Pharmacological characterization of RWJ-676070, a dual vasopressin V1A/V2 receptor antagonist

European Journal of Pharmacology

Volumn 590, Issue 1-3, 2008, Pages 333-342

  Gunnet, Joseph W ^a,b   Wines, Pamela ^a,c   Xiang, Min ^a   Rybczynski, Philip ^a,d   Andrade Gordon, Patricia ^a   de Garavilla, Lawrence ^a   Parry, Tom J ^a   Cheung, Wai man ^a   Minor, Lisa ^a   Demarest, Keith T ^a   Maryanoff, Bruce E ^a   Damiano, Bruce P ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

^b Chromocell Corporation   (United States)

^c Amicus Therapeutics ^*  (United States)

^d Amicus Therapeutics   (United States)

Author keywords

Aquaresis; Arginine vasopressin; Arterial blood pressure; Hypertension; RWJ 676070; Vasopressin antagonist

Indexed keywords

1 [4 [(2 CHLORO 5 FLUOROBENZOYL)AMINO] 3 METHOXYBENZOYL] 1,2,3,5 TETRAHYDROSPIRO[4H 1 BENZAZEPINE 4,1' [2]CYCLOPENTENE] 3' CARBOXYLIC ACID; ARGIPRESSIN; CALCIUM; CYCLIC AMP; JNJ 17158063; OXYTOCIN RECEPTOR; RWJ 676070; UNCLASSIFIED DRUG; VASOPRESSIN; VASOPRESSIN RECEPTOR ANTAGONIST; VASOPRESSIN V1A RECEPTOR; VASOPRESSIN V1B RECEPTOR; VASOPRESSIN V2 RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTERIAL PRESSURE; ARTICLE; CALCIUM CELL LEVEL; CALCIUM MOBILIZATION; CONTROLLED STUDY; DOG; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG ELIMINATION; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; FEMALE; HUMAN; HUMAN CELL; HYPERTENSION; IN VITRO STUDY; IN VIVO STUDY; MALE; MONKEY; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; RECEPTOR UPREGULATION; SPONTANEOUSLY HYPERTENSIVE RAT; THROMBOCYTE AGGREGATION; VASCULAR RING; VASOCONSTRICTION;

ANIMALS; BENZAZEPINES; BLOOD PRESSURE; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; HEART RATE; HUMANS; HYPERTENSION; MACACA FASCICULARIS; MALE; PLATELET AGGREGATION; RATS; RATS, INBRED SHR; RECEPTORS, VASOPRESSIN; SPIRO COMPOUNDS; VASOCONSTRICTION; VASOPRESSINS;

EID: 48149103211     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2008.06.010     Document Type: Article

References (52)

