Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 receptor antagonist ELN441958

Journal of Pharmacology and Experimental Therapeutics

Volumn 322, Issue 2, 2007, Pages 619-630

  Hawkinson, Jon E ^a   Szoke, Balazs G ^a   Garofalo, Albert W ^a   Hom, Dennis S ^a   Zhang, Hongbing ^a   Dreyer, Mark ^a   Fukuda, Juri Y ^a   Chen, Linda ^a   Samant, Bhushan ^a   Simmonds, Stellanie ^a,d   Zeitz, Karla P ^a   Wadsworth, Angie ^a   Liao, Anna ^a   Chavez, Raymond A ^a,e   Zmolek, Wes ^a   Ruslim, Lany ^a   Bova, Michael P ^a   Holcomb, Ryan ^a,f   Butelman, Eduardo R ^b   Ko, Mei Chuan ^c   Malmberg, Annika B ^a,g   more..

^a ELAN PHARMACEUTICALS   (United States)

^b ROCKEFELLER UNIVERSITY   (United States)

^c UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

^d PFIZER INC   (United States)

^e Avigen Inc   (United States)

^f Myriad Genetic Laboratories   (United States)

^g AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

7 CHLORO 2 [3 (9 PYRIDIN 4 YL 3,9 DIAZASPIRO[5.5]UNDECANECARBONYL)PHENYL] 2,3 DIHYDRO ISOINDOL 1 ONE; ANALGESIC AGENT; BENZAMIDE B1 RECEPTOR ANTAGONIST; BRADYKININ B1 RECEPTOR; BRADYKININ B2 RECEPTOR; CALCIUM; CARRAGEENAN; DESARGININE KALLIDIN; ELN 441958; ICATIBANT; KALLIDIN; NALTREXONE; NAPROXEN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CALCIUM MOBILIZATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG RECEPTOR BINDING; DRUG STABILITY; FEMALE; FIBROBLAST; HUMAN; HUMAN CELL; HYPERALGESIA; KNOCKOUT MOUSE; MALE; MOUSE; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIMATE; PRIORITY JOURNAL; RAT; RHESUS MONKEY; RODENT; SPRAGUE DAWLEY RAT;

ANALGESICS; ANIMALS; BRADYKININ; CALCIUM; CARRAGEENAN; CELL LINE; CELL MEMBRANE PERMEABILITY; FIBROBLASTS; HUMANS; HYPERALGESIA; KALLIDIN; MACACA MULATTA; MICE; MICE, KNOCKOUT; MICROSOMES, LIVER; MOLECULAR STRUCTURE; NALTREXONE; NAPROXEN; P-GLYCOPROTEIN; RATS; RECEPTOR, BRADYKININ B1; RECEPTORS, OPIOID; SPECIES SPECIFICITY; SPIRO COMPOUNDS; TRANSFECTION;

EID: 34547112030     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.107.120352     Document Type: Article

References (43)

