دورية أكاديمية
أعرض في EDS

The calcilytics Calhex-231 and NPS 2143 and the calcimimetic Calindol reduce vascular reactivity via inhibition of voltage-gated Ca 2+ channels.

التفاصيل البيبلوغرافية
العنوان: The calcilytics Calhex-231 and NPS 2143 and the calcimimetic Calindol reduce vascular reactivity via inhibition of voltage-gated Ca 2+ channels.
المؤلفون: Greenberg HZE; Vascular Biology Research Centre, Institute of Cardiovascu lar & Cell Sciences, St. George's, University of London, Cranmer Terrace, London SW17 0RE, UK. Electronic address: m0600877@sgul.ac.uk., Jahan KS; Vascular Biology Research Centre, Institute of Cardiovascu lar & Cell Sciences, St. George's, University of London, Cranmer Terrace, London SW17 0RE, UK., Shi J; Vascular Biology Research Centre, Institute of Cardiovascu lar & Cell Sciences, St. George's, University of London, Cranmer Terrace, London SW17 0RE, UK., Vanessa Ho WS; Vascular Biology Research Centre, Institute of Cardiovascu lar & Cell Sciences, St. George's, University of London, Cranmer Terrace, London SW17 0RE, UK., Albert AP; Vascular Biology Research Centre, Institute of Cardiovascu lar & Cell Sciences, St. George's, University of London, Cranmer Terrace, London SW17 0RE, UK.
المصدر: European journal of pharmacology [Eur J Pharmacol] 2016 Nov 15; Vol. 791, pp. 659-668. Date of Electronic Publication: 2016 Oct 08.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Elsevier Science Country of Publication: Netherlands NLM ID: 1254354 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1879-0712 (Electronic) Linking ISSN: 00142999 NLM ISO Abbreviation: Eur J Pharmacol Subsets: MEDLINE
أسماء مطبوعة: Publication: 2005- : Amsterdam : Elsevier Science
Original Publication: Amsterdam, North Holland Pub. Co.
مواضيع طبية MeSH: Benzamides/*pharmacology , Calcimimetic Agents/*pharmacology , Calcium Channel Blockers/*pharmacology , Calcium Channels/*metabolism , Cyclohexylamines/*pharmacology , Indoles/*pharmacology , Mesenteric Arteries/*drug effects , Naphthalenes/*pharmacology, Animals ; Calcium/metabolism ; Dose-Response Relationship, Drug ; Extracellular Space/drug effects ; Extracellular Space/metabolism ; Male ; Mesenteric Arteries/cytology ; Mesenteric Arteries/metabolism ; Mesenteric Arteries/physiology ; Methoxamine/pharmacology ; Potassium Chloride/pharmacology ; Rabbits ; Receptors, Calcium-Sensing/metabolism ; Vasoconstriction/drug effects ; Vasodilation/drug effects
مستخلص: The present study investigates the effect of commonly used negative and positive allosteric modulators of the calcium-sensing receptor (CaSR) on vascular reactivity. In wire myography studies, increasing [Ca 2+ ] o from 1mM to 6mM induced concentration-dependent relaxations of methoxamine-induced pre-contracted rabbit mesenteric arteries, with 6mM [Ca 2+ ] o producing almost complete relaxation. [Ca 2+ ] o -induced relaxations were attenuated in the presence of the calcilytics Calhex-231 and NPS 2143, and abolished by the removal of the endothelium. In addition to their calcilytic effects, Calhex-231 and NPS 2143 also produced concentration-dependent inhibitions of methoxamine- or KCl-induced precontracted tone, which were unaffected by removal of the endothelium and unopposed in the presence of the calcimimetic Calindol. In vessels with depleted Ca 2+ stores, contractions mediated by Ca 2+ influx via voltage-gated Ca 2+ channels (VGCCs) were inhibited by Calhex231. In freshly isolated single rabbit mesenteric artery smooth muscle cells, Calhex-231 and NPS 2143 inhibited whole-cell VGCC currents. Application of Calindol also inhibited methoxamine- and KCl-induced pre-contracted tone, and inhibited whole-cell VGCC currents. In conclusion, in addition to their CaSR-mediated actions in the vasculature, Calhex-231, NPS 2143 and Calindol reduce vascular contractility via direct inhibition of VGCCs.
(Copyright © 2016 The Authors. Published by Elsevier B.V. All rights reserved.)
