« Previous AbstractComparative topical pheromonotropic activity of insect pyrokinin/PBAN amphiphilic analogs incorporating different fatty and/or cholic acid components    Next Abstract"An amphiphilic, PK/PBAN analog is a selective pheromonotropic antagonist that penetrates the cuticle of a heliothine insect" »

Peptides

Title:		Enhanced oral availability/pheromonotropic activity of peptidase-resistant topical amphiphilic analogs of pyrokinin/PBAN insect neuropeptides
Author(s):		Nachman RJ; Teal PE; Strey A;
Address:		"Areawide Pest Management Research Unit, Southern Plains Agricultural Research Center, USDA, ARS, College Station, TX 77845, USA. nachman@tamu.edu"
Journal Title:		Peptides
Year:		2002
Volume:		23
Issue:		11
Page Number:		2035 - 2043
DOI:		10.1016/s0196-9781(02)00191-2
ISSN/ISBN:		0196-9781 (Print) 0196-9781 (Linking)
Abstract:		"The peptide bond between active core residues Pro and Arg is the primary site of susceptibility for the pyrokinin/PBAN neuropeptides to insect tissue-bound peptidases, and incorporation of modified Pro residues can enhance resistance to peptidase hydrolysis. An Hyp-containing amphiphilic analog (Hex-FT[Hyp]RLa) is shown to operate as a topically active tissue-bound peptidase-resistant analog of the pyrokinin/PBAN class of insect neuropeptides in adult Heliothis virescens moths. An Oic amphiphilic analog (Hex-FT[Oic]RLa) is ineffective topically, but proves to be a superior tissue-bound, peptidase-resistant pyrokinin/PBAN analog for oral administration; outperforming both the Hyp analog and the orally inactive natural hormone PBAN in the moths. The Oic analog is effective in penetrating an isolated, ligated foregut preparation, but less successful in transmigrating an isolated midgut preparation; whereas the opposite behavior is observed for the Hyp analog. The success of the Oic analog via oral administration may be related to its ability to effectively penetrate the foregut, thereby bypassing the hostile environment of the midgut region"
Keywords:		"Administration, Oral Animals Biological Availability Insecta/*chemistry Neuropeptides/administration & dosage/pharmacokinetics/*pharmacology Peptide Hydrolases/*metabolism Pheromones/administration & dosage/pharmacokinetics/*pharmacology;"
Notes:		"MedlineNachman, Ronald J Teal, Peter E A Strey, Allison eng 2002/11/15 Peptides. 2002 Nov; 23(11):2035-43. doi: 10.1016/s0196-9781(02)00191-2"