Tiapamil

Hoick, Mark; Osterrieder, Wolfgang

doi:10.1111/j.1527-3466.1987.tb00503.x

Cited by 4 publications

(4 citation statements)

References 44 publications

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“…Amyloid P component has been purified from the kidneys of a patient who had died of secondary amyloidosis. The molecular weight of the AP subiinil on 15"?^ SDS-PAGti gels was approximately 23.100, with an amino acid composition similar to those reported by Hoick et al [16] and Benson et al f6). Under the electron microscope.…”

Section: Discussionsupporting

confidence: 81%

Human Amyloid P Component: A Circulating Lectin that Modulates Immunological Responses

Pereira

Delellis

et al. 1984

Scand J Immunol

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Amyloid P component (AP/SAP), a glycoprotein, precipitated with purified snail galactans from Helix pomatia and Ariania arbustorum in a dose‐dependent manner. Radiolabelled AP hinds to human peripheral blood mononuclear cells (PBMC), erythrocytes, and cells derived from human non‐T, non‐B acute lymphocytic leukaemia. The AP cell binding is specific in that it is dose‐dependent and can be blocked both by excess cold AP and by Helix promatia galactan. although it cannot be blocked by an equal amount of the monosaccharide galactose. In vitro studies of human PBMC immune responses demonstrated that AP inhibits PBMC proliferation responses to mycobacterial purified protein derivative and to phytohaemagglutinin and the humoral, antibody response to pokeweed mitogen. The AP‐induced suppression of non‐specific antibody production by human PBMC was dependent on the time at which AP was added to the culture. AP was suppressive if added in the first 48 h of the 7‐day culture, and the suppression could not be reversed by washing the cells after the exposure to AP. The mechanism of AP‐induced immunosuppression is still unclear, but human SAP circulates as a pair of pentameric rings, having ten identical subunits that bind to galactose polymers, and our present data suggest that AP affects the immune response through its properties as a lectin.

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Section: Discussionsupporting

confidence: 81%

Human Amyloid P Component: A Circulating Lectin that Modulates Immunological Responses

Pereira

Delellis

et al. 1984

Scand J Immunol

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“…[ 195 ] This drug caused a concentration‐dependent inhibition of [ 3 H]‐desmethoxy‐verapamil binding to pig cardiac membranes with an IC 50 of 250 nM. [ 196 ]…”

Section: Ion Channel Blockersmentioning

confidence: 99%

“…The antimhythmic properties of tiapamil appear to extend beyond the suppression of supraventricular tachycardia. Clinical trials have shown iv administered tiapamil to be effective in decreasing ventricular premature contractions and VT. [ 196 ] Despite successful clinical trials of the drug, it never entered the market.…”

Section: Ion Channel Blockersmentioning

confidence: 99%

“…[195] This drug caused a concentration-dependent inhibition of [ 3 H]-desmethoxyverapamil binding to pig cardiac membranes with an IC 50 of 250 nM. [196] Tiapamil shares many properties with verapamil, but in contrast, does not have negative inotropic activity. Animal studies have shown that tiapamil reduces peripheral resistance, increases coronary perfusion, and has antiarrhythmic properties.…”

Section: Conclusion On Kv15 Blockersmentioning

confidence: 99%

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Linked biaromatic compounds as cardioprotective agents

Mokrov

2021

Archiv der Pharmazie

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Cardiovascular diseases (CVDs) are widespread in the modern world, and their number is constantly growing. For a long time, CVDs have been the leading cause of morbidity and mortality worldwide. Drugs for the treatment of CVD have been developed almost since the beginning of the 20th century, and a large number of effective cardioprotective agents of various classes have been created. Nevertheless, the need for the design and development of new safe drugs for the treatment of CVD remains. Literature data indicate that a huge number of cardioprotective agents of various generations and mechanisms correspond to a single generalized pharmacophore model containing two aromatic nuclei linked by a linear linker. In this regard, we put forward a concept for the design of a new generation of cardioprotective agents with a multitarget mechanism of action within the indicated pharmacophore model. This review is devoted to a generalization of the currently known compounds with cardioprotective properties and corresponding to the pharmacophore model of biaromatic compounds linked by a linear linker. Particular attention is paid to the history of the creation of these drugs, approaches to their design, and analysis of the structure-action relationship within each class.

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Society and Violence in the Early Bronze Age: An Analysis of Human Skeletons from Nord-Trøndelag, Norway

Fyllingen

2003

Norwegian Archaeological Review

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Tiapamil

Cited by 4 publications

References 44 publications

Human Amyloid P Component: A Circulating Lectin that Modulates Immunological Responses

Human Amyloid P Component: A Circulating Lectin that Modulates Immunological Responses

Linked biaromatic compounds as cardioprotective agents

Society and Violence in the Early Bronze Age: An Analysis of Human Skeletons from Nord-Trøndelag, Norway

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