49
Views
10
CrossRef citations to date
0
Altmetric
Review

Recent advances in neurokinin-3 receptor antagonists

, &
Pages 939-960 | Published online: 25 Feb 2005

Bibliography

  • REGOLI D, BOUDON A, FAUCHERE JL: Receptors and antagonists, for substance P and related peptides. Pharmacol. Rev. (1994) 46:551–599.
  • ••General and deep pharmacological review on tachykininreceptors and their antagonists.
  • GIARDINA GAM, RAVEGLIA LF, GRUGNI M: Lead genera- tion, and lead optimization processes in the discovery of selective nonpeptide neurokinin receptor antago-nists. Drugs Fut. (1997) 22(10:1235–1257.
  • ••Well documented description of the rationale which drovemedicinal chemistry in the tachykinin area.
  • GAO Z, PEET NP: Recent advances in neurokinin receptor antagonists. Curr. Med. Chem. (1999) 6:375–388.
  • VON SPRECHER A, GERSPACHER M, ANDERSON GP: Neurokinin antagonists as potential therapies for inflammation and rheumatoid arthritis. IDrugs (1998) 1 (1):73–91.
  • SWAIN CJ: Neurokinin receptor antagonists. In: Progress in Medicinal Chemistry (Volume 35). Ellis GP, Luscombe DK, Oxford AW (Eds.), Elsevier Science B.V. (1998):57–81.
  • SEWARD EM, SWAIN CJ: Neurokinin receptor antago-nists. Exp. Opin. Ther. Patents (1999) 9(5):571–582.
  • EMONDS-ALT X, BICHON D, DUCOUX JP et al: SR 142801, the first potent non-peptide antagonist of the tachykinin NK-3 receptor. Life Sci. (1995) 56:PL27–32.
  • ••Disclosure of the first potent and selective non-peptide NK-3receptor antagonist.
  • GIARDINA GAM, SARAU HM, FARINA C et al.: 2-Pheny1-4- quinolinecarboxamides,: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor. J. Med. Chem. (1996) 39:2281–2284.
  • ••First medicinal chemistry paper on quinoline hNK-3receptor antagonists and in vitro profile of SB–223412.
  • GIARDINA GAM, RAVEGLIA LF: Neurokinin-3 receptor antagonists,. Exp. Opin. Ther. Patents (1997) 7 (4):307–323.
  • •The present review update is a continuation of this review.
  • HARRISON T, KORSGAARD MPG, SWAIN CJ, CASCIERI MA, SADOWSKI S, SEABROOK GR: High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template. Bioorg. Med. Chem. Lett. (1998) 8:1343–1348.
  • •It rationalises some key findings on NK-3 versus NK-2 receptor selectivity in the dichlorophenylalkylpiperidine series.
  • CHEN MH, CHUNG F-Z, ROTH BD, KUO BS, ATHERTON J, LEE HT: Syntheses and biological activities of chiral piperidines-tachykinin NK-3 antagonists. Acta Pharmacol. Sin. (1999) 20(3):283–288.
  • RAVEGLIA LF, VITALI M, ARTICO M et al.: Investigation of SAR requirements of SR142801 through an indexed combinatorial library in solution. Eur. J. Med. Chem. (1999) 34:825–835.
  • PIRRUNG MC, CHEN J: Preparation and screening against acetylcholinesterase of a non-peptide 'indexed' combinatorial library. J. Am. Chem. Soc. (1995) 117:1240–1245.
  • GIARDINA GAM, GRUGNI M, RIGOLIO R, VASSALLO M, ERHARD K, FARINA C: A reliable and efficient synthesis of SR 142,801. Bioorg. Med. Chem. Lett. (1996) 6:2307–2310.
  • CHENG HG, CHUNG F-Z, GOEL OP. et al.: A practical and scalable synthesis of SR 142,801, a tachykinin NK-3 antagonist. Bioorg. Med. Chem. Lett. (1997) 7:555–560.
  • SNIDER RM, CONSTANTINE SJW, LOWE JA et al.: A potent non-peptide antagonist of the substance P (NK-1) receptor. Science (1991) 251:435–437.
  • ••A milestone in the discovery of non-peptide NK-1 receptorantagonists.
  • GIARDINA GAM, SARAU HM, FARINA C et al: Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. I. Identification of the 4-quinolinecarboxamide framework. J. Med. Chem. (1997) 40:1794–1807.
  • GIARDINA GAM, RAVEGLIA LF, GRUGNI M et al.:Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. II. Identification of SB 223412. J. Med. Chem. (1999) 42:1053–1065.
  • •It describes in detail the rationale behind the identification of SB-223412.
  • SARAU HM, GRISWOLD D, POTTS W et al.: Nonpeptide tachykinin, receptor antagonists. I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective NK-3 receptor antagonist. J. Pharmacol. Exp. Ther. (1997) 281:1303–1311.
  • •Full pharmacological description of SB-223412.
