Results 121 to 130 of about 1,525 (166)

Analogs of 3-quinuclidinyl benzilate

Journal of Medicinal Chemistry, 1982
A number of analogues of 3-quinuclidinyl benzilate (QNB) have been synthesized and their affinities to muscarinic receptor from rat or dog ventricular muscle measured. We have determined that the muscarinic receptor can to a different degree accommodate either a halogen in the ortho, meta, or para position of one phenyl ring or the replacement of one ...
W J, Rzeszotarski, R E, Gibson, W C, Eckelman, D A, Simms, E M, Jagoda, N L, Ferreira, R C, Reba   +6 more
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SYNTHESIS OF 3-QUINUCLIDINYL BENZILATE DERIVATIVES

Organic Preparations and Procedures International, 1990
(1990). SYNTHESIS OF 3-QUINUCLIDINYL BENZILATE DERIVATIVES. Organic Preparations and Procedures International: Vol. 22, No. 1, pp. 87-94.
G. W. Kabalka, S. B. Mathur, Y.-Z. Gai
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Syntheses and Biological Properties of Chiral Fluoroalkyl Quinuclidinyl Benzilates

Journal of Medicinal Chemistry, 1995
Previously, (R)-quinuclidinyl (R)-4-iodobenzilate ((R,R)-IQNB), a muscarinic receptor antagonist, has been labeled with 123I and 125I for use in in vitro and in vivo studies in animals and humans. We have prepared fluoroalkyl analogs of QNB, which are amenable to labeling with 18F, for potential imaging applications with positron emission tomography ...
D O, Kiesewetter, J V, Silverton, W C, Eckelman   +2 more
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3-Quinuclidinyl Benzilate Hydrolysis in Dilute Aqueous Solution

Journal of Pharmaceutical Sciences, 1979
The hydrolysis kinetics of 3-quinuclidinyl benzilate were determined over the pH 0-14 range at different temperatures in solutions buffered to a constant pH. Analysis of data extrapolated to zero buffer concentrations permitted construction of an overall rate expression for pH 0-14 and 0-100 degrees. Reaction mechanisms are discussed.
L A, Hull, D H, Rosenblatt, J, Epstein
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Binding kinetics of quinuclidinyl benzilate and methyl-quinuclidinyl benzilate enantiomers at neuronal (M1), cardiac (M2), and pancreatic (M3) muscarinic receptors.

Molecular Pharmacology, 1991
We analyzed the competition kinetics of quinuclidinyl benzilate (QNB) and QNB methiodide enantiomers on human NB-OK1 neuroblastoma (M1), rat cardiac (M2), and rat pancreas (M3) muscarinic binding sites. The association rate constants of the four drugs depended on the receptor subtype studied and were lower with pancreas (M3) (1-9 x 10(5) M-1 sec-1 ...
Waelbroeck, Magali, Tastenoy, Michèle, Camus, Jean Claude, Christophe, Jean   +3 more
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ChemInform Abstract: ANALOGS OF 3‐QUINUCLIDINYL BENZILATE

Chemischer Informationsdienst, 1983
AbstractGemäß Formelschema werden die Verbindungen (VI) und (IX) hergestellt.
W. J. RZESZOTARSKI, R. E. GIBSON, W. C. ECKELMAN, D. A. SIMMS, E. M. JAGODA, N. L. FERREIRA, R. C. REBA   +6 more
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THE DISTRIBUTION OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR ANTAGONISTS, QUINUCLIDINYL BENZILATE AND QUINUCLIDINYL BENZILATE METHIODIDE (BOTH TRITIATED), IN RAT, GUINEA PIG, AND RABBIT

Journal of Computer Assisted Tomography, 1980
The distribution of [3H]quinuclidinyl benzilate and its methiodide salt was determined in rat, guinea pig, and rabbit. Accumulation in the myocardium of up to 2% of the injected dose per gram of tissue was obtained with both compounds, providing heart-to-blood ratios of approximately 30 and heart-to-lung ratios of approximately 4.
R. E. Gibson, W. C. Eckelman, F. Vieras, R. C. Reba, M. J. Welch   +4 more
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Two-step isomerization of quinuclidinyl benzilate-muscarinic receptor complex

Neurochemistry International, 1988
A kinetic analysis was made of the dissociation reaction of the muscarinic receptor-l-[(3)H]quinuclidinyl benzilate complex at 25 degrees C in 0.05 M K-phosphate buffer. The course of the reaction was followed by the decrease in the concentration of the membrane-bound radiolabelled antagonist while rebinding was prevented by the excess of ...
M, Eller, J, Järv
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Autoradiographic Localization of Quinuclidinyl Benzilate Binding to Rat Pituitary Gland

Neuroendocrinology, 1983
The location of muscarinic receptors in the rat pituitary gland was examined with an autoradiographic technique. Slides containing 10 or 20 micron horizontal sections of tissue were incubated in a solution of 1 n M[3H]quinuclidinyl benzilate (QNB) in phosphate-buffered saline to label muscarinic receptors.
Hoover, Donald B., Hancock, J. C.
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Kinetic aspects of l-quinuclidinyl benzilate interaction with muscarinic receptor

Neurochemistry International, 1988
l-Quinuclidinyl benzilate is undoubtedly the most widely used radioactive reporter ligand for studies on muscarinic receptor. In the present Commentary the kinetic aspects of the interaction of this ligand with muscarinic receptor are summarized. On the basis of these results a kinetic mechanism has been proposed involving consequential isomerization ...
J, Järv, M, Eller
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