Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-2
pubmed:dateCreated
2005-7-18
pubmed:abstractText
Self-association properties of CS-088, an antiglaucoma ophthalmic agent, were investigated. Various analytical methods, such as surface tension measurement, demonstrated that CS-088 is a self-associating compound with critical micellar concentration (CMC) of approximately 10 mg/mL. Light scattering analysis revealed that the micellar molecular weight (MMW) of CS-088 aggregates well above the CMC was approximately 2260, corresponding to a pentamer. In addition, the MMW corresponding to a dimer was detected by NMR spectroscopy, indicating that self-association of monomers to pentamers is via the formation of dimers. According to the Stokes-Einstein equation, hydrodynamic radii of the dimer and pentamer were calculated to be 0.87 and 1.16 nm, respectively. The concentration-dependent change in the NMR chemical shift indicated that hydrophobic interaction between biphenyl groups is an important factor in the self-association of CS-088 molecules. Furthermore, measurement of particle size distribution using a Nicomp Submicron Particle-Sizer revealed that the addition of either n-propanol or urea to CS-088 solution led to monomerization of the dimers and pentamers, suggesting that not only hydrophobic interaction but also hydrogen bonding is involved in stabilizing CS-088 aggregates. No bigger aggregate than a pentamer was formed in the absence of NaCl, whereas further aggregation was observed with increasing concentrations of NaCl.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0378-5173
pubmed:author
pubmed:issnType
Print
pubmed:day
11
pubmed:volume
299
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
100-6
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2005
pubmed:articleTitle
Self-association properties of 4-[1-hydroxy-1-methylethyl]-2-propyl-1-[4-[2-[tetrazole-5-yl]phenyl]phenyl] methylimidazole-5-carboxylic acid monohydrate (CS-088), an antiglaucoma ophthalmic agent.
pubmed:affiliation
Pharmaceutical Development Laboratories, Sankyo Co. Ltd., 1-12-1, Shinomiya, Hiratsuka, Kanagawa 254-0014, Japan. tkikuc@sankyo.co.jp
pubmed:publicationType
Journal Article