Recent developments in transient receptor potential vanilloid receptor 1 agonist-based therapies

Expert Opinion on Investigational Drugs

Volumn 13, Issue 11, 2004, Pages 1445-1456

  Bley, Keith R ^a  

^a NeurogesX Inc   (United States)

Author keywords

Analgesia; Bladder; Capsaicin; Joints; Nociceptors; Pain; Skin; TRPV1

Indexed keywords

12 HYDROXYICOSATETRAENOIC ACID; [[[4 (2 AMINOETHOXY) 3 METHOXYPHENYL]METHYL]AMINO] N [[4 (TERT BUTYL)PHENYL]METHYL]CARBOXAMIDE; ANALGESIC AGENT; ANANDAMIDE; CAPSAICIN; CAPSAICIN DERIVATIVE; CAPSAVANIL; CIS CAPSAICIN; N [3 (3,4 DIMETHYLPHENYL)PROPYL] 4 (2 AMINOETHOXY) 3 METHOXYPHENYLACETAMIDE; NGX 4010; NUVANIL; OLVANIL; RESINIFERATOXIN; SDZ 249665; TRANSIENT RECEPTOR POTENTIAL CHANNEL; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1; WL 1001; ZOSTRIX HP;

ANALGESIC ACTIVITY; ANTINOCICEPTION; CALCIUM SIGNALING; CHANNEL GATING; CLINICAL TRIAL; DRUG INDICATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; HEMATURIA; HIGH THROUGHPUT SCREENING; HUMAN; INCONTINENCE; LACRIMATION; MEDICAL RESEARCH; MOUSE; NEUROPATHIC PAIN; NOCICEPTION; NONHUMAN; NOSE IRRITATION; OVERACTIVE BLADDER; PATENT; PATHOPHYSIOLOGY; PELVIS PAIN SYNDROME; RECEPTOR BLOCKING; REVIEW; SENSORY NERVE CELL; SIDE EFFECT; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; URINARY TRACT DISEASE;

CAPSAICIN; HUMANS; PAIN; RECEPTORS, DRUG; URINARY BLADDER;

EID: 8844221985     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.13.11.1445     Document Type: Review

References (79)

