A potent and selective agonist for NK-2 tachykinin receptor.
Replacement of the glycine in position 8 of the C-terminal heptapeptide NKA(4-10) with beta-alanine give rise to a potent and selective agonist for the NK-2 tachykinin receptor. The affinity of [beta-Ala8]-NKA(4-10) to the NK-2 receptor is enhanced by almost one order of magnitude as compared to NKA(4-10), while affinity decreases at about the same extent at NK-1 and NK-3 receptors, respectively. Synthesis and biological activities of a series of NKA(4-10) analogues systematically replaced in each position with beta-alanine are also reported.
Rovero
P
P
Peptide Synthesis Laboratory, Chemistry Department, Firenze, Italy.
Pestellini
V
V
Patacchini
R
R
Giuliani
S
S
Santicioli
P
P
Maggi
C A
CA
Meli
A
A
Giachetti
A
A
D000409:Alanine; D000818:Animals; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology; D015288:Neurokinin A / Q000031:analogs & derivatives / Q000494:pharmacology*; D010446:Peptide Fragments / Q000494:pharmacology*; D011169:Portal Vein / Q000187:drug effects / Q000502:physiology; D051381:Rats; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000502:physiology*; D018039:Receptors, Tachykinin; D013329:Structure-Activity Relationship; D015320:Tachykinins / Q000502:physiology*; D014649:Vas Deferens / Q000187:drug effects / Q000502:physiology
D010446:Peptide Fragments; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D015320:Tachykinins; D015288:Neurokinin A; C056408:neurokinin A(4-10); D000409:Alanine