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Several azaline B analogs (2–10) were synthesized and evaluated for their ability to antagonize GnRH in vitro and for duration of action in inhibiting luteinizing hormone secretion in a castrated male rat assay in vivo. Analogs, 8 (IC 50 =1.85nM), and 9 (IC 50 =1.78nM), are equipotent with azaline B (1, IC 50 =1.36nM) in vitro. Whereas 9 is short acting, 8 is as long acting...
The venoms of cone snails are rich in multiply disulfide-crosslinked peptides, the conotoxins. Conotoxins are grouped into families on the basis of shared cysteine patterns and homologous molecular targets. For example, both the κA- and αA-conotoxin families share the same Class IV Cys pattern (-CC-C-C-C-C-), but differ in their molecular targets. The κA-conotoxins are excitatory toxins that purportedly...
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