Progress in the development of potent bombesin receptor antagonists
Article Abstract:
Bombesin receptor antagonists can be classified into four distinct analogue classes exhibiting various structure-function properties. These four classes are designated as analogues of D-amino acid-substituted substance P, D-amino acid His12-substituted bombesin, reduced peptide bond bombesin and desMet14 bombesin or desMet27 gastrin releasing peptide. The desMet analogues exhibit the greatest potency and selectivity among the four classes of receptor antagonists. Moreover, receptor affinity studies in the gastrointestinal and CNS tissues show that bombesin receptors can be characterized using the classification of the four receptor antagonists.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1991
User Contributions:
Comment about this article or add new information about this topic:
Clinical development of endothelin receptor antagonists
Article Abstract:
Clinical trials involving endothelin (ET) receptor antagonists are being developed in relation to the field of pharmacology. M. Yanagisawa of the University of Texas Southwestern initiated the development of ET knockout mice strains, ET-1, ET-3 and ETB. ET1 is being associated in the pathogenesis of primary and secondary pulmonary hypertension and lung allograft transplant failure. ET antagonists are considered as primary therapeutic agents for congestive heart failure. Other therapeutic strategies such as bosentan therapy are also being tested clinically.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1997
User Contributions:
Comment about this article or add new information about this topic:
Peptide YY and neuropeptide Y: two peptides intimately involved in electrolyte homeostasis
Article Abstract:
Studies have suggested that peptide YY (PYY) and neuropeptide Y (NPY) play a vital role in controlling homeostatic mechanisms by actions upon gastrointestinal and renal targets. PYY may well be responsible for the setting of the overall 'tone' of electrolyte homeostasis while NPY functions as a 'fine control' in local target areas. The availability of selective antagonists and stable agonist analogues has increased the understanding of the pharmacology of PYY and NPY.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1996
User Contributions:
Comment about this article or add new information about this topic:
- Abstracts: Recent developments with neuropeptide Y receptor antagonists. The role of neuropeptide Y in cardiovascular regulation
- Abstracts: Clinical evaluation of 5-HT3 receptor antagonists as anti-emetics. The 5-HT(sub 4) receptor: a place in the sun
- Abstracts: Clarke and Bond reply. Keeping an eye on the I site: imidazoline-preferring receptors