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Article: Antiplatelet and antiproliferative effects of SCH 51866, a novel type 1 and type 5 phosphodiesterase inhibitor

TitleAntiplatelet and antiproliferative effects of SCH 51866, a novel type 1 and type 5 phosphodiesterase inhibitor
Authors
Issue Date1996
PublisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/
Citation
Journal Of Cardiovascular Pharmacology, 1996, v. 28 n. 6, p. 862-869 How to Cite?
AbstractSCH 51866 is a potent and selective PDE1 and PDE5 inhibitor. The antiplatelet, antiproliferative, and hemodynamic effects of SCH 51866 were compared with those of E4021, a highly selective PDE5 inhibitor. SCH 51866 inhibited PDE1 and PDE5 isozymes with a 50% inhibitory concentration (IC50) of 70 and 60 nM, respectively. SCH 51866 and E4021 inhibited washed human platelet aggregation induced by collagen with an IC50 of 10 and 4 μM, respectively, and attenuated (p < 0.05) the adhesion of 111indium-labeled platelets to the nylon filament injured rat aorta. The doses of SCH 51866 and E4021 that inhibited platelet adhesion caused significant increases in platelet cyclic guanosine monophosphate (cGMP; p < 0.05). SCH 51866 (1-10 mg/kg, p.o. twice daily) but not E4021 (3-30 mg/kg, p.o. twice daily) inhibited neointima formation in the carotid arteries of spontaneously hypertensive rats (SHRs) subjected to balloon angioplasty. Moreover, SCH 51866 (0.3-10 mg/kg, p.o.) elicited dose-dependent reduction in blood pressure in SHRs, whereas E4021 (3-30 mg/kg, p.o.) did not affect blood pressure in SHRs. In conclusion, the data suggest that inhibition of PDE1 and PDE5 isozymes by SCH 51866 exerts antiplatelet and vascular protective effects. In comparison, inhibition of PDE5 alone by E4021 exhibited antiplatelet effects without affecting neointima formation.
Persistent Identifierhttp://hdl.handle.net/10722/170058
ISSN
2015 Impact Factor: 2.462
2015 SCImago Journal Rankings: 0.962
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorVemulapalli, Sen_US
dc.contributor.authorWatkins, RWen_US
dc.contributor.authorChintala, Men_US
dc.contributor.authorDavis, Hen_US
dc.contributor.authorAhn, HSen_US
dc.contributor.authorFawzi, Aen_US
dc.contributor.authorTulshian, Den_US
dc.contributor.authorChiu, Pen_US
dc.contributor.authorChatterjee, Men_US
dc.contributor.authorLin, CCen_US
dc.contributor.authorSybertz, EJen_US
dc.date.accessioned2012-10-30T06:05:03Z-
dc.date.available2012-10-30T06:05:03Z-
dc.date.issued1996en_US
dc.identifier.citationJournal Of Cardiovascular Pharmacology, 1996, v. 28 n. 6, p. 862-869en_US
dc.identifier.issn0160-2446en_US
dc.identifier.urihttp://hdl.handle.net/10722/170058-
dc.description.abstractSCH 51866 is a potent and selective PDE1 and PDE5 inhibitor. The antiplatelet, antiproliferative, and hemodynamic effects of SCH 51866 were compared with those of E4021, a highly selective PDE5 inhibitor. SCH 51866 inhibited PDE1 and PDE5 isozymes with a 50% inhibitory concentration (IC50) of 70 and 60 nM, respectively. SCH 51866 and E4021 inhibited washed human platelet aggregation induced by collagen with an IC50 of 10 and 4 μM, respectively, and attenuated (p < 0.05) the adhesion of 111indium-labeled platelets to the nylon filament injured rat aorta. The doses of SCH 51866 and E4021 that inhibited platelet adhesion caused significant increases in platelet cyclic guanosine monophosphate (cGMP; p < 0.05). SCH 51866 (1-10 mg/kg, p.o. twice daily) but not E4021 (3-30 mg/kg, p.o. twice daily) inhibited neointima formation in the carotid arteries of spontaneously hypertensive rats (SHRs) subjected to balloon angioplasty. Moreover, SCH 51866 (0.3-10 mg/kg, p.o.) elicited dose-dependent reduction in blood pressure in SHRs, whereas E4021 (3-30 mg/kg, p.o.) did not affect blood pressure in SHRs. In conclusion, the data suggest that inhibition of PDE1 and PDE5 isozymes by SCH 51866 exerts antiplatelet and vascular protective effects. In comparison, inhibition of PDE5 alone by E4021 exhibited antiplatelet effects without affecting neointima formation.en_US
dc.languageengen_US
dc.publisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/en_US
dc.relation.ispartofJournal of Cardiovascular Pharmacologyen_US
dc.subject.mesh3',5'-Cyclic-Gmp Phosphodiesterases - Antagonists & Inhibitorsen_US
dc.subject.meshAnimalsen_US
dc.subject.meshArteries - Cytology - Injuries - Physiopathologyen_US
dc.subject.meshBlood Platelets - Drug Effects - Metabolismen_US
dc.subject.meshCattleen_US
dc.subject.meshCell Divisionen_US
dc.subject.meshCyclic Nucleotide Phosphodiesterases, Type 5en_US
dc.subject.meshDogsen_US
dc.subject.meshEnzyme Inhibitors - Pharmacologyen_US
dc.subject.meshHumansen_US
dc.subject.meshHypertension - Drug Therapyen_US
dc.subject.meshImidazoles - Pharmacologyen_US
dc.subject.meshNucleotides, Cyclic - Metabolismen_US
dc.subject.meshPhosphodiesterase Inhibitors - Pharmacologyen_US
dc.subject.meshPhosphoric Diester Hydrolases - Metabolismen_US
dc.subject.meshPiperidines - Pharmacologyen_US
dc.subject.meshPlatelet Aggregation Inhibitors - Pharmacologyen_US
dc.subject.meshQuinazolines - Pharmacologyen_US
dc.subject.meshRatsen_US
dc.subject.meshRats, Inbred Shren_US
dc.titleAntiplatelet and antiproliferative effects of SCH 51866, a novel type 1 and type 5 phosphodiesterase inhibitoren_US
dc.typeArticleen_US
dc.identifier.emailChiu, P:pkychiu@hkucc.hku.hken_US
dc.identifier.authorityChiu, P=rp00379en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1097/00005344-199612000-00018en_US
dc.identifier.pmid8961086-
dc.identifier.scopuseid_2-s2.0-10544224533en_US
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-10544224533&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume28en_US
dc.identifier.issue6en_US
dc.identifier.spage862en_US
dc.identifier.epage869en_US
dc.identifier.isiWOS:A1996VX27900018-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridVemulapalli, S=7003838161en_US
dc.identifier.scopusauthoridWatkins, RW=25939152900en_US
dc.identifier.scopusauthoridChintala, M=6701560648en_US
dc.identifier.scopusauthoridDavis, H=7402189540en_US
dc.identifier.scopusauthoridAhn, HS=7202926229en_US
dc.identifier.scopusauthoridFawzi, A=7003745923en_US
dc.identifier.scopusauthoridTulshian, D=6602130454en_US
dc.identifier.scopusauthoridChiu, P=7202988127en_US
dc.identifier.scopusauthoridChatterjee, M=7202603616en_US
dc.identifier.scopusauthoridLin, CC=8150067300en_US
dc.identifier.scopusauthoridSybertz, EJ=7007065529en_US

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