Reproductive Physiology and General Pharmacology of LHRH Antagonists

作者: B. H. Vickery

DOI: 10.1007/978-94-009-3229-6_13

关键词: Reproductive physiologyIn vitroSerotoninIn vivoPotencyPharmacologyBiologyReceptorPeptideHistamine

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].

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