On the Concept of a Bivalent Pharmacophore for SKCa Channel Blockers: Synthesis, Pharmacological Testing, and Radioligand Binding Studies on Mono‐, Bis‐, and Tris‐quinolinium Compounds

No abstract is available for this paper.

• Publication year

  1996

• Venue

  Archiv der Pharmazie

• Publication date

  Unknown publication date

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1002/ardp.19963291203PMID 9038419
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Synthesis and quantitative structure-activity relationship of a novel series of small conductance Ca(2+)-activated K+ channel blockers related to dequalinium.

  1996cited by this paper
• Synthesis and pharmacological testing of dequalinium analogues as blockers of the apamin-sensitive Ca(2+)-activated K+ channel: variation of the length of the alkylene chain.

  1996cited by this paper
• Synthesis and quantitative structure-activity relationships of dequalinium analogues as K+ channel blockers: investigation into the role of the substituent at position 4 of the quinoline ring.

  1995cited by this paper
• Synthesis and qsar of dequalinium analogues AS K+ channel blockers. investigations on the role of the 4-amino group

  1995cited by this paper
• Bivalent indoles exhibiting serotonergic binding affinity

  1995cited by this paper
• Synthesis and structure-activity relationships of dequalinium analogues as K+ channel blockers. Investigations on the role of the charged heterocycle.

  1995cited by this paper
• Dequalinium, a selective blocker of the slow afterhyperpolarization in rat sympathetic neurones in culture.

  1994cited by this paper
• Purification and reconstitution of the high-conductance, calcium-activated potassium channel from tracheal smooth muscle.

  1994cited by this paper
• Synthesis and muscarinic receptors affinity of a series of antagonist bivalent ligands.

  1994cited by this paper
• Possible role of apamin‐sensitive K+ channels in myotonic dystrophy

  1994cited by this paper
• Comparable 30-kDa apamin binding polypeptides may fulfill equivalent roles within putative subtypes of small conductance Ca(2+)-activated K+ channels.

  1994cited by this paper
• Primary sequence and immunological characterization of beta-subunit of high conductance Ca(2+)-activated K+ channel from smooth muscle.

  1994cited by this paper
• Dequalinium: a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle.

  1993cited by this paper
• Cloning and expression of an inwardly rectifying ATP-regulated potassium channel

  1993cited by this paper
• Primary structure and functional expression of a rat G-protein-coupled muscarinic potassium channel

  1993cited by this paper
• Structural basis of voltage-gated K+ channel pharmacology.

  1992cited by this paper
• Apamin: A Probe for Small-Conductance, Calcium-Activated Potassium Channels

  1992cited by this paper
• Selective naltrexone-derived opioid receptor antagonists.

  1992cited by this paper
• Increase of apamin receptors in skeletal muscle induced by colchicine: possible role in myotonia.

  1992cited by this paper
• Edward E. Smissman-Bristol-Myers Squibb Award Address. The role of concepts in structure-activity relationship studies of opioid ligands.

  1992cited by this paper
• Binding and toxicity of apamin. Characterization of the active site.

  1991cited by this paper
• Bivalent ligands and the message-address concept in the design of selective opioid receptor antagonists.

  1989cited by this paper
• Rings of negatively charged amino acids determine the acetylcholine receptor channel conductance

  1988cited by this paper
• The Apamin-Sensitive Ca 2+ -Dependent K + Channel: Molecular Properties, Differentiation, Involvement in Muscle Disease, and Endogeneous Ligands in Mammalian Brain

  1988cited by this paper
• Beta-adrenoceptor antagonist activity of bivalent ligands. 1. Diamide analogues of practolol.

  1987cited by this paper
• Expression of apamin receptor in muscles of patients with myotonic muscular dystrophy

  1986cited by this paper
• Effects of apamin, quinine and neuromuscular blockers on calcium‐activated potassium channels in guinea‐pig hepatocytes.

  1985cited by this paper
• (+)-Tubocurarine blocks the Ca2+-dependent K+-channel of the bullfrog sympathetic ganglion cell.

