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ABT-627, an endothelin ETA receptor-selective antagonist, attenuates tactile allodynia in a diabetic rat model of neuropathic pain
- Source :
- European Journal of Pharmacology. 388:29-35
- Publication Year :
- 2000
- Publisher :
- Elsevier BV, 2000.
-
Abstract
- Tactile allodynia, the enhanced perception of pain in response to normally non-painful stimulation, represents a common complication of diabetic neuropathy. The activation of endothelin ET(A) receptors has been implicated in diabetes-induced reductions in peripheral neurovascularization and concomitant endoneurial hypoxia. Endothelin receptor activation has also been shown to alter the peripheral and central processing of nociceptive information. The present study was conducted to evaluate the antinociceptive effects of the novel endothelin ET(A) receptor-selective antagonist, 2R-(4-methoxyphenyl)-4S-(1,3-benzodioxol-5-yl)-1-(N, N-di(n-butyl)aminocarbonyl-methyl)-pyrrolidine-3R-carboxylic acid (ABT-627), in the streptozotocin-induced diabetic rat model of neuropathic pain. Rats were injected with 75 mg/kg streptozotocin (i. p.), and drug effects were assessed 8-12 weeks following streptozotocin treatment to allow for stabilization of blood glucose levels (>/=240 mg/dl) and tactile allodynia thresholds (
- Subjects :
- Endothelin Receptor Antagonists
Male
Pyrrolidines
Analgesic
Pain
Stimulation
Pharmacology
Diabetes Mellitus, Experimental
Rats, Sprague-Dawley
Diabetic Neuropathies
Physical Stimulation
medicine
Animals
Humans
Vasoconstrictor Agents
Pain Measurement
business.industry
Antagonist
Stereoisomerism
Analgesics, Non-Narcotic
Receptor, Endothelin A
Receptor, Endothelin B
Rats
Allodynia
Nociception
Anesthesia
Atrasentan
Neuropathic pain
Morphine
medicine.symptom
Endothelin receptor
business
medicine.drug
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 388
- Database :
- OpenAIRE
- Journal :
- European Journal of Pharmacology
- Accession number :
- edsair.doi.dedup.....3596e935ee55565494c8e63eb85e86cc