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Pharmacological profile of NPC 12626, a novel, competitive N-methyl-D-aspartate receptor antagonist.
- J. Ferkany, D. Kyle, S. Borosky
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 July 1989
The results of the current study indicate that NPC 12626 is a novel, systemically active and competitive NMDA receptor antagonist.
A novel m2-selective muscarinic antagonist: binding characteristics and autoradiographic distribution in rat brain
Receptor-binding radiotracers: a class of potential radiopharmaceuticals.
- W. Eckelman, R. Reba, B. Francis
- Biology, MedicineJournal of nuclear medicine : official…
- 1 April 1979
Theoretical calculations showed that derivatives binding to the estrogen receptor, the beta adrenoceptor, or the cholinergic receptor are capable of achieving satisfactory target-to-blood ratios.
External imaging of cerebral muscarinic acetylcholine receptors.
A radioiodinated ligand that binds to muscarinic acetylcholine receptors was shown to distribute in the brain by a receptor-mediated process, showing good definition of the caudate putamen and cortex in man.
In vivo competition studies with analogues of 3-quinuclidinyl benzilate.
There is a linear correlation between the ability to compete with (-)-[3H]I for the m-AChR and the affinity constant of the analogue as determined by in vitro assay, suggesting that the test is a valid indicator of in vivo distribution.
Pharmacologic profile of NPC 168 (naltrexone phenyl oxime), a novel compound with activity at opioid receptors
Irreversible enzyme inhibitors. CIV. Inhibitors of thymidine phosphorylase. 8. Further studies on hydrophobic bonding with 6-substituted uracils.
Preliminary Clinical Evaluation of Glybenclamide in Treatment of Diabetes Mellitus
The results to date do not suggest that this compound is clinically advantageous to other orally active hypoglycemic agents, but greatly enhanced activity compared to other sulfonylureas may be due to increased hydrophobic bonding to the receptor vicinity.
Chemical and biologic properties of isolated radiolabeled bleomycin preparations.
- W. Eckelman, W. Rzeszotarski, R. C. Rebra
- ChemistryJournal of nuclear medicine : official…
- 1 November 1975
It appears that the major components A2 and B2 are the most useful for diagnostic tumor imaging.
[I-125] 17α-Iodovinyl 11β-Methoxyestradiol: In Vivo and In Vitro Properties of a High-Affinity Estrogen-Receptor Radiopharmaceutical
By in vivo competition studies with nonradioactive estradiol, it is found that 95% of the [I-125]MIVE2 bound in the uterus is specifically bound to estrogen receptors.