  • YOUNG RC, MITCHELL RC, BROWN TH et al. Develop- ment, of a new physicochemical model for brain penetration and its application to the design of centrally acting 112 receptor histamine antagonists. J. Med. Chem. (1988) 31(3):656–671.
  • RAVEGLIA LF, GIARDINA GAM, GRUGNI M et al.: Discovery of potent and selective, non-brain penetrant NK-3 receptor antagonists. Proceedings of the 1st Italian-Swiss Meeting on Medicinal Chemistry. Torino, Italy (1997):49.
  • RAVEGLIA LF, POTTS WM, GRAZIANI D et al.: Quinoline NK-3 receptor antagonists: chemical strategies to prevent (?-1) metabolic oxidation. Proceedings of the 15th EFMC International Symposium on Medicinal Chemistry. Edinburgh, UK (1998):62
  • GIARDINA GAM, ARTICO M, CAVAGNERA S et al.: Replacement of the quinoline system in 2-phenyl-4-quinolinecarboxamide NK-3 receptor antagonists. II Farmaco (1999) 54(6):364–374.
  • MILEUSNIC D, LEE JM, MAGNUSON DJ et al.: Neurokinin-3 receptor distribution in rat and human brain:an immunohistochemical study. Neuroscience (1999) 89(4):1269–1290.
  • MILEUSNIC D, MAGNUSON DJ, HEINA MJ, LORENS JB, LORENS SA, LEE JM: Age and species-dependent differences, in the neurokinin B system in rat and human brain. Neurobiol. Ageing (1999) 20:19–35.
  • ZERARI F, KARPITSKIJ V, KRAUSE J, DESCARRIES L,COUTURE R: Immunoelectron microscopic localiza-tion of NK-3 receptor in the rat spinal cord. Neuroreport (1997) 8:2661–2664.
  • SEYBOLD VS, GRKOVIC I, PORTBURY AL et al.: Relation-ship of NK-3 receptor immunoreactivity to subpopula-tions of neurones in rat spinal cord. J. Comparative Neurol. (1997) 381: 439–448.
  • MANN PT, SOUTHWELL BR, DING Y-Q, SHIGEMOTO R,MIZUNO N, FURNESS JB: Localisation of neurokinin 3 (NK3) receptor immunoreactivity in the rat gastroin-testinal tract. Cell. Tissue Res. (1997) 289:1–9.
  • MEDHURST AD, PARSONS AA, ROBERTS JC, HAY DWP:Characterization of NK-3 receptors in rabbit isolated iris sphincter muscle. Br. J. Pharmacol. (1997) 120(1):93–101.
  • MEDHURST AD, HAY DWP, PARSONS AA, MARTIN LD,GRISWOLD DE: In vitro and in vivo characterization of NK-3 receptors in the rabbit eye by use of selective non-peptide NK-3 receptor antagonists. Br. J. Pharmacol. (1997) 122(3)469–476.
  • MEDHURST AD, HIRST WD, JERMAN JC et al.: Molecularand pharmacological characterization of a functional tachykinin NK-3 receptor cloned from the rabbit iris sphincter muscle. Br. J. Pharmacol (1999) 128:627–636.
  • OYAMADA H, TAKATSUJI K, SENBA E, MANTYH PW, TOHYAMA M: Postnatal development of NK-1, NK-2 and NK-3 neurokinin receptors expression in the rat retina. Dev. Brain Res. (1999) 117:59–70.
  • COUDORE-CIVIALE M-A, COURTEIX C, ESCHALIER A, FIALIP J: Effect of tachykinin receptor antagonists in experimental neuropathic pain. Eur. J. Pharmacol (1998) 361:175–184.
  • SCHMID G, CARITA F, BONANNO G, RAITERI M: NK-3 receptors mediate enhancement of substance P release from capsaicin-sensitive spinal cord afferent terminals. Br. J. Pharmacol. (1998) 125:621–626.
  • •First strong evidence that NK-3 receptor antagonists (like SR 142,801) might be useful in controlling pain transmission.
  • ZARATIN P, ANGELICI 0, CLARKE GD et al.: NK3 receptor blockade, prevents hyperalgesia and the associated spinal cord substance P release in monoarthritic rats. Neuropharmacology (1999) 39 (0 :141–149.
  • ••It demonstrates that SB-223412 administered systemically tomonoarthritic rats significantly reduces the thermal hyperal-gesia and, hence, NK-3 receptor antagonists may be useful to treat inflammatory pain conditions.
  • LINDEN DR, JIA Y-P, SEYBOLD VS: Spinal neurokinin 3receptors facilitate the nociceptive flexor reflex via a pathway involving nitric oxide. Pain (1999) 80:301–308.
  • LINDEN DR, SEYBOLD VS: Spinal neurokinin 3receptors mediate thermal but not mechanical hyperalgesia via nitric oxide. Pain (1999) 80:309–317.
  • COUTURE R, TOMA N, BARBOT L: SR 142,801 behaves as a, tachykinin receptor agonist on spinal nociceptive reflex in the rat. Life Sci. (2000) 66(0:51–65.
  • •First evidence that SR 142,801 behaves as an agonist at the central rat NK-3 receptor.
