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MedKoo product information:

RC3095

MedKoo Code#: 202430

Name: RC3095

CAS#: 138147-78-1

 

Synonym:   RC3095; RC-3095; L-Leucinamide, (3R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-L-histidyl-L-leucyl-.psi.(CH2-NH)-; L-Histidinamide, N2-[(2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-3-yl)carbonyl]-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-N-[1-[[[1-(aminocarbonyl)-3-methylbutyl]amino]methyl]-3-methylbutyl]-, [1(R),6[S-(R*,R*)]]-; 1H-Pyrido[3,4-b]indole;  (D-Tpi6, Leu13 Ψ(CH2-NH)-Leu14)bombesin (6-14), (3R)-2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole-3-carbonyl-L-glutaminyl-L-tryptophyl-L-alanyl-L-valylglycyl-L-histidyl-L-leucyl-Ψ(CH2-NH)-L-Leucinamide trifluoroacetate salt.

 

Amino acid sequences: (D-TPI6, LEU13 y(CH2-NH)-LEU14)BOMBESIN (6-14).

 

IUPAC/Chemical name: 

(S)-N1-((2S,5S,8S,14S,17S,20S)-14-((1H-imidazol-5-yl)methyl)-20-carbamoyl-1-(1H-indol-3-yl)-17-isobutyl-8-isopropyl-5,22-dimethyl-3,6,9,12,15-pentaoxo-4,7,10,13,16,19-hexaazatricosan-2-yl)-2-((R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxamido)pentanediamide

Chemical structure: Theoretical analysis

 

  

 

Chemical Formula: C56H79N15O9

Exact Mass: 1105.61852

Molecular Weight: 1106.32

 

m/z: 1105.61852 (100.0%), 1106.62187 (60.6%), 1107.62523 (18.0%), 1106.61555 (5.5%), 1108.62858 (3.5%), 1107.61891 (3.4%), 1107.62276 (1.8%), 1108.62612 (1.1%).

 

 Elemental Analysis: C, 60.80; H, 7.20; N, 18.99; O, 13.02

 

 

Availability and price:

This agent is not in stock, which may be available through custom synthesis. To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

 

Quality control data:

Product will be shipped with supporting analytical data.

 

 

Information about this agent

RC-3095 is a potent BB2 (GRP-preferring) bombesin receptor antagonist.

 

Current developer:   AEterna Zentaris Inc

 

References

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2: Cassol OJ Jr, Rezin GT, Petronilho FC, Scaini G, Gonçalves CL, Ferreira GK, Roesler R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effects of N-acetylcysteine/deferoxamine, taurine and RC-3095 on respiratory chain complexes and creatine kinase activities in rat brain after sepsis. Neurochem Res. 2010 Apr;35(4):515-21. PubMed PMID: 20238483.

3: Valvassori SS, Moretti M, Kauer-Sant'Anna M, Roesler R, Petronilho F, Schwartsmann G, Kapczinski F, Dal-Pizzol F, Quevedo J. Effects of a gastrin-releasing peptide receptor antagonist on D-amphetamine-induced oxidative stress in the rat brain. J Neural Transm. 2010 Mar;117(3):309-16. Epub 2010 Feb 4. PubMed PMID: 20131069.

4: Sotomayor S, Muńoz-Moreno L, Carmena MJ, Schally AV, Sánchez-Chapado M, Prieto JC, Bajo AM. Regulation of HER expression and transactivation in human prostate cancer cells by a targeted cytotoxic bombesin analog (AN-215) and a bombesin antagonist (RC-3095). Int J Cancer. 2010 Jan 22. [Epub ahead of print] PubMed PMID: 20099275.

5: Cassol OJ Jr, Rezin GT, Petronilho FC, Scaini G, Gonçalves CL, Ferreira GK, Roesler R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effects of N-Acetylcysteine/Deferoxamine, Taurine and RC-3095 on Respiratory Chain Complexes and Creatine Kinase Activities in Rat Brain After Sepsis. Neurochem Res. 2009 Nov 13. [Epub ahead of print] PubMed PMID: 19911272.

6: Damin DC, Santos FS, Heck R, Rosito MA, Meurer L, Kliemann LM, Roesler R, Schwartsmann G. Effects of the Gastrin-Releasing Peptide Antagonist RC-3095 in a Rat Model of Ulcerative Colitis. Dig Dis Sci. 2009 Nov 6. [Epub ahead of print] PubMed PMID: 19894117.

