The NK2 receptor antagonist SR48968 inhibits thalamic responses evoked by thermal but not mechanical nociception.
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.
Sanofi Recherche, Montpellier, France.
V
V
Santucci
C
C
Gueudet
X
X
Edmonds-Alt
J C
JC
Brelière
P
P
Soubrié
G
G
Le Fur
D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D006358:Hot Temperature; D008297:Male; D015288:Neurokinin A / Q000037:antagonists & inhibitors*; D010147:Pain Measurement / Q000187:drug effects*; D010812:Physical Stimulation; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors*; D018039:Receptors, Tachykinin; D013237:Stereoisomerism; D013787:Thalamic Nuclei / Q000187:drug effects*
D001549:Benzamides; D010880:Piperidines; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; C073839:SR 48968; D015288:Neurokinin A