  1984cited by this paper
• Calcium-activated potassium channels in liver cells.

  1983cited by this paper
• Calcium-dependent 86 Rb efflux and ethanol intoxication: studies of human red blood cells and rodent brain synaptosomes.

  1983cited by this paper
• Apamin, a neurotoxin specific for one class of Ca2+-dependent K+ channels.

  1983cited by this paper
• Preparation of a pure monoiodo derivative of the bee venom neurotoxin apamin and its binding properties to rat brain synaptosomes.

  1982cited by this paper
• Effects of quinine and apamin on the calcium‐dependent potassium permeability of mammalian hepatocytes and red cells.

  1981cited by this paper
• A tripod hexaketone as a ligand for manganese

  1981cited by this paper
• Apamin blocks certain neurotransmitter-induced increases in potassium permeability

  1979cited by this paper
• Use of synthetic analogs for a study on the structure-activity relationship of apamin.

  1978cited by this paper
• Structure-function relationships and site of action of apamin, a neurotoxic polypeptide of bee venom with an action on the central nervous system.

  1975cited by this paper
• Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

  1973cited by this paper
• RELATIVE EASE OF CYCLIZATION OF 2-, 3-, AND 4-AMINOPYRIDINE DERIVATIVES. SYNTHESIS OF NAPHTHYRIDINES1

  1950cited by this paper

• Medicinal applications and molecular targets of dequalinium chloride.

  2021cites this paper
• Trafficking of Intermediate (KCa3.1) and Small (KCa2.x) Conductance, Ca2+‐Activated K+ Channels: a Novel Target for Medicinal Chemistry Efforts?

  2012cites this paper
• Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca(2+)-activated K(+) channel blockers.

  2008cites this paper
• K+ channel modulators for the treatment of neurological disorders and autoimmune diseases.

  2008cites this paper
• Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca2+-activated K+ channel (SK(Ca)).

  2007cites this paper
• Modulators of small- and intermediate-conductance calcium-activated potassium channels and their therapeutic indications.

  2007cites this paper
• Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca2+-activated K+ channel (SKCa)

  2007cites this paper
• Calcium-Dependent Regulation of Ion Channels.

  2006cites this paper
• Evidence for a Multivalent Interaction of Symmetrical, N-Linked, Lidocaine Dimers with Voltage-Gated Na+ Channels

  2006cites this paper
• Defining determinant molecular properties for the blockade of the apamin-sensitive SKCa channel in guinea-pig hepatocytes: the influence of polarizability and molecular geometry.

  2004cites this paper
• Modulation of small conductance calcium-activated potassium (SK) channels: a new challenge in medicinal chemistry.

  2003cites this paper
• A review of molecular modeling approaches to pharmacophore models and structure-activity relationships of ion channel modulators in CNS.

  2002cites this paper
• Characterisation of [(125)I]-apamin binding sites in rat brain membranes with HE293 cells transfected with SK channel subtypes.

  2001cites this paper
• Pharmacology of Small-Conductance, Calcium-Activated K+Channels

  2001cites this paper
• bis-Quinolinium cyclophanes: 8,14-diaza-1,7(1, 4)-diquinolinacyclotetradecaphane (UCL 1848), a highly potent and selective, nonpeptidic blocker of the apamin-sensitive Ca(2+)-activated K(+) channel.

  2000cites this paper
• Synthesis, molecular modeling, and pharmacological testing of bis-quinolinium cyclophanes: potent, non-peptidic blockers of the apamin-sensitive Ca(2+)-activated K(+) channel.

  2000cites this paper
• Recent advances in the biology of small conductance calcium-activated potassium channels

  1999cites this paper
• Bis-quinolinium cyclophanes: 6,10-diaza-3(1,3),8(1,4)-dibenzena-1,5(1,4)- diquinolinacyclodecaphane (UCL 1684), the first nanomolar, non-peptidic blocker of the apamin-sensitive Ca(2+)-activated K+ channel.

  1998cites this paper
• Synthesis and structure-activity studies of novel potassium ion channel blockers.

  1997cites this paper