7: Schmidt AL, de Farias CB, Abujamra AL, Kapczinski F, Schwartsmann G, Brunetto AL, Roesler R. BDNF and PDE4, but not the GRPR, regulate viability of human medulloblastoma cells. J Mol Neurosci. 2010 Mar;40(3):303-10. Epub 2009 Jul 30. PubMed PMID: 19642024.

8: de Farias CB, Stertz L, Lima RC, Kapczinski F, Schwartsmann G, Roesler R. Reduced NGF secretion by HT-29 human colon cancer cells treated with a GRPR antagonist. Protein Pept Lett. 2009;16(6):650-2. PubMed PMID: 19519524.

9: Pereira DV, Steckert AV, Mina F, Petronilho F, Roesler R, Schwartsmann G, Ritter C, Dal-Pizzol F. Effects of an antagonist of the gastrin-releasing peptide receptor in an animal model of uveitis. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5300-3. Epub 2009 Jun 10. PubMed PMID: 19516017.

10: Petronilho F, Araújo JH, Steckert AV, Rezin GT, Ferreira GK, Roesler R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effect of a gastrin-releasing peptide receptor antagonist and a proton pump inhibitor association in an animal model of gastritis. Peptides. 2009 Aug;30(8):1460-5. Epub 2009 Jun 6. PubMed PMID: 19505518.

11: González N, Mantey SA, Pradhan TK, Sancho V, Moody TW, Coy DH, Jensen RT. Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors. Peptides. 2009 Aug;30(8):1473-86. Epub 2009 May 20. PubMed PMID: 19463875; PubMed Central PMCID: PMC2766550.

12: Abujamra AL, Almeida VR, Brunetto AL, Schwartsmann G, Roesler R. A gastrin-releasing peptide receptor antagonist stimulates Neuro2a neuroblastoma cell growth: prevention by a histone deacetylase inhibitor. Cell Biol Int. 2009 Aug;33(8):899-903. Epub 2009 May 6. PubMed PMID: 19426821.

13: de Oliveira MS, Cechim G, Braganhol E, Santos DG, Meurer L, de Castro CG Jr, Brunetto AL, Schwartsmann G, Battastini AM, Lenz G, Roesler R. Anti-proliferative effect of the gastrin-release peptide receptor antagonist RC-3095 plus temozolomide in experimental glioblastoma models. J Neurooncol. 2009 Jun;93(2):191-201. Epub 2009 Jan 8. Erratum in: J Neurooncol. 2009 Jun;93(2):203. Schwarstmann, Gilberto [corrected to Schwartsmann, Gilberto]. PubMed PMID: 19129973.

14: Damin DC, Santos FS, Heck R, Schwartsmann G. Gastrin-releasing peptide receptor: a potential target in treatment of IBD? J Clin Gastroenterol. 2009 Mar;43(3):288. PubMed PMID: 18838920.

15: Oliveira PG, Brenol CV, Edelweiss MI, Brenol JC, Petronilho F, Roesler R, Dal-Pizzol F, Schwartsmann G, Xavier RM. Effects of an antagonist of the bombesin/gastrin-releasing peptide receptor on complete Freund's adjuvant-induced arthritis in rats. Peptides. 2008 Oct;29(10):1726-31. Epub 2008 Jun 12. PubMed PMID: 18590783.

16: Mountney C, Anisman H, Merali Z. Effects of gastrin-releasing peptide agonist and antagonist administered to the basolateral nucleus of the amygdala on conditioned fear in the rat. Psychopharmacology (Berl). 2008 Sep;200(1):51-8. Epub 2008 Jun 18. PubMed PMID: 18563394.

17: Sakamoto H, Matsuda K, Zuloaga DG, Hongu H, Wada E, Wada K, Jordan CL, Breedlove SM, Kawata M. Sexually dimorphic gastrin releasing peptide system in the spinal cord controls male reproductive functions. Nat Neurosci. 2008 Jun;11(6):634-6. Epub 2008 May 18. PubMed PMID: 18488022.

18: Flores DG, de Farias CB, Leites J, de Oliveira MS, Lima RC, Tamajusuku AS, Di Leone LP, Meurer L, Brunetto AL, Schwartsmann G, Lenz G, Roesler R. Gastrin-releasing peptide receptors regulate proliferation of C6 Glioma cells through a phosphatidylinositol 3-kinase-dependent mechanism. Curr Neurovasc Res. 2008 May;5(2):99-105. PubMed PMID: 18473825.

