ArticleBritish journal of pharmacology1996
Extra- and intracellular action of quaternary devapamil on muscle L-type Ca(2+)-channels.
Article in British journal of pharmacology, 1996. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- The Stable Gastric Pentadecapeptide BPC 157 Pleiotropic Beneficial Activity and Its Possible Relations with Neurotransmitter Activity.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Novel charged sodium and calcium channel inhibitor active against neurogenic inflammation.eLife · 2019Article
- Verapamil block of T-type calcium channels.Molecular pharmacology · 2011Article
- Interaction of diltiazem with an intracellularly accessible binding site on Ca(V)1.2.British journal of pharmacology · 2011Article
- Structural model for phenylalkylamine binding to L-type calcium channels.The Journal of biological chemistry · 2009Article
- Probing the architecture of an L-type calcium channel with a charged phenylalkylamine: evidence for a widely open pore and drug trapping.The Journal of biological chemistry · 2007Article
- Molecular basis of drug interaction with L-type Ca2+ channels.Journal of bioenergetics and biomembranes · 1998Review
- Molecular mechanism of use-dependent calcium channel block by phenylalkylamines: role of inactivation.Proceedings of the National Academy of Sciences of the United States of America · 1997Article
- A molecular model of the inner pore of the Ca channel in its open state.Channels (Austin, Tex.)Article
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7 authors.
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Abstract
1. The quaternary derivative of the potent verapamil-analogue, (-)-D888, (qD888, 4-cyano-4-(3,4-dimethoxyphenyl)-N-[2-(3-methoxy phenyl)ethyl]-N,N,5-trimethyl-1-hexanaminium) was synthesized as a novel membrane-impermeable probe to study the localization of phenylalkylamine (PAA) effector domains on L-type Ca2+ channels. Channel block by qD888 was investigated in smooth muscle-like (A7r5) cells after extra- and intracellular application by use of the whole-cell configuration of the patch clamp technique. 2. Extracellularly applied qD888 inhibited Sr2+ (Isr) (IC50 = 90 microM) and Na+ (IC50 = 27 microM) inward currents through L-type Ca(2+)-channels mainly in a resting-state-dependent manner. Structurally closely related quaternary PAAs (e.g. D890) were ineffective after extracellular application. 3. QD888 also blocked Isr from the cytoplasmic side, as did other quaternary PAAs (D890, D575). Intracellular block was clearly dependent on channel opening, which resulted in pronounced use-dependence. 4. We conclude that qD888 blocks L-type Ca2+ channels not only from the intracellular side, via interaction with the classical PAA binding domain, but also from the extracellular channel surface. The properties of Ca2+ channel block together with previous biochemical and structural data suggest that extracellular block may be mediated by a site that also confers tonic block by quaternary benzothiazepines.
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