Speciation and chromosomal evolution of the palaearctic species of chironomids of the genus Sergentia Kieffer (Diptera, Chironomidae): Chromosome polymorphism in the populations of S. baueri Wülker et al., 1999, S. prima Proviz et al., 1997, and S. electa Proviz et al., 1999 from the Irkutsk reservoir

208

167

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with 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 over 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/bph.15539. 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‐2021, and supersedes data presented in the 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.

Section: -Ht 3 Receptorsmentioning

confidence: 99%

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Ion channels

Alexander

Mathie

Peters

et al. 2021

208

167

“…Selective agonists -meta-chlorphenylbiguanide [75,199,536,668,669], 2-methyl-5-HT [75,199,536,668], SR57227A [258] -Rat, 1-phenylbiguanide [75] Antagonists -vortioxetine (pK i 8.4) [51], metoclopramide (pK i 6-6.4) [106,397] Selective antagonists -palonosetron (pK i 10.5) [677], alosetron (pK i 9.5) [382], (S)-zacopride (pK i 9) [106], granisetron (pK i ∼8.6-8.8) [397,668], tropisetron (pK i 8.5-8.8) [536,668], ondansetron (pK i ∼7.8-8.3) [106,397,668] Channel blockers picrotoxinin (pIC 50 4.2) [974], bilobalide (pIC 50 2.5) [974], ginkgolide B (pIC 50 2.4) [974] picrotoxinin (pIC 50 5) [973], TMB-8 (pIC 50 4.9) [944], diltiazem (pIC 50 4.7) [973], bilobalide (pIC 50 3.3) [973], ginkgolide B (pIC 50 3.1) [973] Labelled ligands -[ 3 H]ramosetron (Antagonist) (pK d 9.8) [668], [ 3 H]GR65630 (Antagonist) (pK d 8.6-9.3) [382,536], [ 3 H]granisetron (Antagonist) (pK d 8.9) [106,397], Comments: Quantitative data in the table refer to homooligomeric assemblies of the human 5-HT 3 A subunit, or the receptor native to human tissues. Significant changes introduced by co-expression of the 5-HT 3 B subunit are indicated in parenthesis.…”

Section: Overviewmentioning

confidence: 99%

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Ion channels

Alexander

Mathie

Peters

et al. 2019

298

248

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (http://www.guidetopharmacology.org/), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 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.14749. 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‐2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC‐IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

“…To date, inclusion of the 5-HT 3 A subunit appears imperative for 5-HT 3 receptor function. Agonists CSTI-300 (Partial agonist) [1025] CSTI-300 (Partial agonist) [1025] Selective agonists -meta-chlorphenylbiguanide [90,241,659,828,829], 2-methyl-5-HT [90,241,659,828], SR57227A [316] -Rat, 1-phenylbiguanide [90] Antagonists -vortioxetine (pK i 8.4) [63], metoclopramide (pK i 6-6.4) [126,481] Selective antagonists -palonosetron (pK i 10.5) [840], alosetron (pK i 9.5) [466], (S)-zacopride (pK i 9) [126], granisetron (pK i ∼8. 6-8.8) [481, 828], tropisetron (pK i 8.5-8.8) [659,828], ondansetron (pK i ∼ 7.8-8.3) [126,481,828] Channel blockers picrotoxinin (pIC 50 4.2) [1198], bilobalide (pIC 50 2.5) [1198], ginkgolide B (pIC 50 2.4) [1198] picrotoxinin (pIC 50 5) [1197], TMB-8 (pIC 50 4.9) [1163], diltiazem (pIC 50 4.7) [1197], bilobalide (pIC 50 3.3) [1197], ginkgolide B (pIC 50 3.1) [1197] Labelled ligands -[ 3 H]ramosetron (Antagonist) (pK d 9.8) [828], [ 3 H]GR65630 (Antagonist) (pK d 8.6-9.3) [466,659], [ 3 H]granisetron (Antagonist) (pK d 8.9) [126,481], [ 3 H](S)-zacopride (Antagonist) (pK d 8.7) [934], [ Comments: Quantitative data in the table refer to homooligomeric assemblies of the human 5-HT 3 A subunit, or the receptor native to human tissues.…”

Section: -Ht 3 Receptorsmentioning

confidence: 99%

The Concise Guide to PHARMACOLOGY 2023/24: Ion channels

Alexander,

Mathie,

Peters

et al. 2023

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.