19: Luft T, Amaral OB, Schwartsmann G, Roesler R. Transient disruption of fear-related memory by post-retrieval inactivation of gastrin-releasing peptide or N-methyl-D-aspartate receptors in the hippocampus. Curr Neurovasc Res. 2008 Feb;5(1):21-7. PubMed PMID: 18289018.

20: Cornelio DB, Dal-Pizzol F, Roesler R, Schwartsmann G. Targeting the bombesin/gastrin-releasing peptide receptor to treat sepsis. Recent Pat Antiinfect Drug Discov. 2007 Nov;2(3):178-81. Review. PubMed PMID: 18221174.

21: Petronilho F, Roesler R, Schwartsmann G, Dal Pizzol F. Gastrin-releasing peptide receptor as a molecular target for inflammatory diseases. Inflamm Allergy Drug Targets. 2007 Dec;6(4):197-200. Review. PubMed PMID: 18220954.

22: Kauer-Sant'Anna M, Andreazza AC, Valvassori SS, Martins MR, Barbosa LM, Schwartsmann G, Roesler R, Quevedo J, Kapczinski F. A gastrin-releasing peptide receptor antagonist blocks D-amphetamine-induced hyperlocomotion and increases hippocampal NGF and BDNF levels in rats. Peptides. 2007 Jul;28(7):1447-52. Epub 2007 Jun 16. PubMed PMID: 17629354.

23: Preissler T, Luft T, Kapczinski F, Quevedo J, Schwartsmann G, Roesler R. Basic fibroblast growth factor prevents the memory impairment induced by gastrin-releasing peptide receptor antagonism in area CA1 of the rat hippocampus. Neurochem Res. 2007 Aug;32(8):1381-6. Epub 2007 Apr 4. PubMed PMID: 17406984.

24: Kang J, Ishola TA, Baregamian N, Mourot JM, Rychahou PG, Evers BM, Chung DH. Bombesin induces angiogenesis and neuroblastoma growth. Cancer Lett. 2007 Aug 18;253(2):273-81. Epub 2007 Mar 26. PubMed PMID: 17383815; PubMed Central PMCID: PMC2709810.

25: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Jan-Feb;29(1):53-71. PubMed PMID: 17344945.

26: Presti-Torres J, de Lima MN, Scalco FS, Caldana F, Garcia VA, Guimarăes MR, Schwartsmann G, Roesler R, Schröder N. Impairments of social behavior and memory after neonatal gastrin-releasing peptide receptor blockade in rats: Implications for an animal model of neurodevelopmental disorders. Neuropharmacology. 2007 Mar;52(3):724-32. Epub 2006 Nov 13. PubMed PMID: 17097693.

27: Luft T, Flores DG, Vianna MR, Schwartsmann G, Roesler R, Izquierdo I. A role for hippocampal gastrin-releasing peptide receptors in extinction of aversive memory. Neuroreport. 2006 Jun 26;17(9):935-9. PubMed PMID: 16738491.

28: Dantas Ados S, Luft T, Henriques JA, Schwartsmann G, Roesler R. Opposite effects of low and high doses of the gastrin-releasing peptide receptor antagonist RC-3095 on memory consolidation in the hippocampus: possible involvement of the GABAergic system. Peptides. 2006 Sep;27(9):2307-12. Epub 2006 May 2. PubMed PMID: 16650508.

29: Schwartsmann G, DiLeone LP, Horowitz M, Schunemann D, Cancella A, Pereira AS, Richter M, Souza F, da Rocha AB, Souza FH, Pohlmann P, De Nucci G. A phase I trial of the bombesin/gastrin-releasing peptide (BN/GRP) antagonist RC3095 in patients with advanced solid malignancies. Invest New Drugs. 2006 Sep;24(5):403-12. PubMed PMID: 16505950.

30: Dal-Pizzol F, Di Leone LP, Ritter C, Martins MR, Reinke A, Pens Gelain D, Zanotto-Filho A, de Souza LF, Andrades M, Barbeiro DF, Bernard EA, Cammarota M, Bevilaqua LR, Soriano FG, Cláudio J, Moreira F, Roesler R, Schwartsmann G. Gastrin-releasing peptide receptor antagonist effects on an animal model of sepsis. Am J Respir Crit Care Med. 2006 Jan 1;173(1):84-90. Epub 2005 Sep 28. PubMed PMID: 16192447.

