The NK2 receptor antagonist SR48968 inhibits thalamic responses evoked by thermal but not mechanical nociception

• Published in: European journal of pharmacology Vol. 237; no. 1; p. 143
• Main Authors: Santucci, V, Gueudet, C, Edmonds-Alt, X, Brelière, J C, Soubrié, P, Le Fur, G
• Format: Journal Article
• Language: English
• Published: Netherlands 11-06-1993
• Subjects: Animals; Benzamides - pharmacology; Hot Temperature; Male; Neurokinin A - antagonists & inhibitors; Pain Measurement - drug effects; Physical Stimulation; Piperidines - pharmacology; Rats; Rats, Sprague-Dawley; Receptors, Neurotransmitter - antagonists & inhibitors; Receptors, Tachykinin; Stereoisomerism; Thalamic Nuclei - drug effects
• ISSN: 0014-2999
• DOI: 10.1016/0014-2999(93)90104-P

Extracellular recordings were made in the thalamic posterior nuclear group of anesthetized rats to study the effects of SR48968, a non-peptide NK2 receptor antagonist, on the responses evoked by thermal or mechanical nociceptive cutaneous stimulation. SR48968 (0.125-0.5 mg/kg, i.v. route) inhibited the responses to thermal stimulation while being ineffective on mechanically evoked responses in doses up to 2 mg/kg i.v. This effect was stereoselective since SR48965, the (R) enantiomer of SR48968 with a 2000-fold lower affinity for NK2 receptors, did not modify thermally evoked responses at a dose of 1 mg/kg i.v. These results support the notion that NK2 receptors are involved in thermal nociception.