[A new tachykinin receptor revealed by substance P analogues in the guinea pig ileum].
[Pro9]SP and septide have been described as selective agonists for the SP receptor (NK-1 type). These two peptides contract with a great efficacy the guinea-pig ileum, but unexpectedly septide was practically devoid of affinity for the NK-1 site labelled by 3H-[Pro9]SP. Like septide, SP analogues like SP-O-CH3, [Apa9-10]SP and [Pro9,10]SP share the same peculiar properties. In addition, the contracting activity of these peptides is not explained by an interaction with NK-2 or NK-3 sites. GR 71,251, a compound which has been described as NK-1 antagonist, was more potent in inhibiting the septide- and the [Apa9-10]SP- than the [Pro9]SP-evoked contracting responses. Altogether, these results suggest that septide, SP-O-CH3, [Apa9-10]SP and [Pro9,10]SP exert their high contracting activity in the guinea-pig ileum by acting on a new type of tachykinin receptor.
Petitet
F
F
Collège de France, I.N.S.E.R.M.-U no. 114, Paris.
Beaujouan
J C
JC
Saffroy
M
M
Torrens
Y
Y
Lavielle
S
S
Chassaing
G
G
Loeuillet
D
D
Glowinski
J
J
D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D004386:Duodenum / Q000378:metabolism; D006168:Guinea Pigs; D007082:Ileum / Q000502:physiology*; D009119:Muscle Contraction / Q000187:drug effects; D010446:Peptide Fragments / Q000378:metabolism / Q000494:pharmacology; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives; D051381:Rats; D017207:Rats, Sprague-Dawley; D018039:Receptors, Tachykinin / Q000032:analysis / Q000502:physiology*; D013373:Substance P / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology
D010446:Peptide Fragments; D018039:Receptors, Tachykinin; C067285:substance P, Pro(9)-; D013373:Substance P; C054725:septide; D011761:Pyrrolidonecarboxylic Acid
Un nouveau récepteur des tachykinines révélé par des analogues de la substance P dans l'iléon de cobaye.