31: Martins MR, Reinke A, Valvassori SS, Machado RA, Quevedo J, Schwartsmann G, Roesler R. Non-associative learning and anxiety in rats treated with a single systemic administration of the gastrin-releasing peptide receptor antagonist RC-3095. Peptides. 2005 Dec;26(12):2525-9. Epub 2005 Jul 14. PubMed PMID: 16023260.

32: Stangelberger A, Schally AV, Letsch M, Szepeshazi K, Nagy A, Halmos G, Kanashiro CA, Corey E, Vessella R. Targeted chemotherapy with cytotoxic bombesin analogue AN-215 inhibits growth of experimental human prostate cancers. Int J Cancer. 2006 Jan 1;118(1):222-9. PubMed PMID: 16003723.

33: Schwartsmann G, Di Leone LP, Dal Pizzol F, Roesler R. MAPK pathway activation in colorectal cancer: a therapeutic opportunity for GRP receptor antagonists. Lancet Oncol. 2005 Jul;6(7):444-5. PubMed PMID: 15992692.

34: Heuser M, Schlott T, Schally AV, Kahler E, Schliephake R, Laabs SO, Hemmerlein B. Expression of gastrin releasing Peptide receptor in renal cell carcinomas: a potential function for the regulation of neoangiogenesis and microvascular perfusion. J Urol. 2005 Jun;173(6):2154-9. PubMed PMID: 15879878.

35: Venturella R, Lessa D, Luft T, Roozendaal B, Schwartsmann G, Roesler R. Dexamethasone reverses the memory impairment induced by antagonism of hippocampal gastrin-releasing peptide receptors. Peptides. 2005 May;26(5):821-5. Epub 2005 Jan 18. PubMed PMID: 15808912.

36: Engel JB, Keller G, Schally AV, Halmos G, Hammann B, Nagy A. Effective inhibition of experimental human ovarian cancers with a targeted cytotoxic bombesin analogue AN-215. Clin Cancer Res. 2005 Mar 15;11(6):2408-15. PubMed PMID: 15788692.

37: Pereira AS, DiLeone L, Souza FH, Lilla S, Richter M, Schwartsmann G, De Nucci G. Quantification of the bombesin/gastrin releasing peptide antagonist RC-3095 by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Feb 25;816(1-2):321-6. PubMed PMID: 15664365.

38: Meller CA, Henriques JA, Schwartsmann G, Roesler R. The bombesin/gastrin releasing peptide receptor antagonist RC-3095 blocks apomorphine but not MK-801-induced stereotypy in mice. Peptides. 2004 Apr;25(4):585-8. PubMed PMID: 15165713.

39: Roesler R, Lessa D, Venturella R, Vianna MR, Luft T, Henriques JA, Izquierdo I, Schwartsmann G. Bombesin/gastrin-releasing peptide receptors in the basolateral amygdala regulate memory consolidation. Eur J Neurosci. 2004 Feb;19(4):1041-5. PubMed PMID: 15009151.

40: Roesler R, Kopschina MI, Rosa RM, Henriques JA, Souza DO, Schwartsmann G. RC-3095, a bombesin/gastrin-releasing peptide receptor antagonist, impairs aversive but not recognition memory in rats. Eur J Pharmacol. 2004 Feb 13;486(1):35-41. PubMed PMID: 14751406.

41: Bajo AM, Schally AV, Groot K, Szepeshazi K. Bombesin antagonists inhibit proangiogenic factors in human experimental breast cancers. Br J Cancer. 2004 Jan 12;90(1):245-52. PubMed PMID: 14710236; PubMed Central PMCID: PMC2395331.

42: Heuser M, Gralla O, Nustede R, Post S. [Significance of regulatory peptide GRP for microcirculation of the small intestine after ischemia/reperfusion]. Langenbecks Arch Chir Suppl Kongressbd. 1998;115(Suppl I):105-7. German. PubMed PMID: 14518222.

43: Roesler R, Meller CA, Kopschina MI, Souza DO, Henriques JA, Schwartsmann G. Intrahippocampal infusion of the bombesin/gastrin-releasing peptide antagonist RC-3095 impairs inhibitory avoidance retention. Peptides. 2003 Jul;24(7):1069-74. PubMed PMID: 14499286.

