- Capsaicin selectively binds to
the to the transient receptor potential cation channel, subfamily V, member 1
(TRPV1). TRPV1 stimulates and then inactivates heat and vanilloid-responsive
nociceptive neurons, namely small myelinated Aδ and unmyelinated C fibers with
no effect on the large myelinated Aβ fibers.(a, b)
a) Caterina MJ, Schumacher
MA, Tominaga M, Rosen TA, Levine JD, Julius D. The capsaicin receptor: a
heat-activated ion channel in the pain pathway. Nature. 1997;389:816–824.
b) Helliwell RJ, McLatchie LM, Clarke M, Winter J, Bevan S, McIntyre P.
Capsaicin sensitivity is associated with the expression of the vanilloid
(capsaicin) receptor (VR1) mRNA in adult rat sensory ganglia. Neurosci Lett.
Fujiuchi, A., Toga, T.
Pharmacologocal effect of capsaicin on rat avoidance behaviours elicited by
sine-wave electrical stimulation of different frequencies by Neurometer.
Journal of Pharmacy and Pharmacology Vol. 60(4):467-71, 2008.
Lee, Y-S., Kho, H-S., Kim,
Y-K., Chung, S-C. Influence of Topical Capsaicin on Facial Sensitivity in
Response to Experimental Pain. Journal of Oral Rehabilitation. Vol
Kiso, T., Nagakura,, Y., Toya,
T., Matsumoto, N., Tamura, S., Ito, H., Okada, M., Yamaguchi, T. Neurometer
measurement of current stimulus threshold in rats. The Journal of
Pharmacology and Experimental Therapeutics, Vol 297(1):352-356, 2001.
Matsumoto M, Inoue M, Hald A,
Yamaguchi A, Ueda H: Characterization of three different sensory fibers by
use of neonatal capsaicin treatment, spinal antagonism and a novel
electrical stimulation-induced paw flexion test. Molecular Pain Vol
Kanai, A., Suzuki, A. Okamoto,
H. Comparison of Cutaneous Anesthetic Effect of 8% Lidocaine Spray with
Lidocaine Patch Using Current Perception Threshold Test. Pain Medicine.
epub. ahead of press, Jan. 2010.
M., Kitagawa, N., Yang, B-X., Totoki, T. Morimoto, M. Quantitative and
fiber-selective evaluation of dose-dependent nerve blockade by intrathecal
lidocaine in rats. The Journal of Pharmacology and Experimental
Therapeutics, Vol 312(3):1132-1137, 2005.
Finkel, J.C., Yang, C.I. Yarvitz, J.L. Patel, K.M. Neuroselective sensory
electrodiagnostic evaluation of 4% liposomal lidocaine. Anesthesia and
Analgesia, Vol 94,:1259-62, 2002.
Tankano, K., Muramori, S. Masaomi, T., Iseki, M., Suzuki,T., Tomono, K.,
Goto, H., Miyazaki, T, Nishitani, A., Watanabe, J. Quantitative
Investigation of the Effect of Sensory Nerve Anesthesia with 9% Lidocaine
Ointment on Healthy Subjects by use of the Neuroselective Current Perception
Threshold. J. Pharm. Sci. Technol., (Yakuzaigaku Jpn.), Vol 62(3):105-112,
Sakura, S., Sumi, M., Kushizaki, H., Saito, Y., Kosaka, Y. Concentration of
Lidocaine Affects Intensity of Sensory Block During Lumbar Epidural
Anesthesia. Anesthesia and Analgesia, Vol 88(1):123-7, 1998.
B., Wallace, M.S., Irving, G. Quantitative Assessment of Differential
Sensory Blockade after Lumbar Epidural Lidocaine. Anesthesia and Analgesia,
Vol 84:1071-1075, 1997.
S., Kopacz, D.J., Carpenter, R.L. Quantitative Assessment of Differential
Sensory Nerve Block after Lidocaine Spinal Anesthesia. Anesthesiology, Vol
top of page
selectively block pain transmission. In humans and rat studies spinal
opiates are observed to have an isolated effect on 5 Hz measures, in contrast
systemic administration effects 5 Hz and 250 Hz measures and in rats at high
doses 2000 Hz measures as well. Examples of publications:
Gustorff, B., Hoerauf, K.H., Lierz, P., Kress, H.G. Comparison of different
quantitative sensory testing methods during remifentanil infusion in
volunteers. British Journal of Anaesthesia. Vol. 91(2):203-8, 2003.
Kiso, T., Nagakura,, Y., Toya, T., Matsumoto, N., Tamura, S., Ito, H.,
Okada, M., Yamaguchi, T. Neurometer measurement of current stimulus
threshold in rats. The Journal of Pharmacology and Experimental
Therapeutics, Vol 297(1):352-356, 2001.
Liu, S.S., Gerancher, J.C., Bainton, B.G., Kopacz, D.J., Carpenter, R.L:
Effects of Electrical Stimulation at Different Frequencies on Perception and
Pain in Human Volunteers: Epidural Versus Intravenous Administration of
Fentanyl. Anesthesia & Analgesia, Vol 82:98-102, 1996.
Paclitaxel and Gabapentin
Matsumoto, ,M. Inoue, M., Hald,
A., Xie, W., Ueda, H. Inhibition of Paclitaxel-Induced A-Fiber
Hypersensitization by Gabapentin. The Journal of Pharmacology and
Experimental Therapeutics Vol. 318(2): 318:735–740, 2006.
- RTX is a
naturally occurring analogue of capsaicin. RTX functions as an ultra potent
capsaicin analogue but also has unique effects such as desensitization without
excitation (Szallasi, A. and Blumberg, P. M.: Vanilloid receptors: new insights
enhance potential as a therapeutic target. Pain, 68: 195, 1996).
- Yokoyama, T., Nozaki,
K., Fujita, O., Nose, H., Inoue, M., Kumon, H. Role of C afferent fibers and
monitoring of intravesical resiniferatoxin therapy for patients with
idiopathic detrusor overactivity. Journal of Urology, Vol
- Gater, L. Tolterodine
Causes Measurable Restoration of Urethral Sensation in Women With Urge
Urinary Incontinence. Paper 56. Presented at the American Urogynecologic
Society 29th Annual Scientific Meeting (AUGS), 2008.