1. Bowen CA, Fischer BD, Mello NY, and Negus SS (2002) Antagonism of the antinociceptive and discriminative stimulus effects of heroin and morphine by 3-methoxynaltrexone and naltrexone in rhesus monkeys. J Pharmacol Exp Ther 302:264-273.
2. Butelman ER, Ball JW, Harris TJ, and Kreek MJ (2003) Topical capsaicin-induced hyperalgesia in unanesthetized primates: pharmacological modulation. J Pharmacol Exp Ther 306:1106-1114.
3. 1 receptors in rats. Br J Pharmacol 135:1107-1114.
4. 1 receptor antagonist. Eur J Pharmacol 527:44-51.
5. Demeule M, Regina A, Jodoin J, Laplante A, Dagenais C, Berthelet F, Moghrabi A, and Beliveau R (2002) Drug transport to the brain: key roles for the efflux pump P-glycoprotein in the blood-brain barrier. Vascul Pharmacol 38:339-348.
6. Eisenbarth H, Rukwied R, Petersen M, and Schmelz M (2004) Sensitization to bradykinin B1 and B2 receptor activation in UV-B irradiated human skin. Pain 110:197-204.
7. 1 receptors induces chemotaxis of human neutrophils. J Leukoc Biol 80:117-124.
8. Emmerson PL, Liu MR, Woods JH, and Medzihradsky F (1994) Binding affinity and selectivity of opioids at mu, delta and kappa receptors in monkey brain membranes. J Pharmacol Exp Ther 271:1630-1637.
9. Evans CA, Jolivette LJ, Nagilla R, and Ward KW (2006) Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics. Drug Metab Dispos 34:1255-1265.
10. 2 receptor knockout mice and selective antagonists to characterize the nociceptive responses caused by kinins at the spinal level. Neuropharmacology 43:1188-1197.
11. 2 receptor knockout mice. Neuropharmacology 41:1006-1012.
12. 1 receptor. Br J Pharmacol 144:889-899.
13. 1 bradykinin receptors in inflammatory mechanical hyperalgesia. Pain 104:683-691.
14. 1 receptor: biochemical and pharmacological characterization. J Pharmacol Exp Ther 309:661-669.
15. Grant FS, Bartulis S, Brogley L, Dappen MS, Kasar R, Holcomb R, Pleiss MA, Thorsett ED, Ye M, and Hawkinson JE (2006) inventors; Elan Pharmaceuticals, Inc., assignee. Sulfonylquinoxaline derivatives as bradykinin antagonists. U.S. Patent 7,056,937. 2006 Jun 6.
16. Ha SN, Hey PJ, Ransom RW, Bock MG, Su DS, Murphy KL, Chang R, Chen TB, Pettibone D, and Hess JF (2006) Identification of the critical residues of bradykinin receptor B1 for interaction with the kinins guided by site-directed mutagenesis and molecular modeling. Biochemistry 45:14355-14361.
17. Hess JF, Derrick AW, MacNeil T, and Borkowski JA (1996) The agonist selectivity of a mouse B1 bradykinin receptor differs from human and rabbit B1 receptors. Immunopharmacology 33:1-8.
18. 1 (substance P) receptor antagonists- why are they not analgesic in humans. Trends Pharmacol Sci 21:244-246.
19. Hökfelt T, Holmberg K, Shi TJ, and Broberger C (2001) CCK-ergic mechanisms in sensory systems. Scand J Clin Lab Invest Suppl 234:69-74.
20. 1 receptors from rat and human. Eur J Pharmacol 374:423-433.
21. 2 analysis in rhesus monkeys. J Pharmacol Exp Ther 285:518-526.
22. Ko MC and Lee H (2002) An experimental model of inflammatory pain in monkeys: comparison of antinociceptive effects of opioids and NSAIDs against carrageenan-induced thermal hyperalgesia, in 10th World Congress on Pain (Abstract), p. 136, International Association for the Study of Pain (IASP) Press, Seattle, WA.
23. Ko MCH, Song MS, Edwards T, Lee H, and Naughton NN (2004) The role of central mu opioid receptors in opioid-induced itch in primates. J Pharmacol Exp Ther 310:169-176.
24. 1 receptor antagonists. J Med Chem 47:6439-6442.
25. 1 receptor antagonist on increased plasma extravasation in streptozotocin-induced diabetic rats: distinct vasculopathic profile of major key organs. Eur J Pharmacol 514:69-78.
26. Leeb-Lundberg LM, Marceau F, Muller-Esterl W, Pettibone DJ, and Zuraw BL (2005) International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences. Pharmacol Rev 57:27-77.
27. Levy D and Zochodne DW (2000) Increased mRNA expression of the B1 and B2 bradykinin receptors and antinociceptive effects of their antagonists in an animal model of neuropathic pain. Pain 86:265-271.
28. 1 receptors. Can J Physiol Pharmacol 75:735-740.
29. 1 receptor expression and leukocyte trafficking across mouse mesenteric postcapillary venules. J Exp Med 192:367-380.
30. 1 receptors. Br J Pharmacol 117:1619-1624.
31. 8]-BK and HOE 140, in two models of persistent hyperalgesia in the rat. Pain 53:191-197.
32. Pesquero JB, Araujo RC, Heppenstall PA, Stucky CL, Silva JA, Walther T, Oliveira SM, Pesquero JL, Paiva AC, Calixto JB, et al. (2000) Hypoalgesia and altered inflammatory responses in mice lacking kinin B1 receptors. Proc Natl Acad Sci U S A 97:8140-8145.
33. 2 receptors, tumour necrosis factor α and inflammatory hyperalgesia. Br J Pharmacol 126:649-656.
34. 1 receptor antagonist. J Pharmacol Exp Ther 318:195-205.
35. Raidoo DM and Bhoola KD (1997) Kinin receptors on human neurones. J Neuroimmunol 77:39-44.
36. 1 receptor antagonist. Eur J Pharmacol 499:77-84.
37. Regoli D, Rizzi A, Perron SI, and Gobeil F (2001) Classification of kinin receptors. Biol Chem 382:31-35.
38. Salvemini D, Wang ZQ, Wyatt PS, Bourdon DM, Marino MH, Manning PT, and Currie MG (1996) Nitric oxide: a key mediator in the early and late phase of carrageenan-induced rat paw inflammation. Br J Pharmacol 118:829-838.
39. 1 receptor agonists. Am J Physiol 284:H1959-H1968.
40. Shughrue PJ, Ky B, and Austin CP (2003) Localization of B1 bradykinin receptor mRNA in the primate brain and spinal cord: an in situ hybridization study. J Comp Neurol 465:372-384.
41. 1 receptor antagonist. J Am Chem Soc 125:7516-7517.
42. 1 receptor in MH-S murine alveolar macrophage cell line. Biochem Biophys Res Commun 259:476-482.
43. Wotherspoon G and Winter J (2000) Bradykinin B1 receptor is constitutively expressed in the rat sensory nervous system. Neurosci Lett 294:175-178.