44: Bajo AM, Schally AV, Krupa M, Hebert F, Groot K, Szepeshazi K. Bombesin antagonists inhibit growth of MDA-MB-435 estrogen-independent breast cancers and decrease the expression of the ErbB-2/HER-2 oncoprotein and c-jun and c-fos oncogenes. Proc Natl Acad Sci U S A. 2002 Mar 19;99(6):3836-41. Epub 2002 Mar 12. PubMed PMID: 11891317; PubMed Central PMCID: PMC122610.

45: Chatzistamou I, Schally AV, Szepeshazi K, Groot K, Hebert F, Arencibia JM. Inhibition of growth of ES-2 human ovarian cancers by bombesin antagonist RC-3095, and luteinizing hormone-releasing hormone antagonist Cetrorelix. Cancer Lett. 2001 Sep 28;171(1):37-45. PubMed PMID: 11485826.

46: Chatzistamou I, Schally AV, Sun B, Armatis P, Szepeshazi K. Inhibition of growth of OV-1063 human epithelial ovarian cancers and c- jun and c- fos oncogene expression by bombesin antagonists. Br J Cancer. 2000 Oct;83(7):906-13. PubMed PMID: 10970693; PubMed Central PMCID: PMC2374679.

47: Heuser M, Pfaar O, Gralla O, Gröne HJ, Nustede R, Post S. Impact of gastrin-releasing peptide on intestinal microcirculation after ischemia-reperfusion in rats. Digestion. 2000;61(3):172-80. PubMed PMID: 10773722.

48: Kahán Z, Sun B, Schally AV, Arencibia JM, Cai RZ, Groot K, Halmos G. Inhibition of growth of MDA-MB-468 estrogen-independent human breast carcinoma by bombesin/gastrin-releasing peptide antagonists RC-3095 and RC-3940-II. Cancer. 2000 Mar 15;88(6):1384-92. PubMed PMID: 10717621.

49: Kiaris H, Schally AV, Sun B, Armatis P, Groot K. Inhibition of growth of human malignant glioblastoma in nude mice by antagonists of bombesin/gastrin-releasing peptide. Oncogene. 1999 Nov 25;18(50):7168-73. PubMed PMID: 10597318.

50: Szepesházi K, Halmos G, Schally AV, Arencibia JM, Groot K, Vadillo-Buenfil M, Rodriguez-Martin E. Growth inhibition of experimental pancreatic cancers and sustained reduction in epidermal growth factor receptors during therapy with hormonal peptide analogs. J Cancer Res Clin Oncol. 1999 Aug-Sep;125(8-9):444-52. PubMed PMID: 10480336.

51: Alvaro-Alonso I, Muńoz-Acedo G, Rodríguez-Martín E, Schally AV, Arilla E. Bombesin induces a reduction of somatostatin inhibition of adenylyl cyclase activity, Gi function, and somatostatin receptors in rat exocrine pancreas. Peptides. 1999;20(6):723-30. PubMed PMID: 10477127.

52: Koppán M, Halmos G, Arencibia JM, Lamharzi N, Schally AV. Bombesin/gastrin-releasing peptide antagonists RC-3095 and RC-3940-II inhibit tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma. Cancer. 1998 Oct 1;83(7):1335-43. PubMed PMID: 9762934.

53: Miyazaki M, Lamharzi N, Schally AV, Halmos G, Szepeshazi K, Groot K, Cai RZ. Inhibition of growth of MDA-MB-231 human breast cancer xenografts in nude mice by bombesin/gastrin-releasing peptide (GRP) antagonists RC-3940-II and RC-3095. Eur J Cancer. 1998 Apr;34(5):710-7. PubMed PMID: 9713279.

54: Szepeshazi K, Schally AV, Halmos G, Lamharzi N, Groot K, Horvath JE. A single in vivo administration of bombesin antagonist RC-3095 reduces the levels and mRNA expression of epidermal growth factor receptors in MXT mouse mammary cancers. Proc Natl Acad Sci U S A. 1997 Sep 30;94(20):10913-8. PubMed PMID: 9380734; PubMed Central PMCID: PMC23529.

55: Halmos G, Schally AV. Reduction in receptors for bombesin and epidermal growth factor in xenografts of human small-cell lung cancer after treatment with bombesin antagonist RC-3095. Proc Natl Acad Sci U S A. 1997 Feb 4;94(3):956-60. PubMed PMID: 9023364; PubMed Central PMCID: PMC19621.

