Synthesis, biological activity, and conformational analysis of [pGlu6, N-MePhe8, Aib9] substance P (6-11): A selective agonist for the NK-3 receptor

Biopolymers ◽  
1993 ◽  
Vol 33 (6) ◽  
pp. 915-926 ◽  
Author(s):  
M. Tallon ◽  
D. Ron ◽  
D. Halle ◽  
P. Amodeo ◽  
G. Saviano ◽  
...  
1988 ◽  
Vol 31 (2) ◽  
pp. 416-421 ◽  
Author(s):  
Ariel Ewenson ◽  
Ralph Laufen ◽  
Michael Chorev ◽  
Zvi Selinger ◽  
Chaim Gilon

Biochemistry ◽  
1998 ◽  
Vol 37 (36) ◽  
pp. 12465-12476 ◽  
Author(s):  
Y. Larry Zhang ◽  
Hanumantha Rao Marepalli ◽  
Hui-fen Lu ◽  
Jeffrey M. Becker ◽  
Fred Naider

1999 ◽  
Vol 276 (4) ◽  
pp. G875-G885 ◽  
Author(s):  
N. A. Deshpande ◽  
T. J. McDonald ◽  
M. A. Cook

Isolated myenteric ganglion networks were used in a perifusion protocol to characterize the response of interstitial adenosine levels to changes in prevailing[Formula: see text]. The biological activity of such adenosine was assessed using inhibition of release of substance P (SP) as a functional measure of adenosine activity, and the effect of altered O2 tension on both spontaneous and elevated extracellular K+ concentration-evoked SP release from networks was determined over a range of[Formula: see text] values from hypoxic ([Formula: see text] = 54 mmHg) to hyperoxic ([Formula: see text] = 566 mmHg). Release of SP was found to be sensitive to [Formula: see text], and a linear graded relationship was obtained. Perifusion in the additional presence of the adenosine A1-receptor-selective antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) revealed considerable adenosinergic inhibition with an inverse exponential relationship and hyperoxic threshold [Formula: see text]. Disinhibition of evoked SP release by DPCPX in the absence of TTX was double that observed in its presence, indicating a neural source for some of the adenosine released during hypoxia. A postulated neuroprotective role for adenosine is consistent with the demonstrated relationship between interstitial adenosine and prevailing O2 tension.


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