Antagonist analogs

Calcitonin, LHRH, lypressin, and somatostatin have been formulated in lactide/glycolide copolymers as injectable, controlled release formulations (117). Various agonistic and antagonistic analogs have been studied. Generally these compounds are hydrophilic polypeptides,... 

Delta opioid receptor Antagonist analog Hydroxyphenyl piperidine 153... 

Furthermore, we believe that our hypothesis regarding design of antagonist analogs with prolonged activity offers a potentially useful approach to peptide drug design. 

At present, pituitary hormones—and potent antagonist analogs of GnRH—are receiving increased attention. A GnRH antagonist in combination with testosterone has been shown to produce reversible azoospermia in nonhuman primates. 

Rekasi Z, Schally AV (1993) A method for evaluation of activity of antagonistic analogs growth hormone-releasing hormone in a superfusion system. Proc Natl Acad Sci USA 90 2146-2149... 

Table 2.4 Binding and Cyclase Activity of Selected Antagonist Analogs of PTH with Bone-Derived ROS 17/2.8 Cells...

Neurohormones are structurally diverse so that it is possible to synthesize a wide array of agonistic or antagonistic analogs. 

Receptor Antagonists Development of Oxytocin and Glucagon Antagonist Analogs... 

On the other hand, the evidence we have obtained with [l-penicillamine]-oxy-tocin antagonist analogs strongly supports a central role of the Tyr-2 and Asn-5 side chain for the transduction process (see [14] for a review). In particular we have shown, primarily by NMR and CD methods, that [Pen ]oxytocin (replacement of the Cys-1 residue (-CHj-S- side chain) by a Pen-1 residue (-C(CH3)2-S- side chain)... 

The development of a glucagon antagonist which lowers blood glucose levels in diabetic animals [66] illustrates the importance of careful binding studies in conjunction with full dose-response analysis of activity. In addition these studies provide another illustration of the manner in which steric changes which cause conformational perturbations apparently can lead to antagonist analogs. 

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