56: Konety BR, Getzenberg RH. Novel therapies for advanced prostate cancer. Semin Urol Oncol. 1997 Feb;15(1):33-42. Review. PubMed PMID: 9050138.

57: Wang QJ, Knezetic JA, Schally AV, Pour PM, Adrian TE. Bombesin may stimulate proliferation of human pancreatic cancer cells through an autocrine pathway. Int J Cancer. 1996 Nov 15;68(4):528-34. PubMed PMID: 8945626.

58: Kozacko MF, Mang TS, Schally AV, Priore RL, Liebow C. Bombesin antagonist prevents CO2 laser-induced promotion of oral cancer. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2953-7. PubMed PMID: 8610149; PubMed Central PMCID: PMC39741.

59: Qin Y, Ertl T, Cai RZ, Horvŕth JE, Groot K, Schally AV. Antagonists of bombesin/gastrin-releasing peptide inhibit growth of SW-1990 human pancreatic adenocarcinoma and production of cyclic AMP. Int J Cancer. 1995 Oct 9;63(2):257-62. PubMed PMID: 7591214.

60: Groot K, Horvŕth JE, Cai RZ, Schally AV. Development of a radioimmunoassay for a pseudononapeptide bombesin/GRP antagonist with antitumor activity. Int J Pept Protein Res. 1995 Jun;45(6):561-6. PubMed PMID: 7558587.

61: Pinski J, Schally AV, Halmos G, Szepeshazi K, Groot K. Somatostatin analogues and bombesin/gastrin-releasing peptide antagonist RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. Cancer Res. 1994 Nov 15;54(22):5895-901. PubMed PMID: 7954420.

62: Pinski J, Schally AV, Halmos G, Szepeshazi K, Groot K, O'Byrne K, Cai RZ. Effects of somatostatin analogue RC-160 and bombesin/gastrin-releasing peptide antagonists on the growth of human small-cell and non-small-cell lung carcinomas in nude mice. Br J Cancer. 1994 Nov;70(5):886-92. PubMed PMID: 7947094; PubMed Central PMCID: PMC2033546.

63: Szepshazi K, Halmos G, Groot K, Schally AV. Combination treatment of nitrosamine-induced pancreatic cancers in hamsters with analogs of LH-RH and a bombesin/GRP antagonist. Int J Pancreatol. 1994 Oct-Dec;16(2-3):141-9. PubMed PMID: 7868940.

64: Halmos G, Pinski J, Szoke B, Schally AV. Characterization of bombesin/gastrin-releasing peptide receptors in membranes of MKN45 human gastric cancer. Cancer Lett. 1994 Sep 30;85(1):111-8. PubMed PMID: 7923093.

65: Reile H, Armatis PE, Schally AV. Characterization of high-affinity receptors for bombesin/gastrin releasing peptide on the human prostate cancer cell lines PC-3 and DU-145: internalization of receptor bound 125I-(Tyr4) bombesin by tumor cells. Prostate. 1994 Jul;25(1):29-38. PubMed PMID: 8022709.

66: Pinski J, Halmos G, Yano T, Szepeshazi K, Qin Y, Ertl T, Schally AV. Inhibition of growth of MKN45 human gastric-carcinoma xenografts in nude mice by treatment with bombesin/gastrin-releasing-peptide antagonist (RC-3095) and somatostatin analogue RC-160. Int J Cancer. 1994 May 15;57(4):574-80. PubMed PMID: 7910153.

67: Liebow C, Crean DH, Lee MT, Kamer AR, Mang TS, Schally AV. Synergistic effects of bombesin and epidermal growth factor on cancers. Proc Natl Acad Sci U S A. 1994 Apr 26;91(9):3804-8. PubMed PMID: 8170991; PubMed Central PMCID: PMC43670.

68: Qin Y, Ertl T, Cai RZ, Halmos G, Schally AV. Inhibitory effect of bombesin receptor antagonist RC-3095 on the growth of human pancreatic cancer cells in vivo and in vitro. Cancer Res. 1994 Feb 15;54(4):1035-41. PubMed PMID: 8313359.

