values of 12.9 +/- 3.9 and 3.6 +/- 1.3 micrograms/kg i.v. respectively [4].

Biological context of Ro 31-6930

In addition, Ro 31-6930 was an effective bronchodilator when given by inhalation to the anaesthetised guinea-pig [5].
A specific LC-MS assay was developed for simultaneous determination of Ro 31-7837 (I) and its metabolite Ro 31-6930 (II) in rat plasma, using on-line SPE by column-switching reversed-phase HPLC combined with atmospheric pressure chemical ionization (APCI) tandem mass spectrometry for detection in the selected reaction monitoring mode [6].

Anatomical context of Ro 31-6930

In view of the protective activity of Ro 31-6930 against antigen challenge in the sensitised guinea-pig and its potency in relation to other bronchodilators, it is considered that compounds which relax airway smooth muscle by the opening of plasmalemmal potassium channels may have a role in the treatment of asthma [5].

Gene context of Ro 31-6930

The KATP opener Ro 31-6930 (0.5 and 5 microM) shortened the APD50 and APD80 during coronary ligation, to significantly below both their control and pre-occlusion values (P < 0.05), and caused a concentration-dependent increase in both the incidence and duration of VT during the ligation [7].

Analytical, diagnostic and therapeutic context of Ro 31-6930

Ro 31-6930 at 5 microM also shortened APD50 and APD80 even before ligation (by 50 and 62% respectively, P < 0.05), and abolished the normal APD-lengthening seen during ischaemia [7].

References

Effects of potassium channel openers and their antagonists on rat locus coeruleus neurones. Finta, E.P., Harms, L., Sevcik, J., Fischer, H.D., Illes, P. Br. J. Pharmacol. (1993) [Pubmed]
Differential effects of endothelin-1 on the vasorelaxant properties of benzopyran and non-benzopyran potassium channel openers. Lawson, K., Barras, M., Zazzi-Sudriez, E., Martin, D.J., Armstrong, J.M., Hicks, P.E. Br. J. Pharmacol. (1992) [Pubmed]
Glibenclamide and procaine, but not apamin, inhibit the relaxant responses to Ro 31-6930 in guinea-pig taenia caeci. Perkins, R.S., Paciorek, P.M., Waterfall, J.F. Br. J. Pharmacol. (1989) [Pubmed]
The inhibitory effects of Ro 31-6930 and BRL 38227 on cholinergically-mediated bronchoconstriction in the guinea-pig. Gater, P.R., Paciorek, P.M., McKean, J.C., Wilson, K., Brewster, M., Waterfall, J.F. Eur. J. Pharmacol. (1993) [Pubmed]
Inhibition by Ro 31-6930 of agonist and allergen induced bronchoconstriction in anaesthetised guinea-pigs and cats. Paciorek, P.M., Burden, D.T., Gater, P.R., Hawthorne, Y.M., Spence, A.M., Taylor, J.C., Waterfall, J.F. Pulmonary pharmacology. (1991) [Pubmed]
Simultaneous determination of a potassium channel opener and its metabolite in rat plasma with column-switching liquid chromatography using atmospheric pressure chemical ionisation. Zell, M., Husser, C., Erdin, R., Hopfgartner, G. J. Chromatogr. B Biomed. Sci. Appl. (1997) [Pubmed]
Do KATP channels open as a prominent and early feature during ischaemia in the Langendorff-perfused rat heart? Workman, A.J., MacKenzie, I., Northover, B.J. Basic Res. Cardiol. (2000) [Pubmed]

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