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Article: Respective contributions of α-adrenergic and non-adrenergic mechanisms in the hypotensive effect of imidazoline-like drugs

TitleRespective contributions of α-adrenergic and non-adrenergic mechanisms in the hypotensive effect of imidazoline-like drugs
Authors
Issue Date2001
PublisherJohn Wiley & Sons Ltd. The Journal's web site is located at http://www.wiley.com/bw/journal.asp?ref=0007-1188&site=1
Citation
British Journal Of Pharmacology, 2001, v. 133 n. 2, p. 261-266 How to Cite?
Abstract1. The hypotensive effect of imidazoline-like drugs, such as clonidine, was first attributed to the exclusive stimulation of central α 2-adrenoceptors (α 2ARs). 2. However, a body of evidence suggests that non-adrenergic mechanisms may also account for this hypotension. 3. This work aims (i) to check whether imidazoline-like drugs with no α 2adrenergic agonist activity may alter blood pressure (BP) and (ii) to seek a possible interaction between such a drug and an α 2ARs agonist α-methylnoradrenaline (α-MNA). 4. We selected S23515 and S23757, two imidazoline-like drugs with negligible affinities and activities at α 2ARs but with high affinities for non-adrenergic imidazoline binding sites (IBS). 5. S23515 decreased BP dose-dependently (-27±5% maximal effect) when administered intracisternally (i.c.) to anaesthetized rabbits. The hypotension induced by S23515 (100 μg kg -1 i.c.) was prevented by S23757 (1 mg kg -1 i.c.) and efaroxan (10 μgkg -1 i.c.), while these compounds, devoid of haemodynamic action by themselves, did not alter the hypotensive effect of α-MNA (3 and 30 μg kg -1 i.c.). Moreover, the α 2ARs antagonist rauwolscine (3 μg kg -1 i.c.) did not prevent the effect of S23515. 6. Finally, whilst 3 μg kg -1 of S23515 or 0.5 μg kg -1 of α-MNA had weak hypotensive effects, the sequential i.c. administration of these two drugs induced a marked hypotension (-23±2%). 7. These results indicate that an imidazoline-like drug with no α 2-adrenergic properties lowers BP and interacts synergistically with an α 22ARs agonist.
Persistent Identifierhttp://hdl.handle.net/10722/171262
ISSN
2015 Impact Factor: 5.259
2015 SCImago Journal Rankings: 2.368
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorBruban, Ven_US
dc.contributor.authorFeldman, Jen_US
dc.contributor.authorGreney, Hen_US
dc.contributor.authorDontenwill, Men_US
dc.contributor.authorSchann, Sen_US
dc.contributor.authorJarry, Cen_US
dc.contributor.authorPayard, Men_US
dc.contributor.authorBoutin, Jen_US
dc.contributor.authorScalbert, Een_US
dc.contributor.authorPfeiffer, Ben_US
dc.contributor.authorRenard, Pen_US
dc.contributor.authorVanhoutte, Pen_US
dc.contributor.authorBousquet, Pen_US
dc.date.accessioned2012-10-30T06:13:02Z-
dc.date.available2012-10-30T06:13:02Z-
dc.date.issued2001en_US
dc.identifier.citationBritish Journal Of Pharmacology, 2001, v. 133 n. 2, p. 261-266en_US
dc.identifier.issn0007-1188en_US
dc.identifier.urihttp://hdl.handle.net/10722/171262-