69: Yano T, Pinski J, Szepeshazi K, Halmos G, Radulovic S, Groot K, Schally AV. Inhibitory effect of bombesin/gastrin-releasing peptide antagonist RC-3095 and luteinizing hormone-releasing hormone antagonist SB-75 on the growth of MCF-7 MIII human breast cancer xenografts in athymic nude mice. Cancer. 1994 Feb 15;73(4):1229-38. PubMed PMID: 8313327.

70: Qin Y, Halmos G, Cai RZ, Szoke B, Ertl T, Schally AV. Bombesin antagonists inhibit in vitro and in vivo growth of human gastric cancer and binding of bombesin to its receptors. J Cancer Res Clin Oncol. 1994;120(9):519-28. PubMed PMID: 8045917.

71: Radulovic S, Schally AV, Reile H, Halmos G, Szepeshazi K, Groot K, Milovanovic S, Miller G, Yano T. Inhibitory effects of antagonists of bombesin/gastrin releasing peptide (GRP) and somatostatin analog (RC-160) on growth of HT-29 human colon cancers in nude mice. Acta Oncol. 1994;33(6):693-701. PubMed PMID: 7946450.

72: Pinski J, Reile H, Halmos G, Groot K, Schally AV. Inhibitory effects of somatostatin analogue RC-160 and bombesin/gastrin-releasing peptide antagonist RC-3095 on the growth of the androgen-independent Dunning R-3327-AT-1 rat prostate cancer. Cancer Res. 1994 Jan 1;54(1):169-74. PubMed PMID: 7903203.

73: Shirahige Y, Cai RZ, Szepeshazi K, Halmos G, Pinski J, Groot K, Schally AV. Inhibitory effect of bombesin/gastrin-releasing peptide (GRP) antagonists RC-3950-II and RC-3095 on MCF-7 MIII human breast cancer xenografts in nude mice. Biomed Pharmacother. 1994;48(10):465-72. PubMed PMID: 7858155.

74: Pinski J, Schally AV, Halmos G, Szepeshazi K. Effect of somatostatin analog RC-160 and bombesin/gastrin releasing peptide antagonist RC-3095 on growth of PC-3 human prostate-cancer xenografts in nude mice. Int J Cancer. 1993 Dec 2;55(6):963-7. PubMed PMID: 7902829.

75: Pinski J, Halmos G, Szepeshazi K, Schally AV. Antagonists of bombesin/gastrin-releasing peptides as adjuncts to agonists of luteinizing hormone-releasing hormone in the treatment of experimental prostate cancer. Cancer. 1993 Dec 1;72(11):3263-70. PubMed PMID: 8242552.

76: Crean DH, Liebow C, Penetrante RB, Mang TS. Evaluation of porfimer sodium fluorescence for measuring tissue transformation. Cancer. 1993 Nov 15;72(10):3068-77. PubMed PMID: 8106141.

77: Pinski J, Halmos G, Schally AV. Somatostatin analog RC-160 and bombesin/gastrin-releasing peptide antagonist RC-3095 inhibit the growth of androgen-independent DU-145 human prostate cancer line in nude mice. Cancer Lett. 1993 Jul 30;71(1-3):189-96. PubMed PMID: 8103419.

78: Szepeshazi K, Schally AV, Groot K, Halmos G. Effect of bombesin, gastrin-releasing peptide (GRP)(14-27) and bombesin/GRP receptor antagonist RC-3095 on growth of nitrosamine-induced pancreatic cancers in hamsters. Int J Cancer. 1993 May 8;54(2):282-9. PubMed PMID: 8387464.

79: Konturek SJ, Tasler J, Bilski J, Cieszkowski M, Cai RZ, Schally AV. Antagonism of receptors for gastrin, cholecystokinin and GRP/bombesin in postprandial stimulation of exocrine pancreas in dogs. J Physiol Pharmacol. 1993 Mar;44(1):43-53. PubMed PMID: 8390873.

80: Liebow C, Crean DH, Schally AV, Mang TS. Peptide analogues alter the progression of premalignant lesions, as measured by Photofrin fluorescence. Proc Natl Acad Sci U S A. 1993 Mar 1;90(5):1897-901. PubMed PMID: 8095335; PubMed Central PMCID: PMC45987.

81: Radulovic S, Comaru-Schally AM, Milovanovic S, Schally AV. Somatostatin analogue RC-160 and LH-RH antagonist SB-75 inhibit growth of MIA PaCa-2 human pancreatic cancer xenografts in nude mice. Pancreas. 1993 Jan;8(1):88-97. PubMed PMID: 8093555.