1. CATERINA MJ, JULIUS D: The vanilloid receptor: a molecular gateway to the pain pathway. Ann. Rev. Neurosci. (2001) 24 487-517.
2. LOPEZ-RODRIGUEZ ML, VISO A, ORTEGA-GUTIERREZ S: VR1 receptor modulators as potential drugs for neuropathic pain. Mini Rev. Med. Chem. (2003) 3:729-748.
3. PUNTAMBEKAR P, VAN BUREN J, RAISINGHANI M et al.: Direct interaction of adenosine with the TRPV1 channel protein. J. Neurosci. (2004) 24:3663-3671.
4. CHEN SC, CHANG TJ, WU FS: Competitive inhibition of the capsaicin receptor-mediated current by dehydroepiandrosterone in rat dorsal root ganglion neurons. J. Pharmacol. Exp. Ther. (2004) [Epub ahead of print].
5. CORTRIGHT DN, SZALLASI A: Biochemical pharmacology of the vanilloid receptor TRPV1. An update. Eur. J. Biochem. (2004) 271 1814-1819.
6. HOEGYES E: Beitrage zur physiologischen wirkung der bestandteile des capsicum annum. Arch. Exp. Pathol. Pharmacol. (1878) 9:117-130.
7. JANCSO N: The role of sensory nerve endings in inflammatory reactions Bull. Millard Fillmore Hosp. (1960) 7:53-77.
8. CATERINA MJ, SCHUMACHER MA, TOMINAGA M et al.: The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature (1997) 389:816-824.
9. STERNER O, SZALLASI A: Novel natural vanilloid receptor agonists: new therapeutic targets for drug development. Trends Pharmacol Sci. (1999) 20:459-465.
10. CORDELL GA, ARAUJO OE: Capsaicin: identification, nomenclature, and pharmacotherapy. Ann. Pharmacother. (1993) 27 330-336.
11. TEWKSBURY JJ, NABHAN GP: Seed dispersal. Directed deterrence by capsaicin in chilies. Nature (2001) 412:403-404.
12. JORDT SE, JULIUS D: Molecular basis for species-specific sensitivity to 'hot' chili peppers. Cell (2002) 108:421-430.
13. KENNEDY WR: Opportunities afforded by the study of unmyelinated nerves in skin and other organs. Muscle Nerve (2004) 29:756-767.
14. SIMONE DA, NOLANO M, JOHNSON T et al.: Intradermal injection of capsaicin in humans produces degeneration and subsequent reinnervation of epidermal nerve fibers: correlation with sensory function. J. Neurosci. (1998) 18:8947-8959.
15. DUX M, SANN H, SCHEMANN M et al.: Changes in fibre populations of the rat hairy skin following selective chemodenervation by capsaicin. Cell Tissue Res. (1999) 296:471-477.
16. STANDER S, MOORMANN C, SCHUMACHER M et al.: Expression of vanilloid receptor subtype 1 in cutaneous sensory nerve fibers, mast cells, and epithelial cells of appendage structures. Exp. Dermatol. (2004) 13:129-139.
17. MORBIN M, CAPOBIANCO R, BORGNA M et al.: Painful diabetic neuropathy (PDN): a morphological study of capsaicin receptor distribution. J. Peripheral Nervous System. (2004) 9:119-120.
18. PETERSEN KL, RICE FL, SUESS F et al.: Relief of postherpetic neuralgia by surgical removal of painful skin. Pain (2002) 98:119-126.
19. SOUTHALL MD, LI T, GHARIBOVA LS et al.: Activation of epidermal vanilloid receptor-1 induces release of proinflammatory mediators in human keratinocytes. J. Pharmacol. Exp. Ther. (2003) 304:217-222.
20. KO F, DIAZ M, SMITH P et al.: Toxic effects of capsaicin on keratinocytes and fibroblasts. J. Burn Care Rehabil. (1998) 19:409-413.
21. AVELINO A, CRUZ C, NAGY I et al.: Vanilloid receptor 1 expression in the rat urinary tract. Neuroscience (2002) 109 4):787-98.
22. DE GROAT WC: A neurologic basis for the overactive bladder. Urology (1997) 50(6A Suppl.):36-52.
23. BIRDER LA, NAKAMURA Y, KISS S et al.: Altered urinary bladder function in mice lacking the vanilloid receptor TRPV1. Nat. Neurosci. (2002) 5:856-860.
24. BIRDER LA, KANAI AJ, DE GROAT WC et al.: Vanilloid receptor expression suggests a sensory role for urinary bladder epithelial cells. Proc. Natl. Acad. Sci. USA (2001) 98 13396-13401.
25. CRUZ F: Mechanisms involved in new therapies for overactive bladder. Urology (2004) 63(3 Suppl. 1):65-73.
26. TYMPANIDIS P, TERENGHI G, DOWD P: Increased innervation of the vulval vestibule in patients with vulvodynia. Br. J. Dermatol. (2003) 148:1021-1027.
27. TYMPANIDIS P, CASULA MA, YIANGOU Y et al.: Increased vanilloid receptor VR1 innervation in vulvodynia. Eur. J. Pain (2004) 8:129-133.
