Role of K+ channels in N-acetylprocainamide-induced relaxation of bovine tracheal smooth muscle

Nakahara, Tsutomu; Moriuchi, Hiroshi; Tanaka, Yoshio; Yunoki, Motonari; Kubota, Yuko; Sakamato, Kenji; Shigenobu, Koki; Ishii, Kunio

doi:10.1016/s0014-2999(01)00796-8

Cited by 6 publications

(7 citation statements)

References 12 publications

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“…The 87 Sr/ 86 Sr ratio in the bones also helps in dating archaeological specimens 4. Barium, in lower concentrations, acts as a muscle relaxant 5. However, the presence of Sr 2+ and Ba 2+ beyond a threshold concentration is known to have adverse effects causing cardiac and nervous system disorders and even paralysis 6.…”

Section: Introductionmentioning

confidence: 99%

Competitive binding of Ba²⁺and Sr²⁺ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site

et al. 2011

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Owing to their immense biological significance, development of sensors for the selective detection of alkaline earth metal ions has attracted vast research interest. In this article we have reported the synthesis, characterisation and ion binding studies of a new RuII‐polypyridyl‐crown‐anthraquinone complex (5). Studies confirm selective binding of BaII, SrII and CaII ions, with K Ba 2+ > K Sr 2+ >> K Ca 2+, over all other metal ions, to the crown ether moiety and not to the methoxy anthraquinone component, the latter being the second binding site available and known for its affinity towards alkaline earth metal ions from one of our previous reports.

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Section: Introductionmentioning

confidence: 99%

Competitive binding of Ba²⁺and Sr²⁺ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site

et al. 2011

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“…Alternatively, amine drugs could stimulate fluid uptake indirectly via an apparently unrelated mode of action. Procaine and/or procainamide are known to block or stimulate several types of ion channels (Stephenson and Wendt, 1986;Mieyal et al, 1998;Huang et al, 1999;Nakahara et al, 2001); notably, procainamide blocks the delayed rectifier K ϩ channel human ether-a-go-go-related gene (HERG; Yang et al, 2001;Ridley et al, 2003). Further cellular actions of millimolar levels of procaine and procainamide include DNA demethylation (Villar-Garea et al, 2003).…”

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confidence: 99%

Massive Cell Vacuolization Induced by Organic Amines Such as Procainamide

Morissette¹,

Moreau²,

C.‐Gaudreault³

et al. 2004

J Pharmacol Exp Ther

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Procaine and some other basic drugs reportedly induce vacuolization of various cell types. We addressed the concentrationeffect and structure-activity relationships as well as the mechanism of this effect using three cell lines. Massive vacuolization occurs over several hours in primary cultures of rabbit pulmonary artery smooth muscle cells (SMCs) and COS-1 cells in response to procaine and loosely related amine compounds (procainamide, N-acetyl-procainamide, metoclopramide, lidocaine, triethylamine, nicotine) used at 2.5 mM. Furthermore, chloroquine, propranolol, diphenhydramine, and neutral red are active in this respect at 100 to 250 M in SMCs and COS-1 cells.

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“…To assess the participation of K + channels in the trachylobane-318 relaxant activity we used TEA + 10 mM, a non-selective K + channel blocker (21) in addition to selective K + channel blockers such as apamin (10 –6 M; blocker of small conductance calcium-activated K + channels; SK ca ) (22), BaCl 2 (10 –4 M; blocker of inward rectifier K + channels; K ir ) (23), glibenclamide (3 × 10 ‑6 M; blocker of ATP‑sensitive potassium channels; K ATP ) (24), 4‑AP (2 × 10 –3 M; blocker of voltage‑activated K + channels) (24) and IbTx (10 –7 M; blocker of big conductance calcium-activated K + channels; BK ca ) (25). The blockers were added to different tracheal preparations for 20 minutes, after which a contraction was induced using CCh (10 –6 M) before trachylobane-318 was added cumulatively.…”

Section: Methodsmentioning

confidence: 99%

Relaxant effect of <i>Ent</i>-7α-hydroxytrachyloban-18-oic acid, a trachylobane diterpene from <i>Xylopia langsdorfiana</i> A. St-Hil. & Tul., on tracheal smooth muscle

Martins

Santos

Correia

et al. 2013

J. Smooth Muscle Res.

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Ent-7α-hydroxytrachyloban-18-oic acid, a trachylobane diterpene from Xylopia langsdorfiana, has previously been shown to relax the guinea-pig trachea in a concentration-dependent manner. In this study we aimed to elucidate the mechanisms underlying this action and so contribute to the discovery of natural products with therapeutic potential. A possible interaction between diterpene and the Ca2+-calmodulin complex was eliminated as chlorpromazine (10-6 M), a calmodulin inhibitor, did not significantly alter the diterpene-induced relaxation (pD2 = 4.38 ± 0.07 and 4.25 ± 0.07; mean ± S.E.M., n=5). Trachylobane-318 showed a higher relaxant potency when the trachea was contracted by 18 mM KCl than it did with 60 mM KCl (pD2 = 4.90 ± 0.25 and 3.88 ± 0.01, n=5), suggesting the possible activation of K+ channels. This was confirmed, as in the presence of 10 mM TEA+ (a non-selective K+ channel blocker), diterpene relaxation potency was significantly reduced (pD2 = 4.38 ± 0.07 to 4.01 ± 0.06, n=5). Furthermore, K+ channel subtypes KATP, KV, SKCa and BKCa seem to be modulated positively by trachylobane-318 (pD2 = 3.91 ± 0.003, 4.00 ± 0.06, 3.45 ± 0.14 and 3.80 ± 0.05, n=5) but not the Kir subtype channel (pD2 = 4.15 ± 0.10, n=5). Cyclic nucleotides were not involved as the relaxation due to aminophylline (pD2 = 4.27 ± 0.09, n=5) was not altered in the presence of 3 × 10-5 M trachylobane-318 (pD2 = 4.46 ± 0.08, n=5). Thus, at a functional level, trachylobane-318 seems to relax the guinea-pig trachea by positive modulation of K+ channels, particularly the KATP, KV, SKCa and BKCa subtypes.

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Role of K+ channels in N-acetylprocainamide-induced relaxation of bovine tracheal smooth muscle

Cited by 6 publications

References 12 publications

Competitive binding of Ba²⁺and Sr²⁺ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site

Competitive binding of Ba²⁺and Sr²⁺ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site

Massive Cell Vacuolization Induced by Organic Amines Such as Procainamide

Relaxant effect of <i>Ent</i>-7α-hydroxytrachyloban-18-oic acid, a trachylobane diterpene from <i>Xylopia langsdorfiana</i> A. St-Hil. & Tul., on tracheal smooth muscle

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Role of K+ channels in N-acetylprocainamide-induced relaxation of bovine tracheal smooth muscle

Cited by 6 publications

References 12 publications

Competitive binding of Ba2+and Sr2+ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site

Competitive binding of Ba2+and Sr2+ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site

Massive Cell Vacuolization Induced by Organic Amines Such as Procainamide

Relaxant effect of <i>Ent</i>-7α-hydroxytrachyloban-18-oic acid, a trachylobane diterpene from <i>Xylopia langsdorfiana</i> A. St-Hil. & Tul., on tracheal smooth muscle

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Competitive binding of Ba²⁺and Sr²⁺ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site

Competitive binding of Ba²⁺and Sr²⁺ to 18‐Crown‐6 in a Receptor with a 1‐Methoxyanthraquinone Analogue as the Other Binding Site