Recent efforts in the field of thrombin inhibitor research have focused on the identification of
compounds with good oral bioavailability and pharmacokinetics. In this manuscript we …

In an effort to discover potent, clinically useful thrombin inhibitors, a rapid analogue synthetic
approach was used to explore the P 1 region. Various benzylamines were coupled to a …

A growing body of evidence has implicated the calcitonin gene–related peptide (CGRP)
receptors in migraine pathophysiology. With the approval of monoclonal antibodies targeting …

Novel 3-cyanoisoquinoline Kv1.5 antagonists have been prepared and evaluated in in vitro
and in vivo assays for inhibition of the Kv1.5 potassium channel and its associated cardiac …

Calcitonin gene-related peptide (CGRP) has long been hypothesized to play a key role in
migraine pathophysiology, and the advent of small-molecule antagonists has clearly …

The specificities of orphenadrine and methimazole on eight human liver P450 enzyme
activities were evaluated by studying the extent of inhibition at different concentrations in two …

In vitro methods were used to identify the cytochrome P450 (GYP) enzyme (s) involved in S-mephenytoin
N-demethylation. S-Mephenytoin (200 tM) was incubated with human liver …

A new series of imidazopyridine CB2 agonists is described. Structural optimization improved
CB2/CB1 selectivity in this series and conferred physical properties that facilitated high in …

In this manuscript we demonstrate that a modification principally directed toward the improvement
of the aqueous solubility (ie, introduction a P3 pyridine N-oxide) of the previous lead …

RP 73401 is a potent inhibitor of cyclic nucleotide phosphodiesterase type IV. RP 73401 is
metabolized by human liver microsomes almost exclusively by transhydroxylation of the …