28. SCHMIDT RF: The articular polymodal nociceptor in health and disease. Prog. Brain Res. (1996) 113:53-81.
29. MACH DB, ROGERS SD, SABINO MC et al.: Origins of skeletal pain: sensory and sympathetic innervation of the mouse femur. Neuroscience (2002) 113:155-166.
30. NIV D, GOFELD M, DEVOR M: Causes of pain in degenerative bone and joint disease: a lesson from vertebroplasty. Pain (2003) 105 387-392.
31. 2+ by vanilloid receptor 1 in rat dorsal root ganglion neurons. J. Biol. Chem. (2003) 278:5462-5472.
32. SZALLASI A, BLUMBERG PM: Vanilloid (capsaicin) receptors and mechanisms. Pharmacol. Rev. (1999) 51:159-212.
33. MICHAELIS M: Electrophysiological characteristics of injured peripheral nerves. In: Mechanisms and Mediators of Neuropathic Pain. AB Malmberg, SR Chaplan (Eds), Birkhaeuser Verlag, Basel, Switzerland (2002).
34. ROWBOTHAM MC, YOSIPOVITCH G, CONNOLLY MK et al.: Cutaneous innervation density in the allodynic form of postherpetic neuralgia. Neurobiol. Dis. (1996) 3:205-214.
35. OAKLANDER AL: The density of remaining nerve endings in human skin with and without postherpetic neuralgia after shingles. Pain (2001) 92:139-145.
36. KENNEDY WR, WENDELSCHAFER-CRABB G, JOHNSON T: Quantitation of epidermal nerves in diabetic neuropathy. Neurology (1996) 47 1042-1048.
37. POLYDEFKIS M, YIANNOUTSOS CT, COHEN BA et al.: Reduced intraepidermal nerve fiber density in HIV-associated sensory neuropathy. Neurology (2002) 58:115-119.
38. LINDENLAUB T, SOMMER C: Epidermal innervation density after partial sciatic nerve lesion and pain-related behavior in the rat. Acta. Neuropathol. (2002) 104:137-143.
39. CAMPBELL JN: Nerve lesions and the generation of pain. Muscle Nerve (2001) 24:1261-1273.
40. MILLER MS, BUCK SH, SIPES IG et al.: Regulation of substance P by nerve growth factor: disruption by capsaicin. Brain Res. (1982) 250:193-196.
41. PETRUSKA JC, MENDELL LM: The many functions of nerve growth factor: multiple actions on nociceptors. Neurosci. Lett. (2004) 361:168-171.
42. BJERRING P, ARENDT-NIELSEN L, SODERBERG U: Argon laser induced cutaneous sensory and pain thresholds in post-herpetic neuralgia. Quantitative modulation by topical capsaicin. Acta. Derm. Venereol. (1990) 70:121-125.
43. NOLANO M, SIMONE DA, WENDELSCHAFER-CRABB G et al.: Topical capsaicin in humans: parallel loss of epidermal nerve fibers and pain sensation. Pain (1999) 81:135-145.
44. TURNBULL A: Tincture of capsaicin as a remedy for chilblains and toothache. Dublin Free Press (1850) 1:95-96.
45. MASON L, MOORE RA, DERRY S et al.: Systematic review of topical capsaicin for the treatment of chronic pain. Br. Med. J. (2004) 328:991-994.
46. McMAHON SB, LEWIN G, BLOOM SR: The consequences of long-term topical capsaicin application in the rat. Pain (1991) 44 301-310.
47. BJERRING P, ARENDT-NIELSEN L: Use of a new argon laser technique to evaluate changes in sensory and pain thresholds in human skin following topical capsaicin treatment. Skin Pharmacol. (1989) 2:162-167.
48. WALKER FO, LEWIS SF: Somesthetic and electrophysiologic effects of topical 0.025% capsaicin in man. Reg. Anesth. (1990) 15:61-66.
49. SIMONE DA, OCHOA J: Early and late effects of prolonged topical capsaicin on cutaneous sensibility and neurogenic vasodilatation in humans. Pain (1991) 47:285-294.
50. CATERINA MJ, ROSEN TA, TOMINAGA M et al.: A capsaicin-receptor homologue with a high threshold for noxious heat. Nature (1999) 398:436-441.
51. SERRA J, CAMPERO M, OCHOA J: Flare and hyperalgesia after intradermal capsaicin injection in human skin. J. Neurophysiol. (1998) 80:2801-2810.
52. PAICE JA, FERRANS CE, LASHLEY FR et al.: Topical capsaicin in the management of HIV-associated peripheral neuropathy. J. Pain Symptom Manage. (2000) 19:45-52.
53. MAGGI CA, BARBANTI G, SANTICIOLI P et al.: Cystometric evidence that capsaicin-sensitive nerves modulate the afferent branch of micturition reflex in humans. J. Urol. (1989) 142:150-154.
54. CHANCELLOR MB, DE GROAT WC: Intravesical capsaicin and resiniferatoxin therapy: spicing up the ways to treat the overactive bladder. J. Urol. (1999) 162:3-11.
