TY - JOUR
T1 - Receptor binding profile of neuropeptide γ and its fragments
T2 - Comparison with the nonmammalian peptides carassin and ranakinin at three mammalian tachykinin receptors
AU - Badgery-Parker, Tim
AU - Lovas, Sandor
AU - Conlon, J. Michael
AU - Burcher, Elizabeth
PY - 1993
Y1 - 1993
N2 - The tachykinin binding site preferences of neuropeptide γ (NPγ), its C-terminal fragments AcNPγ(3-21), AcNPγ(5-21), AcNPγ(7-21), and AcNPγ(9-21), other mammalian tachykinins, and the nonmammalian tachykinins ranakinin and carassin were examined in membrane binding competition studies. [125I]-Bolton-Hunter [Sar9,Met(O2)11]SP (BHSarSP), [125I]-neurokinin A (INKA) and [125I]-Bolton-Hunter scyliorhinin II (BHScyII) were used to investigate NK-1, NK-2, and NK-3 sites, in rat submandibular gland, gastric fundus, and brain, respectively. Elongation of the neurokinin A molecule does not appear to influence binding to rat tachykinin NK-1 and NK-2 binding sites. Ranakinin has affinity for the NK-1 and NK-2 site similar to that of substance P and neurokinin A, respectively, but has low affinity for the NK-3 site. Despite its structural similarities to neuropeptide γ, carassin has only moderate affinity for rat tachykinin binding sites. Possession of an acidic residue at position 4 appears critical for binding to rat NK-2 sites.
AB - The tachykinin binding site preferences of neuropeptide γ (NPγ), its C-terminal fragments AcNPγ(3-21), AcNPγ(5-21), AcNPγ(7-21), and AcNPγ(9-21), other mammalian tachykinins, and the nonmammalian tachykinins ranakinin and carassin were examined in membrane binding competition studies. [125I]-Bolton-Hunter [Sar9,Met(O2)11]SP (BHSarSP), [125I]-neurokinin A (INKA) and [125I]-Bolton-Hunter scyliorhinin II (BHScyII) were used to investigate NK-1, NK-2, and NK-3 sites, in rat submandibular gland, gastric fundus, and brain, respectively. Elongation of the neurokinin A molecule does not appear to influence binding to rat tachykinin NK-1 and NK-2 binding sites. Ranakinin has affinity for the NK-1 and NK-2 site similar to that of substance P and neurokinin A, respectively, but has low affinity for the NK-3 site. Despite its structural similarities to neuropeptide γ, carassin has only moderate affinity for rat tachykinin binding sites. Possession of an acidic residue at position 4 appears critical for binding to rat NK-2 sites.
KW - Carassin
KW - Neurokinin A
KW - Neuropeptide γ
KW - NK-2 receptors
KW - Radioligand binding
KW - Ranakinin
KW - Structure-activity
KW - Tachykinin receptor
UR - http://www.scopus.com/inward/record.url?scp=0027249462&partnerID=8YFLogxK
U2 - 10.1016/0196-9781(93)90112-T
DO - 10.1016/0196-9781(93)90112-T
M3 - Article
C2 - 8234024
AN - SCOPUS:0027249462
SN - 0196-9781
VL - 14
SP - 771
EP - 775
JO - Peptides
JF - Peptides
IS - 4
ER -