1. Ali F., Guglin M., Vaitkevicius P., and Ghali J.K. Therapeutic potential of vasopressin receptor antagonists. Drugs 67 (2007) 847-858
2. Anderson R.J., Chung H.M., Kluge R., and Schrier R.W. Hyponatremia: a prospective analysis of its epidemiology and the pathogenetic role of vasopressin. Ann. Intern. Med. 102 (1985) 164-168
3. Arai Y., Fujimori A., Sudoh K., and Sasamata M. Vasopressin receptor antagonists: potential indications and clinical results. Curr. Opin. Pharmacol. 7 (2007) 124-129
4. Bakris G., Bursztyn M., Gavras I., Bresnahan M., and Gavras H. Role of vasopressin in essential hypertension: racial differences. J. Hypertens. 15 (1997) 545-550
5. Bankir L., Bardoux P., and Ahloulay M. Vasopressin and diabetes mellitus. Nephron 87 (2001) 8-18
6. Burrell L.M., Phillips P.A., Stephenson J.M., Risvanis J., Rolls K.A., and Johnston C.I. Blood pressure-lowering effect of an orally active vasopressin V1 receptor antagonist in mineralocorticoid hypertension in the rat. Hypertension 23 (1994) 737-743
7. Chatterjee K. Neurohormonal activation in congestive heart failure and the role of vasopressin. Am. J. Cardiol. 95 (2005) 8B-13B
8. Clair M.J., King M.K., Goldberg A.T., Hendrick J.W., Nisato R., Gay D.M., Morrison A.E., McElmurray III J.H., Krombach R.S., Bond B.R., Cazaubon C., Nisato D., and Spinale F.G. Selective vasopressin, angiotensin II, or dual receptor blockade with developing congestive heart failure. J. Pharmacol. Exp. Ther. 293 (2000) 852-860
9. Crofton J.T., Ota M., and Share L. Role of vasopressin, the renin-angiotensin system and sex in Dahl salt-sensitive hypertension. J. Hypertens. 11 (1993) 1031-1038
10. Doczi T., Laszlo F.A., Szerdahelyi P., and Joo F. Involvement of vasopressin in brain edema formation: further evidence obtained from the Brattleboro diabetes insipidus rat with experimental subarachnoid hemorrhage. Neurosurgery 14 (1984) 436-441
11. Filep J., and Rosenkranz B. Mechanism of vasopressin-induced platelet aggregation. Thromb. Res. 45 (1987) 7-15
12. Francis G.S., Benedict C., Johnstone D.E., Kirlin P.C., Nicklas J., Liang C.S., Kubo S.H., Rudin-Toretsky E., and Yusuf S. Comparison of neuroendocrine activation in patients with left ventricular dysfunction with and without congestive heart failure. A substudy of the studies of left ventricular dysfunction (SOLVD). Circulation 82 (1990) 1724-1729
13. Fukuzawa J., Haneda T., and Kikuchi K. Arginine vasopressin increases the rate of protein synthesis in isolated perfused adult rat heart via the V1 receptor. Mol. Cell. Biochem. 195 (1999) 93-98
14. Gavras H., Hatzinikolaou P., North W.G., Bresnahan M., Gavras I., Doggrell S.A., Guay Woodford L.M., Konstam M.A., Naitoh M., Risvanis J., Balding L.C., Johnston C.I., Burrell L.M., Zwieten P.A.v., Aldred K.L., Kenney P.J., Phillips P.A., Hutchins A.M., Buschauer A., Berecek K.H., Wyss J.M., Swords B.H., Ruffolo Jr. R.R., Hieble J.P., Brooks D.P., Feuerstein G.Z., and Nichols A.J. Interaction of the sympathetic nervous system with vasopressin and renin in the maintenance of blood pressure. Hypertension 4 (1982) 400-405
15. 2-receptor blockade with tolvaptan in patients with chronic heart failure: results from a double-blind, randomized trial. Circulation 107 (2003) 2690-2696
16. Gheorghiade M., Gattis W.A., O'Connor C.M., Adams Jr. K.F., Elkayam U., Barbagelata A., Ghali J.K., Benza R.L., McGrew F.A., Klapholz M., Ouyang J., and Orlandi C. Acute and chronic therapeutic impact of a vasopressin antagonist in congestive heart failure, I., Effects of tolvaptan, a vasopressin antagonist, in patients hospitalized with worsening heart failure: a randomized controlled trial. JAMA 291 (2004) 1963-1971