82: Szepeshazi K, Schally AV, Halmos G, Groot K, Radulovic S. Growth inhibition of estrogen-dependent and estrogen-independent MXT mammary cancers in mice by the bombesin and gastrin-releasing peptide antagonist RC-3095. J Natl Cancer Inst. 1992 Dec 16;84(24):1915-22. PubMed PMID: 1460673.

83: Pinski J, Yano T, Schally AV. Inhibitory effects of the new bombesin receptor antagonist RC-3095 on the luteinizing hormone release in rats. Neuroendocrinology. 1992 Dec;56(6):831-7. PubMed PMID: 1369591.

84: Pinski J, Yano T, Rekasi Z, Cai RZ, Radulovic S, Schally AV. High potency of a new bombesin antagonist (RC-3095) in inhibiting serum gastrin levels; comparison of different routes of administration. Regul Pept. 1992 Oct 13;41(3):185-93. PubMed PMID: 1438988.

85: Pinski J, Yano T, Groot K, Cai RZ, Radulovic S, Schally AV. Endocrine effects of new bombesin/gastrin-releasing peptide antagonists in rats. Am J Physiol. 1992 Oct;263(4 Pt 1):E712-7. PubMed PMID: 1415689.

86: Yano T, Pinski J, Groot K, Schally AV. Stimulation by bombesin and inhibition by bombesin/gastrin-releasing peptide antagonist RC-3095 of growth of human breast cancer cell lines. Cancer Res. 1992 Aug 15;52(16):4545-7. PubMed PMID: 1643647.

87: Jaworek J, Konturek PK, Konturek SJ, Cai RZ, Schally AV. Actions of novel bombesin receptor antagonists on pancreatic secretion in rats. Eur J Pharmacol. 1992 Apr 22;214(2-3):239-45. PubMed PMID: 1381317.

88: Milovanovic SR, Radulovic S, Groot K, Schally AV. Inhibition of growth of PC-82 human prostate cancer line xenografts in nude mice by bombesin antagonist RC-3095 or combination of agonist [D-Trp6]-luteinizing hormone-releasing hormone and somatostatin analog RC-160. Prostate. 1992;20(4):269-80. PubMed PMID: 1376910.

89: Radulovic S, Cai RZ, Serfozo P, Groot K, Redding TW, Pinski J, Schally AV. Biological effects and receptor binding affinities of new pseudononapeptide bombesin/GRP receptor antagonists with N-terminal D-Trp or D-Tpi. Int J Pept Protein Res. 1991 Dec;38(6):593-600. PubMed PMID: 1726427.

90: Radulovic S, Miller G, Schally AV. Inhibition of growth of HT-29 human colon cancer xenografts in nude mice by treatment with bombesin/gastrin releasing peptide antagonist (RC-3095). Cancer Res. 1991 Nov 1;51(21):6006-9. PubMed PMID: 1682040.

91: Szepeshazi K, Schally AV, Cai RZ, Radulovic S, Milovanovic S, Szoke B. Inhibitory effect of bombesin/gastrin-releasing peptide antagonist RC-3095 and high dose of somatostatin analogue RC-160 on nitrosamine-induced pancreatic cancers in hamsters. Cancer Res. 1991 Nov 1;51(21):5980-6. PubMed PMID: 1682039.

92: Dembiński A, Warzecha Z, Konturek SJ, Banas M, Cai RZ, Schally AV. The effect of antagonist of receptors for gastrin, cholecystokinin and bombesin on growth of gastroduodenal mucosa and pancreas. J Physiol Pharmacol. 1991 Sep;42(3):263-77. PubMed PMID: 1665365.

93: Dembiński A, Warzecha Z, Konturek SJ, Cai RZ, Schally AV. The effects of antagonists of receptors for gastrin, cholecystokinin and bombesin on growth of gastroduodenal mucosa and pancreas. J Physiol Pharmacol. 1991 Jun;42(2):195-209. PubMed PMID: 1664265.

94: Konturek SJ, Dembinski A, Warzecha Z, Jaworek J, Konturek PK, Cai RZ, Schally AV. Antagonism of receptors for bombesin, gastrin and cholecystokinin in pancreatic secretion and growth. Digestion. 1991;48(2):89-97. PubMed PMID: 1714408.

 

 

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