作者: B. H. Vickery
DOI: 10.1007/978-94-009-3229-6_13
关键词: Reproductive physiology 、 In vitro 、 Serotonin 、 In vivo 、 Potency 、 Pharmacology 、 Biology 、 Receptor 、 Peptide 、 Histamine
摘要: Competitive antagonism of LHRH at its pituitary receptors by a peptide administered systemically would be expected, because the hemodilution involved, to require dauntingly large dose effective. Nonetheless, chemical manipulation and substitution in molecule [1–3] have now resulted agents whose potency is sufficient permit clinical evaluation humans [4,5]. Pharmacological these peptides has demonstrated them powerful tools for dissecting reproductive physiology suggests that they may find contraceptive therapeutic niches as drugs which do not duplicate utilities agonist analogs. However, studies also sounded cautionary note since many degranulate mast cells with consequent release mediators including histamine serotonin. Available analogs differ their histamine-releasing relative antagonizing vitro [6] vivo [7], leading expectation further able separate two activities [8–10].