References: Mol Pharmacol. 2009 Dec;76(6):1131-44. (PMID: 19779033)
Br J Pharmacol. 2008 Jun;154(3):652-62. (PMID: 18414396)
Cardiovasc Res. 2009 Feb 1;81(2):260-8. (PMID: 18852253)
PLoS One. 2012;7(1):e30682. (PMID: 22295103)
Transplant Proc. 2009 Jul-Aug;41(6):2385-7. (PMID: 19715927)
Am J Physiol Regul Integr Comp Physiol. 2010 Oct;299(4):R1020-6. (PMID: 20660105)
PLoS One. 2014 Dec 15;9(12):e115178. (PMID: 25506941)
Lancet. 2005 Jun 25-Jul 1;365(9478):2237-9. (PMID: 15978932)
Hypertension. 1997 Dec;30(6):1431-9. (PMID: 9403564)
Am J Physiol Cell Physiol. 2016 Feb 1;310(3):C193-204. (PMID: 26538090)
Hypertension. 2002 Feb;39(2):251-7. (PMID: 11847193)
Vascul Pharmacol. 2016 May;80:75-84. (PMID: 26772767)
Am J Hypertens. 2005 Mar;18(3):364-71. (PMID: 15797655)
Annu Rev Med. 2006;57:349-64. (PMID: 16409154)
Br J Pharmacol. 2011 Oct;164(3):884-93. (PMID: 21410453)
Beilstein J Org Chem. 2013 Jul 09;9:1383-7. (PMID: 23946832)
J Pharmacol Exp Ther. 1999 Apr;289(1):245-50. (PMID: 10087011)
Br J Pharmacol. 2011 Feb;162(3):749-62. (PMID: 20958288)
Circulation. 2005 Jun 14;111(23):3105-11. (PMID: 15939821)
Am J Physiol Renal Physiol. 2007 Sep;293(3):F946-55. (PMID: 17537980)
J Pharmacol Exp Ther. 2001 Oct;299(1):323-31. (PMID: 11561095)
Sci Transl Med. 2015 Apr 22;7(284):284ra60. (PMID: 25904744)
Circ Res. 2012 Aug 3;111(4):469-81. (PMID: 22730443)
J Endocrinol. 2006 Oct;191(1):189-95. (PMID: 17065402)
Br J Pharmacol. 2012 Jan;165(1):35-48. (PMID: 21627634)
Biochem Biophys Res Commun. 2006 Mar 31;342(1):153-63. (PMID: 16472767)
Biochem Biophys Res Commun. 2006 Oct 6;348(4):1215-23. (PMID: 16919596)
Curr Neuropharmacol. 2007 Sep;5(3):180-6. (PMID: 19305800)
J Am Soc Nephrol. 2006 Mar;17(3):655-62. (PMID: 16421225)
Pharmacol Rep. 2006 Jul-Aug;58(4):533-9. (PMID: 16963800)
J Cardiovasc Pharmacol. 2013 Jun;61(6):528-35. (PMID: 23429586)
Circ Res. 2013 Feb 15;112(4):640-50. (PMID: 23300272)
Am J Physiol. 1998 May;274(5):H1655-61. (PMID: 9612376)
Kidney Int. 2010 Mar;77(5):436-42. (PMID: 20016465)
J Pharmacol Exp Ther. 2013 Jul;346(1):38-47. (PMID: 23639802)
Mol Genet Metab. 1998 Jul;64(3):198-204. (PMID: 9719629)
Nat Rev Mol Cell Biol. 2003 Jul;4(7):530-8. (PMID: 12838336)
J Physiol Pharmacol. 2010 Apr;61(2):163-70. (PMID: 20436216)
J Biomed Sci. 2011 Feb 11;18:16. (PMID: 21314926)
Reprod Sci. 2013 Aug;20(8):882-90. (PMID: 23287098)
Circ Res. 1977 Jul;41(1):19-26. (PMID: 862138)
Bone. 2011 Oct;49(4):845-52. (PMID: 21742071)
Proc Natl Acad Sci U S A. 1998 Mar 31;95(7):4040-5. (PMID: 9520489)
N Engl J Med. 1992 Jul 9;327(2):76-81. (PMID: 1603139)
J Membr Biol. 2000 Jun 1;175(3):203-12. (PMID: 10833530)
Vascul Pharmacol. 2007 Oct;47(4):222-8. (PMID: 17690018)
Bone. 2014 Jul;64:204-10. (PMID: 24769332)
Circ Res. 2005 Aug 19;97(4):391-8. (PMID: 16037572)
Circ Res. 2008 May 23;102(10):1247-55. (PMID: 18403729)
Cell Physiol Biochem. 2008;22(5-6):413-22. (PMID: 19088423)
J Biol Chem. 2003 Dec 5;278(49):49487-94. (PMID: 14506236)
Int J Clin Pract. 2012 Feb;66(2):199-209. (PMID: 22257045)
J Biol Chem. 2004 Apr 30;279(18):18990-7. (PMID: 14976203)
Eur J Pharmacol. 2016 Aug 5;784:15-21. (PMID: 27164419)
Cell Calcium. 2009 Nov-Dec;46(5-6):323-32. (PMID: 19836834)
PLoS One. 2015 Sep 16;10(9):e0138384. (PMID: 26375676)
Physiol Rev. 2001 Jan;81(1):239-297. (PMID: 11152759)
Br J Pharmacol. 1998 Dec;125(7):1397-404. (PMID: 9884066)
معلومات مُعتمدة: FS/13/10/30021 United Kingdom BHF_ British Heart Foundation; FS/15/44/31570 United Kingdom BHF_ British Heart Foundation
فهرسة مساهمة: Keywords: Calcilytic; Calcimimetic; Calcium-sensing receptor; Calhex-231; Calindol; NPS 2143
المشرفين على المادة: 0 ((R)-2-(1-(1-naphthyl)ethyl-aminom-ethyl)indole)
0 (Benzamides)
0 (Calcimimetic Agents)
0 (Calcium Channel Blockers)
0 (Calcium Channels)
0 (Cyclohexylamines)
0 (Indoles)
0 (N(1)-(4-chlorobenzoyl)-N(2)-(1-(1-naphthyl)ethyl)-1,2-diaminocyclohexane)
0 (N-(2-hydroxy-3-(2-cyano-3-chlorophenoxy)propyl)-1,1-dimethyl-2-(2-nephthyl)ethylamine)
0 (Naphthalenes)
0 (Receptors, Calcium-Sensing)
660YQ98I10 (Potassium Chloride)
HUQ1KC1YLI (Methoxamine)
SY7Q814VUP (Calcium)
تواريخ الأحداث: Date Created: 20161012 Date Completed: 20170404 Latest Revision: 20240603
رمز التحديث: 20240603
مُعرف محوري في PubMed: PMC5127511
DOI: 10.1016/j.ejphar.2016.10.008
PMID: 27725162
قاعدة البيانات: MEDLINE
الوصف
تدمد:1879-0712
DOI:10.1016/j.ejphar.2016.10.008