55. DASGUPTA P, CHANDIRAMANI VA, BECKETT A et al.: The effect of intravesical capsaicin on the suburothelial innervation in patients with detrusor hyperreflexia. BJU Int. (2000) 85 238-245.
56. JANUSZ JM, BUCKWALTER BL, YOUNG PA et al.: Vanilloids. 1. Analogs of capsaicin with antinociceptive and antiinflammatory activity. J. Med. Chem. (1993) 36:2595-2604.
57. LIU L, LO Y, CHEN I, SIMON SA: The responses of rat trigeminal ganglion neurons to capsaicin and two nonpungent vanilloid receptor agonists, olvanil and glyceryl nonamide. J. Neurosci. (1997) 17:4101-4111.
58. URBAN L, DRAY A: Capsazepine, a novel capsaicin antagonist, selectively antagonises the effects of capsaicin in the mouse spinal cord in vitro. Neurosci. Lett. (1991) 134:9-11.
59. URBAN L, CAMPBELL EA, PANESAR M et al.: In vivo pharmacology of SDZ 249-665, a novel, non-pungent capsaicin analogue. Pain (2000) 89:65-74.
60. SZALLASI A, BLUMBERG PM: Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper. Neuroscience (1989) 30:515-520.
61. +)-resiniferatoxin. J. Amer. Chem. Soc. (1997) 119 12976-12977.
62. LAZZERI M, BENEFORTI P, TURINI D: Urodynamic effects of intravesical resiniferatoxin in humans: preliminary results in stable and unstable detrusor. J. Urol. (1997) 158:2093-2096.
63. CHANCELLOR MB: Discussion: resiniferatoxin-preliminary data. Urology (2000) 55(5A Suppl.):65.
64. GIANNANTONI A, DI STASI SM, STEPHEN RL et al.: Intravesical resiniferatoxin versus botulinum-A toxin injections for neurogenic detrusor overactivity: a prospective randomized study. J. Urol. (2004) 172:240-243.
65. KIM JH, RIVAS DA, SHENOT PJ et al.: Intravesical resiniferatoxin for refractory detrusor hyperreflexia: a multicenter, blinded, randomized, placebo-controlled trial. J. Spinal Cord Med. (2003) 26:358-363.
66. HUA XY, CHEN P, HWANG J et al.: Antinociception induced by civamide, an orally active capsaicin analogue. Pain (1997) 71 313-322.
67. DIAMOND S, FREITAG F, PHILLIPS SB et al.: Intranasal civamide for the acute treatment of migraine headache. Cephalalgia (2000) 20:597-602.
68. SAPER JR, KLAPPER J, MATHEW NT et al.: Intranasal civamide for the treatment of episodic cluster headaches. Arch. Neurol. (2002) 59:990-994.
69. BOURNE N, BERNSTEIN DI, STANBERRY LR: Civamide (cis capsaicin) for treatment of primary or recurrent experimental genital herpes. Antimicrob. Agents Chemother. (1999) 43:2685-2688.
70. ARNAR DO, CAI JJ, LEE HC et al.: Electrophysiologic effects of civamide (zucapsaicin) on canine cardiac tissue in vivo and in vitro. J. Cardiovasc. Pharmacol. (1998) 32:875-883.
71. CHENG YP, WANG YH, CHENG LP et al.: Electrophysiologic effects of capsaicin on pacemaker cells in sinoatrial nodes of rabbits. Acta Pharmacol. Sin. (2003) 24:826-830.
72. ROBBINS WR, STAATS PS, LEVINE J et al.: Treatment of intractable pain with topical large-dose capsaicin: preliminary report. Anesth. Analg. (1998) 86:579-583.
73. MALMBERG AB, MIZISIN AP, CALCUTT NA et al.: Reduced heat sensitivity and epidermal nerve fiber immunostaining following single applications of a high-concentration capsaicin patch. Pain (2004) 111:360-367.
74. MALAN TP, TUCHMAN M, MOLLEN M et al.: A single one-hour application of high-concentration trans-capsaicin patches leads to four weeks of pain relief in postherpetic neuralgia (PHN) patients. World Congress of Anesthesiology Paris, France (2004).
75. LEE JJ, SHIM HJ, KIM SH et al.: Pharmacokinetics of a non-narcotic analgesic, DA-5018, in rats. Biopharm. Drug Dispos. (1998) 19:101-108.
76. KIM DH, AHN BO, KIM SH et al.: Antipruritic effect of DA-5018, a capsaicin derivative, in mice. Arch Pharm Res. (1999) 22:549-653.
77. CHA BJ, LEE ED, KIM WB et al.: Enhanced skin permeation of a new capsaicin derivative (DA-5018) from a binary vehicle system composed of isopropyl myristate and ethoxydiglycol. Arch. Pharm. Res. (2001) 24:224-228.
78. KARAI L, BROWN DC, MANNES AJ et al.: Deletion of vanilloid receptor 1-expressing primary afferent neurons for pain control. J. Clin. Invest. (2004) 113:1344-1352.
79. VESALUOMA M, MULLER L, GALLAR J et al.: Effects of oleoresin capsicum pepper spray on human corneal morphology and sensitivity. Invest Ophthalmol. Vis. Sci. (2000) 41 2138-2147.