Regarding Methadone and the QTc Interval: Paucity of Clinically Significant Factors in a Retrospective Cohort, Gavin Bart et al

Stoklosa, Ted; Haber, Paul S.

doi:10.1097/adm.0000000000000382

Cited by 1 publication

(1 citation statement)

References 2 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…3) [57], GSK1702934A (Agonist) (pIC 50 6.4) [1352], pyrazolopyrimidine 4n (pEC 50 5.9) [1002], OptoBI-1 (photoswitch activation; concentration range: 1-2x10 -5 M) [1209], Op-toDArG (photoswitch activation; concentration range: 3x10 -5 M) [701], flufenamate, hyp 9 [685], hyperforin [686] pyrazolopyrimidine 4n (pIC 50 6.1) [1002], OptoBI-1 (photoswitch activation; concentration range: 1-2x10 -5 M) [1209] Selective activators AM237 (pEC 50 7. --Functional Characteristics = 41-63 pS; conducts mono-and di-valent cations non-selectively (P Ca /P Na = 1.8-9.5); dual rectification (inward and outward) as a homomer, outwardly rectifying when expressed with TRPC1 or TRPC4 = 28-37 pS; conducts mono and divalent cations with a preference for divalents (P Ca /P Na = 4.5-5.0); monovalent cation current suppressed by extracellular Ca 2+ and Mg 2+ , dual rectification (inward and outward), or inward rectification = 25-75 pS; conducts mono and divalent cations with a preference for divalents (P Ca /P Cs = 5.9); modest outward rectification (monovalent cation current recorded in the absence of extracellular divalents); monovalent cation current suppressed by extracellular Ca 2+ Channel blockers isosakuranetin (pIC 50 6.3) [1152], primidone (pIC 50 6.2) [643], maprotiline (pIC 50 5.8) [643], diclofenac (pIC 50 5.2) [1172], liquiritigenin (pIC 50 5.2) [1152], naringenin (pIC 50 5.2) [1152,1153], Gd 3+ (Antagonist) (pIC 50 4) [405,671], La 3+ (Antagonist) (pIC 50 4) [405,671], chloroform (Antagonist) (pIC 50 3.8) [582], halothane (Antagonist) (pIC 50 3.3) [582] compound 6 (pIC 50 6.4) [1148], LBA (pIC 50 5.8) [1148], compound 5 (Antagonist) (pIC 50 5.7) [923], meclofenamic acid (pIC 50 5. = 40-87 pS; permeable to mono-and di-valent cations with a preference for divalents (Mg 2+ > Ca 2+ ; P Ca /P Na = 6.9), conductance sequence Zn 2+ > Ba 2+ > Mg 2+ = Ca 2+ = Mn 2+ > Sr 2+ > Cd 2+> Ni 2+ ; strong outward rectification abolished by removal of extracellular divalents, inhibited by intracellular Mg 2+ (IC 50 = 0.5 mM) and ATP…”

Section: Nomenclaturementioning

confidence: 99%

The Concise Guide to PHARMACOLOGY 2023/24: Ion channels

Alexander,

Mathie,

Peters

et al. 2023

British J Pharmacology

View full text Add to dashboard Cite

The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and over 6000 interactions with about 3900 ligands. There is an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (https://www.guidetopharmacology.org/), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes almost 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point‐in‐time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.16178. Ion channels are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein‐coupled receptors, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid‐2023, and supersedes data presented in the 2021/22, 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC‐IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

show abstract