Bombesin receptor antagonists

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References (215)

  • A Hajri et al.

    Expression of GRP receptors in normal and cancerous pancreatic cells

    Regul Pept

    (1992)
  • RT Jensen et al.

    Progress in the development of potent bombesin receptor antagonists

    Trends Pharmacol Sci

    (1991)
  • K Tan-No et al.

    Spantide-induced antinociception in the opioid mechanism

    Regul Pept

    (1993)
  • KG Bitar et al.

    Effect of substance P/bombesin antagonists on the release of growth hormone by GHRP and GHRH

    Biochem Biophys Res Commun

    (1991)
  • A Cowan et al.

    Effects of bombesin on behavior

    Life Sci

    (1985)
  • H Mukai et al.

    Antagonism by GRP(18–27) and substance P analogues on insulin release stimulated by GRP(18–27)

    Peptides

    (1990)
  • M Spanarkel et al.

    Cholecytokinin-27-32-amide. A member of a new class of cholecystokinin receptor antagonists

    J Biol Chem

    (1983)
  • L-H Wang et al.

    Des-Met carboxyl terminal modified analogues of bombesin function as potent bombesin receptor antagonists, partial agonists, or agonists

    J Biol Chem

    (1990)
  • N Alptekin et al.

    Comparison of prolonged in vivo inhibitory activity of several potent bombesin (BN) antagonists on BN-stimulated amylase secretion in the rat

    Peptides

    (1991)
  • P Singh et al.

    A novel bombesin receptor antagonist (2258U89) potently inhibits bombesin evoked release of gastrointestinal hormones from rats and dogs, in vitro and in vivo

    Regul Pept

    (1992)
  • J Staley et al.

    [Des-Met14] bombesin analogues function as small cell lung cancer bombesin receptor antagonists

    Peptides

    (1991)
  • N Weigert et al.

    Effect of bombesin antagonist D-Phe6-BN(6–13)OMe on vagally induced gastrin release from perfused rat stomach

    Life Sci

    (1993)
  • G Varga et al.

    Effect of potent bombesin receptor antagonist on release of gut hormones in rats

    Regul Pept

    (1992)
  • G Varga et al.

    Effects of potent bombesin antagonist on exocrine pancreatic secretion in rats

    Peptides

    (1991)
  • DH Coy et al.

    Development of a potent bombesin receptor antagonist with prolonged in vivo inhibitory activity on bombesin-stimulated amylase and protein release in the rat

    Peptides

    (1992)
  • EE Ladenheim et al.

    Bombesin receptor antagonists differentiate receptor subtypes in rat brain

    Eur J Pharmacol

    (1993)
  • S Guard et al.

    Structure-activity requirements of bombesin for gastrin-releasing peptide- and neuromedin B-preferring bombesin receptors in rat brain

    Eur J Pharmacol

    (1993)
  • KG Bitar et al.

    Identification and initial characterization of a putative neuromedin B-type receptor from rat urinary bladder membranes

    Eur J Pharmacol

    (1992)
  • TP Davis et al.

    Metabolic stability and tumor inhibition of bombesin/GRP receptor antagonists

    Peptides

    (1992)
  • RI Feldman et al.

    Purification and characterization of the bombesin/gastrin releasing peptide receptor from Swiss 3T3 cells

    J Biol Chem

    (1990)
  • Y Taché et al.

    Gastrin releasing peptide (GRP): central nervous system (CNS) action to inhibit gastric secretion in rats

    Regul Pept

    (1980)
  • D.C. Heimbrook et al.

    Carboxyl-terminal modification of a gastrin releasing peptide derivative generates potent antagonists

    J Biol Chem

    (1989)
  • A Anastasi et al.

    Isolation and structure of bombesin and alytesin, two analogous active peptides from the skin of the European amphibian Bombina and Alytes

    Experientia

    (1971)
  • A Anastasi et al.

    Amino acid composition and sequence of litorin, a bombesin-like nonapeptide occurring in methanol extracts of the skin of the Australian leptodactylid frog Litoria aurea

    Experientia

    (1975)
  • T Nakajima et al.

    Isolation and structure of a new vasoactive polypeptide

  • T Yasuhara et al.

    Two new frog skin peptides, phyllolitorins, of the bombesin-ranatensin family Phyllomedusa sauvagei

    Biomed Res

    (1983)
  • TJ McDonald et al.

    Characterization of a gastrin releasing peptide from porcine non-antral gastric tissue

    FEBS Lett

    (1979)
  • R Minamino et al.

    Neuromedin B: a novel bombesin-like peptide identified in porcine spinal cord

    Biochem Biophys Res Commun

    (1983)
  • C Cardona et al.

    Production of neuromedin B and neuromedin B gene expression in human lung tumor cell lines

    Cancer Res

    (1991)
  • ER Spindel et al.

    Cloning and characterization of cDNAs encoding human gastrin-releasing peptides

  • IM Krane et al.

    Molecular cloning of cDNAs encoding the human bombesin-like peptide neuromedin B

    J Biol Chem

    (1988)
  • D Regoli et al.

    Receptors for neurokinins, tachykinins, and bombesin: a pharmacological study

    Ann NY Acad Sci

    (1988)
  • T von Schrenck et al.

    Neuromedin B receptor in esophagus: evidence for subtypes of bombesin receptor

    Am J Physiol

    (1989)
  • EE Ladenheim et al.

    Receptor heterogeneity for bombesin-like peptides in the rat central nervous system

    Brain Res

    (1990)
  • T von Schrenck et al.

    Potent bombesin receptor antagonists distinguish receptor subtypes

    Am J Physiol

    (1990)
  • MH Corjay et al.

    Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells

    J Biol Chem

    (1991)
  • C Cardona et al.

    Evidence for the existence of separate receptors for gastrin releasing peptide, neuromedin B and phyllolitorin in human tumour cell lines

    Br J Cancer

    (1991)
  • E Rozengurt

    Bombesin stimulation of mitogenesis. Specific receptors, signal transduction, and early events

    Am Rev Respir Dis

    (1990)
  • DM Cirillo et al.

    Receptor for bombesin with associated tyrosine kinase activity

    Mol Cell Biol

    (1986)
  • I Zachary et al.

    Bombesin, vasopressin, and endothelin rapidly stimulate tyrosine phosphorylation in intact Swiss 3T3 cells

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      Pretreatment with 7 μg of this antagonist did not influence the hypothermia with statistical significance. However, 2–30 μg of [d-Tyr6]BN(6–13)methylester (TBNME), one of the most selective and potent GRP-R antagonists [3,12], dose-dependently blocked the hypothermia (Fig. 2). In addition, the influence of BIM23127 (30 μg), an NMB-R antagonist [11,14], on the BN-induced effect was examined.

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    This paper was reviewed by Dr Robert T. Jensen, NIH/NIDDK/DDB, 10/9C103, 10 Center DR MSC 1804, Bethesda, MD20892-1804, USA and Jean Martinez, C.P.M.I.B., FacultC de Pharmacie, 15, avenue Charles Flahault, 34060 Montpellier Cedex 1, France.

    1

    Presently retired.

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