Kenneth Lee Hauser

A selective inhibitor of serotonin uptake: Lilly 110140, 3-(p-Trifluoromethylphenoxy)-n-methyl-3-phenylpropylamine

Abstract Lilly 110140 is a highly selective inhibitor of serotonin uptake into synaptosomes of rat brain, unlike previous monoamine uptake inhibitors that also inhibit the uptake of norepinephrine and dopamine. Lilly 110140 should be useful in studying the function of serotoninergic neurons and may be helpful in clariying the role of serotonin in certain types of mental depression.

Reversal of resistance in multidrug resistance protein (MRP1)-overexpressing cells by LY329146.

The benzothiophene LY329146 reverses the drug resistance phenotype in multidrug resistance protein (MRP1)-overexpressing cells when dosed in combination with MRP1-associated oncolytics doxorubicin and vincristine. Additionally, LY329146 inhibited MRP1-mediated uptake of the MRP1 substrate LTC4 into membrane vesicles prepared from MRP1-overexpressing cells.

Chiral recognition of the angiotensin II (AT1) receptor by a highly potent phenoxyproline octanoamide

Abstract The synthesis and in vitro biological evaluation of a novel series of diastereomeric phenoxyproline octanoamides ( 3–h ) as angiotensin II (AT 1 ) receptor antagonists are reported.

Approaches to the chemical synthesis of the prostaglandins

This is a detailed report of efforts to synthesize compounds related to PGE1 (prostaglandin E1). Basically the approach involved attaching 1 or both of the side chains to an appropriately substituted benzene ring and subsequently converting the aromatic nucleus to the cyclopentane system. The chemical structure in each step of the process is diagrammed.

Synthesis and pharmacological evaluation of a novel series of 5-aryl benzimidazole angiotensin II receptor antagonists

Abstract A novel series of benzimidazole angiotensin II (Ang II) receptor antagonists (4, 13, 5, 17) were synthesized and compared pharmacologically to the previously described imidazole analogues (1, 3a-b).