Linked Life Data

8919643

Source:http://linkedlifedata.com/resource/pubmed/id/8919643

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1997-1-10
pubmed:abstractText
1. We characterized the binding sites of VA-045 [(+)-eburunamenine-14- carboxylic acid (2-nitroxyethyl)ester] in the rat brain. 2. VA-045 showed no affinity for various types of well-known neurotransmitter-related receptors or channels. However, radiolabeled VA-045 ([3H]VA-045) bound to rat brain membranes in a saturable and reversible manner. The Kd and Bmax values of [3H]VA-045 binding were 58.2 nM and 2685 fmol/mg of protein, respectively. 3. The largest specific binding of [3H]VA-045 was observed in the cerebellum, among seven brain regions, and in subcellular synaptosomes. 4. Specific binding of [3H]VA-045 was inhibited by VA-045 (Ki = 0.06 microM), a levorotatory enantiomer of VA-045 (VA-213) and its structural analog, vinpocentine. Moreover, compounds with calmodulin antagonistic activity inhibited the [3H]VA-045 binding. 5. These results suggest that VA-045 binds to specific sites, which may resemble calmodulin, on synaptic membranes in the brain.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0306-3623
pubmed:author
pubmed:issnType
Print
pubmed:volume
27
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
279-84
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1996
pubmed:articleTitle
Partial characterization of binding sites of VA-045, a novel apovincaminic acid derivative, in rat brain membranes.
pubmed:affiliation
Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
pubmed:publicationType
Journal Article, Comparative Study