A cyclic analogue selective for the NKB specific binding site on rat brain synaptosomes

The cyclic analogue of NKB, [Cys 2, Cys 5]NKB is as active as SP and NKB in the guinea-pig ileum bioassay. Furthermore, [Cys 2,Cys 5]NKB is a selective substrate for the [ 3H]NKB specific binding site on rat cortical synaptosomes. Its binding potencies for [ 3H]NKB and 125I-BHSP binding sites, IC 50...

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Veröffentlicht in:	European journal of pharmacology 1986-09, Vol.128 (3), p.283-285
Hauptverfasser:	Lavielle, Solange, Chassaing, Gérard, Besseyre, Janine, Marquet, Andrée, Bergström, Lena, Beaujouan, Jean-Claude, Torrens, Yvette, Glowinski, Jacques
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Applied sciences Biological and medical sciences brain Brain Chemistry - drug effects Brain synaptosomes Conformation restriction Exact sciences and technology Guinea Pigs Guinea-pig ileum, Rat In Vitro Techniques Iodine Radioisotopes Medical sciences Miscellaneous Muscle, Smooth - drug effects neurokinin B Neurokinin B - analogs & derivatives Neuropharmacology Other techniques and industries Peptides, Cyclic - chemical synthesis Peptides, Cyclic - pharmacology Pharmacology. Drug treatments rats Substance P - pharmacology synaptosomes Synaptosomes - metabolism Tachykinin
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Zusammenfassung:	The cyclic analogue of NKB, [Cys 2, Cys 5]NKB is as active as SP and NKB in the guinea-pig ileum bioassay. Furthermore, [Cys 2,Cys 5]NKB is a selective substrate for the [ 3H]NKB specific binding site on rat cortical synaptosomes. Its binding potencies for [ 3H]NKB and 125I-BHSP binding sites, IC 50 = 5.2 nM and 3.4 μM respectively were close to those observed for NKB.
ISSN:	0014-2999 1879-0712
DOI:	10.1016/0014-2999(86)90779-X