17. Ghosh P.M., Mikhailova M., Bedolla R., and Kreisberg J.I. Arginine vasopressin stimulates mesangial cell proliferation by activating the epidermal growth factor receptor. Am. J. Physiol. Renal Physiol. 280 (2001) F972-F979
18. Goldsmith S.R. Congestive heart failure: potential role of arginine vasopressin antagonists in the therapy of heart failure. Congest. Heart Fail. 8 (2002) 251-256
19. 2 receptor antagonists?. Am. J. Med. 119 (2006) S93-S96
20. Goldsmith S.R., Francis G.S., Cowley Jr. A.W., Levine T.B., and Cohn J.N. Increased plasma arginine vasopressin levels in patients with congestive heart failure. J. Am. Coll. Cardiol. 1 (1983) 1385-1390
21. Griebel G., Simiand J., Stemmelin J., Gal C.S., and Steinberg R. The vasopressin V1B receptor as a therapeutic target in stress-related disorders. Curr. Drug Targets CNS Neurol. Disord. 2 (2003) 191-200
22. 2 receptor antagonists on the development of salt-induced hypertension in Dahl rats. J. Cardiovasc. Pharmacol. 26 (1995) 548-554
23. Hofbauer K.G., Mah S.C., Wood J.M., Baum H.P., Hanni H., Opperman J.R., and Kraetz J. Contribution of vascular and tubular effects of arginine-vasopressin to the development of deoxycorticosterone acetate (DOCA)-salt hypertension in rats. J. Hypertens., Suppl. 2 (1984) S333-335
24. Inaba K., Umeda Y., Yamane Y., Urakami M., and Inada M. Characterization of human platelet vasopressin receptor and the relation between vasopressin-induced platelet aggregation and vasopressin binding to platelets. Clin. Endocrinol. (Oxf.) 29 (1988) 377-386
25. Konstam M.A., Gheorghiade M., Burnett Jr. J.C., Grinfeld L., Maggioni A.P., Swedberg K., Udelson J.E., Zannad F., Cook T., Ouyang J., Zimmer C., and Orlandi C. Efficacy of vasopressin antagonism in heart failure outcome study with tolvaptan, I. Effects of oral tolvaptan in patients hospitalized for worsening heart failure: the EVEREST outcome trial. JAMA 297 (2007) 1319-1331
26. Kurihara I., Saito T., Obara K., Shoji Y., Hirai M., Soma J., Sato H., Imai Y., and Abe K. Effect of a nonpeptide vasopressin V1 antagonist (OPC-21268) on experimental accelerated focal glomerulosclerosis. Nephron 73 (1996) 629-636
27. 2 receptor antagonist, in a rabbit model of ocular hypertension. J. Ocular Pharmacol. Ther. 16 (2000) 203-216
28. Laszlo F.A., Laszlo Jr. F., and De Wied D. Pharmacology and clinical perspectives of vasopressin antagonists. Pharmacol. Rev. 43 (1991) 73-108
29. Matsuguchi H., Schmid P.G., Van Orden D., and Mark A.L. Does vasopressin contribute to salt-induced hypertension in the Dahl strain?. Hypertension 3 (1981) 174-181
30. Miyazaki T., Fujiki H., Yamamura Y., Nakamura S., and Mori T. Tolvaptan, an orally active vasopressin V(2)-receptor antagonist-pharmacology and clinical trials. Cardiovasc. Drug Rev. 25 (2007) 1-13
31. Mulinari R.A., Gavras I., Wang Y.X., Franco R., and Gavras H. Effects of a vasopressin antagonist with combined antipressor and antiantidiuretic activities in rats with left ventricular dysfunction. Circulation 81 (1990) 308-311
32. Naitoh M., Suzuki H., Murakami M., Matsumoto A., Arakawa K., Ichihara A., Nakamoto H., Oka K., Yamamura Y., and Saruta T. Effects of oral AVP receptor antagonists OPC-21268 and OPC-31260 on congestive heart failure in conscious dogs. Am. J. Physiol. 26 (1994) H2245-H2254
33. Okada H., Suzuki H., Kanno Y., Yamamura Y., and Saruta T. Chronic and selective vasopressin blockade in spontaneously hypertensive rats. Am. J. Physiol. 267 (1994) R1467-R1471
34. Reilly B.A., Brostrom M.A., and Brostrom C.O. Regulation of protein synthesis in ventricular myocytes by vasopressin. The role of sarcoplasmic/endoplasmic reticulum Ca2+ stores. J. Biol. Chem. 273 (1998) 3747-3755