dc.description.abstract1. The hypotensive effect of imidazoline-like drugs, such as clonidine, was first attributed to the exclusive stimulation of central α 2-adrenoceptors (α 2ARs). 2. However, a body of evidence suggests that non-adrenergic mechanisms may also account for this hypotension. 3. This work aims (i) to check whether imidazoline-like drugs with no α 2adrenergic agonist activity may alter blood pressure (BP) and (ii) to seek a possible interaction between such a drug and an α 2ARs agonist α-methylnoradrenaline (α-MNA). 4. We selected S23515 and S23757, two imidazoline-like drugs with negligible affinities and activities at α 2ARs but with high affinities for non-adrenergic imidazoline binding sites (IBS). 5. S23515 decreased BP dose-dependently (-27±5% maximal effect) when administered intracisternally (i.c.) to anaesthetized rabbits. The hypotension induced by S23515 (100 μg kg -1 i.c.) was prevented by S23757 (1 mg kg -1 i.c.) and efaroxan (10 μgkg -1 i.c.), while these compounds, devoid of haemodynamic action by themselves, did not alter the hypotensive effect of α-MNA (3 and 30 μg kg -1 i.c.). Moreover, the α 2ARs antagonist rauwolscine (3 μg kg -1 i.c.) did not prevent the effect of S23515. 6. Finally, whilst 3 μg kg -1 of S23515 or 0.5 μg kg -1 of α-MNA had weak hypotensive effects, the sequential i.c. administration of these two drugs induced a marked hypotension (-23±2%). 7. These results indicate that an imidazoline-like drug with no α 2-adrenergic properties lowers BP and interacts synergistically with an α 22ARs agonist.en_US
dc.languageengen_US
dc.publisherJohn Wiley & Sons Ltd. The Journal's web site is located at http://www.wiley.com/bw/journal.asp?ref=0007-1188&site=1en_US
dc.relation.ispartofBritish Journal of Pharmacologyen_US
dc.subject.meshAnimalsen_US
dc.subject.meshAntihypertensive Agents - Administration & Dosage - Pharmacologyen_US
dc.subject.meshBlood Pressure - Drug Effectsen_US
dc.subject.meshCattleen_US
dc.subject.meshCisterna Magnaen_US
dc.subject.meshCyclic Amp - Metabolismen_US
dc.subject.meshGuanosine 5'-O-(3-Thiotriphosphate) - Metabolismen_US
dc.subject.meshHt29 Cellsen_US
dc.subject.meshHemodynamics - Drug Effectsen_US
dc.subject.meshHumansen_US
dc.subject.meshImidazoles - Administration & Dosage - Pharmacologyen_US
dc.subject.meshInjectionsen_US
dc.subject.meshMaleen_US
dc.subject.meshOxazoles - Pharmacologyen_US
dc.subject.meshRabbitsen_US
dc.subject.meshRadioligand Assayen_US
dc.subject.meshReceptors, Adrenergic, Alpha - Drug Effectsen_US
dc.titleRespective contributions of α-adrenergic and non-adrenergic mechanisms in the hypotensive effect of imidazoline-like drugsen_US
dc.typeArticleen_US
dc.identifier.emailVanhoutte, P:vanhoutt@hku.hken_US
dc.identifier.authorityVanhoutte, P=rp00238en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1038/sj.bjp.0704080-
dc.identifier.pmid11350862-
dc.identifier.scopuseid_2-s2.0-0034985940en_US
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-0034985940&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume133en_US
dc.identifier.issue2en_US
dc.identifier.spage261en_US
dc.identifier.epage266en_US
dc.identifier.isiWOS:000168750800006-
dc.publisher.placeUnited Kingdomen_US
dc.identifier.scopusauthoridBruban, V=6603094282en_US
dc.identifier.scopusauthoridFeldman, J=9943510500en_US
dc.identifier.scopusauthoridGreney, H=7004179763en_US
dc.identifier.scopusauthoridDontenwill, M=7006070867en_US
dc.identifier.scopusauthoridSchann, S=6506821652en_US
dc.identifier.scopusauthoridJarry, C=7005471998en_US
dc.identifier.scopusauthoridPayard, M=7004162994en_US
dc.identifier.scopusauthoridBoutin, J=7102994898en_US
dc.identifier.scopusauthoridScalbert, E=7003716133en_US
dc.identifier.scopusauthoridPfeiffer, B=7102004093en_US
dc.identifier.scopusauthoridRenard, P=24291257400en_US
dc.identifier.scopusauthoridVanhoutte, P=7202304247en_US
dc.identifier.scopusauthoridBousquet, P=7102586122en_US

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