While insect neuropeptides of the insect kinin (IK) and pyrokinin/PBAN (PK/PBAN) family are both potent and specific, these molecular messengers are not suitably designed to be effective either as pest insect control agents and/or tools for insect neuroendocrinologists. Neuropeptides are rapidly degraded by peptidases in the hemolymph and tissues within insects and generally exhibit poor bioavailability (Nachman et al. 2001, 2002a, b). The development of potent agonists and antagonists with enhanced biostability and bioavailability can overcome these limitations and can represent a key step in the development of pest management techniques based on neuropeptide analogs capable of disrupting critical life processes regulated by the IK and PK/PBAN families. In two separate sub-sections, a review is presented on what is known about chemical, conformational, and stereochemical aspects of the interaction of the IK and PK/PBAN families with their putative receptors, and how this knowledge can be harnessed to design and develop biostable mimetic analogs that retain an ability to bind, and potentially activate, those receptors. Strategies for the modification of the PK/PBAN neuropeptides to enhance bioavailability characteristics are also discussed and should be applicable to other insect neuropeptide classes.