Dimeric substance P analogue shows a highly potent activity of the in vivo salivary secretion in the rat.
We have synthesized a dimeric analogue of substance P (SP) COOH-terminal nonapeptide fragment (D-SP-(3-11] and examined the in vivo and in vitro biological activities in the submaxillary gland of the rat. The dimer elicited an enhanced biological response as compared with receptor binding, showing 2.4-fold more potent receptor affinity than its monomer and 75-fold more potent in vivo salivary secretion activity.
Higuchi
Y
Y
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Fukuoka University, Japan.
Takano
Y
Y
Shimazaki
H
H
Shimohigashi
Y
Y
Kodama
H
H
Matsumoto
H
H
Sakaguchi
K
K
Nonaka
S
S
Saito
R
R
Waki
M
M
D000818:Animals; D007457:Iodine Radioisotopes; D008297:Male; D010446:Peptide Fragments / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D012472:Salivation / Q000187:drug effects*; D013363:Submandibular Gland / Q000187:drug effects / Q000378:metabolism; D013373:Substance P / Q000494:pharmacology*
D007457:Iodine Radioisotopes; D010446:Peptide Fragments; D013373:Substance P; C038417:substance P (3-11)