  • RIBEIRO SJ, DE LIMA TCM: Naloxone-induced changesin tachykinin NK-3 receptor modulation of experi-mental anxiety in mice. Neurosci. Lett. (1998) 258:155–158.
  • RIBEIRO SJ, TEIXEIRA RM, CALIXTO JB, DE LIMA TCM:Tachykinin NK-3 receptor involvement in anxiety. Neuropeptides (1999) 33(2):181–188.
  • NALIVAIKO E, MICHAUD J-C, SOUBRIE P, LE FUR G,FELTZ P: Tachykinin neurokinin-1 and neurokinin-3 receptor-mediated responses in guinea-pig substantia nigra: an in vitro electrophysiological study. Neurosci. (1997) 78 (3) :745–757.
  • GUEUDET C, SANTUCCI V, SOUBRIE' P, LE FUR G:Blockade of neurokinin-3 receptors antagonizes drug-induced population response and depolarization block of midbrain neurons in guinea pigs. Synapse (1999) 33:71–79.
  • HAY DWP, BARNETTE MS: Current and potential newtherapies for chronic obstructive pulmonary disease. In: Annual Reports in Medicinal Chemistry (Volume 34). Doherty AM (Ed.), Academic Press (1999):111–120.
  • BUELL G, SCHULZ MF, ARKINSTALL SJ et al.: Molecular characterization, expression and localization of human neurokinin-3 receptor. FEBS Lett. (1992) 299:90–95.
  • ••Historical paper on localisation, cloning and expression ofthe hNK-3 receptor, including evidence for the presence of NK-3 mRNA in human lung.
  • MYERS AC, UNDEM BJ: Electrophysiological effects of tachykinins, and capsaicin on guinea pig bronchial parasympathetic ganglion neurons. J. Physiol (1993) 470:665–679.
  • •First evidence for a neuromodulatory role of the NK-3 receptor in guinea-pig bronchial parasympathetic ganglia.
  • CANNING BJ, FISCHER A, UNDEM BJ: Pharmacologicalanalysis of the tachykinin receptors that mediate activation of nonadrenergic, noncholinergic relaxant nerves that innervate guinea pig trachealis. J. Pharmacol. Exp. Ther. (1998) 284:370–377.
  • DAOUI S, CUI Y-Y, LAGENTE V, EMONDS-ALT X, ADVENIER C: A tachykinin NK3 receptor antagonist, SR 142,801 (osanetant), prevents substance P-induced bronchial hyperreactivity in guinea-pigs. Pulm. Pharmacol. Ther. (1997) 10(5/6):261–270.
  • •First evidence that SR 142,801 is effective against cough and bronchial hyper-reactivity in guinea-pigs.
  • DAOUI S, COGNON C, NALINE E, EMONDS-ALT X, ADVENIER C: Involvement of tachykinin NK3 receptors in citric acid-induced cough and bronchial responses in guinea pigs. Am. J. Resp. Crit. Care Merl. (1998) 158(0:42–48.
  • GOLDHILL J, ANGEL I: Mechanism of tachykinin NK-3receptor-mediated colonic ion transport in the guinea pig. Eur.J. Pharmacol. (1998) 363:161–168.
  • JULIA V, SU X, BUENO L, GEBHART GF: Role of neurokinin 3 receptors on responses to colorectal distension in the rat: electrophysiological and behaviour studies. Gastroenterology (1999) 116:1124–1131.
  • BROCCARDO M, IMPROTA G, TABACCO A: Central tachykinin NK-3 receptors in the inhibitory action on the rat colonic propulsion of a new tachykinin, PG-KII. Eur. J. Pharmacol. (1999) 376:67–71.
  • CELLIER E, BARBOT L, REGOLI D, COUTURE R: Cardio-vascular and behavioural effects of intracerebroven-tricularly administered tachykinin NK-3 receptor antagonists in the conscious rat. Br. J. Pharmacol. (1997) 122:643–654.
  • YUAN Y-D, COUTURE R: Renal effects of intracerebrov-entricularly injected tachykinins in the conscious saline-loaded rat: receptor characterization. Br J. Pharmacol. (1997) 120:785–796.
  • SCRIP No. 2520 (March 8th 2000):8.
  • SARAU HM, GRISWOLD DE, POTTS W: Pharmacology of SB 222200, a selective high affinity orally active nonpeptide NK-3 receptor antagonist. Proceedings of the International Tachykinin Conference - Tachykinins in Health and Disease. Cairns, Australia (1997):5.
  • DONALDSON LF, HASKELL CA, HANLEY MR: Functional characterization by heterologous expression of a novel cloned tachykinin peptide receptor. Biochem. J. (1996) 320:1–5.
  • SARAU HM, SCHMIDT DB, HAY DWP: [311] SB 222200, a nonpeptide NK-3 receptor antagonist ligand: binding to human NK-3 and `IsIK-4' receptors. Proceedings of the International Tachykinin Conference - Tachykinins in Health and Disease. Cairns, Australia (1997)P7, p. 29.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.