35. Rossi J., Orlandi C., and Gheorghiade M. Vasopressin antagonists in the management of heart failure. Expert Rev. Cardiovasc. Ther. 5 (2007) 323-330
36. Russell S.D., Selaru P., Pyne D.A., Ghazzi M.M., Massey K.D., Pressler M., Serikoff A., Coats A.J.S., and Bonow R.O. Rationale for use of an exercise end point and design for the advance (a dose evaluation of a vasopressin antagonist in CHF patients undergoing exercise) trial. Am. Heart J. 145 (2003) 179-186
37. Schrier R.W., and Fassett R.G. Pathogenesis of sodium and water retention in cardiac failure. Ren. Fail. 20 (1998) 773-781
38. Schrier R.W., Gurevich A.K., and Cadnapaphornchai M.A. Pathogenesis and management of sodium and water retention in cardiac failure and cirrhosis. Semin. Nephrol. 21 (2001) 157-172
39. Stromberg P., Akerlund M., Forsling M.L., Granstrom E., and Kindahl H. Vasopressin and prostaglandins in premenstrual pain and primary dysmenorrhea. Acta Obstet. Gynecol. Scand. 63 (1984) 533-538
40. Sulemanjee N.Z., and Schwarz E.R. Conivaptan: a selective vasopressin antagonist. Drugs Today 42 (2006) 379-386
41. Thibonnier M., Kilani A., Rahman M., DiBlasi T.P., Warner K., Smith M.C., Leenhardt A.F., and Brouard R. Effects of the nonpeptide V(1) vasopressin receptor antagonist SR49059 in hypertensive patients. Hypertension 34 (1999) 1293-1300
42. Thibonnier M., Coles P., Thibonnier A., and Shoham M. Molecular pharmacology and modeling of vasopressin receptors. Prog. Brain Res. 139 (2002) 179-196
43. Tomura Y., Tahara A., Tsukada J., Yatsu T., Uchida W., Iizumi Y., and Honda K. Pharmacological profile of orally administered YM087, a vasopressin antagonist, in conscious rats. Clin. Exp. Pharmacol. Physiol. 26 (1999) 399-403
44. Wada K., Fujimori A., Matsukawa U., Arai Y., Sudoh K., Yatsu T., Sasamata M., and Miyata K. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur. J. Pharmacol. 507 (2005) 145-151
45. Walter K.A. Conivaptan: new treatment for hyponatremia. Am. J. Health-Syst. Pharm. 64 (2007) 1385-1395
46. Weber R., Pechere-Bertschi A., Hayoz D., Gerc V., Brouard R., Lahmy J.P., Brunner H.R., and Burnier M. Effects of SR 49059, a new orally active and specific vasopressin V1 receptor antagonist, on vasopressin-induced vasoconstriction in humans. Hypertension 30 (1997) 1121-1127
47. Wigger A., Sanchez M.M., Mathys K.C., Ebner K., Frank E., Liu D., Kresse A., Neumann I.D., Holsboer F., and Plotsky P.M. Alterations in central neuropeptide expression, release, and receptor binding in rats bred for high anxiety: critical role of vasopressin. Neuropsychopharmacology 29 (2004) 1-14
48. 1A/V2 receptor antagonist for human clinical studies. Bioorg. Med. Chem. Lett. 17 (2007) 6623-6628
49. Yamada Y., Yamamura Y., Chihara T., Onogawa T., Nakamura S., Yamashita T., Mori T., Tominaga M., and Yabuuchi Y. OPC-21268, a vasopressin V1 antagonist, produces hypotension in spontaneously hypertensive rats. Hypertension 23 (1994) 200-204
50. Yamamura Y., Ogawa H., Yamashita H., Chihara T., Miyamoto H., Nakamura S., Onogawa T., Yamashita T., Hosokawa T., Mori T., et al. Characterization of a novel aquaretic agent, OPC-31260, as an orally effective, nonpeptide vasopressin V2 receptor antagonist. Br. J. Pharmacol. 105 (1992) 787-791
51. Yeates K.E., and Morton A.R. Vasopressin antagonists: role in the management of hyponatremia. Am. J. Nephrol. 26 (2006) 348-355
52. Yuan B., and Cowley Jr. A.W. Evidence that reduced renal medullary nitric oxide synthase activity of Dahl s rats enables small elevations of arginine vasopressin to produce sustained hypertension. Hypertension 37 (2001) 524-528