Linked Life Data

17300166

Source:http://linkedlifedata.com/resource/pubmed/id/17300166

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
2007-2-15
pubmed:abstractText
The neurohypophyseal peptides arginine vasopressin (AVP) and oxytocin (OT) mediate a wide variety of peripheral and central physiological and behavioral effects by acting on four different G-protein coupled receptors, termed V1a (vascular), V1b (pituitary), V2 (renal), and OT (uterine). We recently reported that d[Cha4]AVP (A), d[Leu4]AVP (B), d[Orn4]AVP (C), and d[Arg4]AVP (D) have high affinity and are selective agonists for the human V1b receptor. However, peptides A-D were subsequently shown to be potent antidiuretic agonists in the rat and are, thus, not selective V1b agonists in the rat. Peptides A-D served as leads for the studies reported here. They were modified at position 8 by Lys, ornithine (Orn), diaminobutyric acid (Dab), and diaminopropionic acid (Dap) to give d[Cha4,Lys8]VP (1), d[Cha4,Orn8]VP (2), d[Cha4,Dab8]VP (3), d[Cha4,Dap8]VP (4), d[Leu4,Lys8]VP (5), d[Leu4,Orn8]VP (6), d[Leu4,Dab8]VP (7), d[Leu4,Dap8]VP (8), d[Orn4,Lys8]VP (9), d[Orn4,Orn8]VP (10), d[Arg4,Lys8]VP (11), d[Arg4,Orn8]VP (12), and d[Arg4,Dab8]VP (13). All peptides were synthesized by the Merrifield solid-phase method. Their binding and functional properties were evaluated in rat AVP V1a, V1b, and V2 receptors and on the rat OT receptor expressed either in native tissues or in stably transfected cells. They were also examined in rat vasopressor, antidiuretic, and in in vitro (no Mg++) oxytocic assays. Functional studies performed on chinese hamster ovary cells expressing the different AVP/OT receptors confirm that d[Cha4,Lys8]VP (1), d[Cha4,Dab8]VP (3), d[Leu4,Lys8]VP (5), and d[Leu4,Dap8]VP (8) are the first selective agonists for the rat V1b receptor. These selective V1b agonists are promising new tools for studies of the role of the V1b receptor in the rat.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
22
pubmed:volume
50
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
835-47
pubmed:dateRevised
2007-12-3
pubmed:meshHeading
pubmed-meshheading:17300166-Adenylate Cyclase, pubmed-meshheading:17300166-Animals, pubmed-meshheading:17300166-Antidiuretic Agents, pubmed-meshheading:17300166-Arginine Vasopressin, pubmed-meshheading:17300166-Cell Line, pubmed-meshheading:17300166-Cricetinae, pubmed-meshheading:17300166-Cricetulus, pubmed-meshheading:17300166-Drug Design, pubmed-meshheading:17300166-Inositol Phosphates, pubmed-meshheading:17300166-Oligopeptides, pubmed-meshheading:17300166-Oxytocics, pubmed-meshheading:17300166-Peptides, Cyclic, pubmed-meshheading:17300166-Protein Isoforms, pubmed-meshheading:17300166-Radioligand Assay, pubmed-meshheading:17300166-Rats, pubmed-meshheading:17300166-Receptors, Oxytocin, pubmed-meshheading:17300166-Receptors, Vasopressin, pubmed-meshheading:17300166-Structure-Activity Relationship, pubmed-meshheading:17300166-Vasoconstrictor Agents
pubmed:year
2007
pubmed:articleTitle
Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8.
pubmed:affiliation
Institut de Génomique Fonctionnelle, CNRS UMR 5203-INSERM U.661, Université Montpellier I et II, 34094 Montpellier Cedex 05, France.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural