Pharmacological profile of hemokinin 1: a novel member of the tachykinin family

Recently, the cloning of a novel preprotachykinin gene (PPT-C) has been reported. This gene codes for a novel peptide named hemokinin 1 (HK-1). In contrast with the known tachykinins, which are exclusively expressed in neuronal tissues, PPT-C mRNA was detected primarily in hematopoietic cells. In th...

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Bibliographic Details
Published in:Life sciences (1973) 2002-06, Vol.71 (4), p.363-370
Main Authors: Camarda, V., Rizzi, A., Calo, G., Guerrini, R., Salvadori, S., Regoli, D.
Format: Article
Language:English
Subjects:
Animals
Bioassay
Hemokinin 1
Jugular Veins - drug effects
Jugular Veins - metabolism
Male
NK 1 receptor
Portal Vein - drug effects
Portal Vein - metabolism
Protein Precursors - pharmacology
Pulmonary Artery - drug effects
Pulmonary Artery - metabolism
Rabbits
Rats
Receptors, Neurokinin-1 - metabolism
Receptors, Neurokinin-2 - metabolism
Receptors, Neurokinin-3 - metabolism
Tachykinins
Tachykinins - pharmacology
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Summary:Recently, the cloning of a novel preprotachykinin gene (PPT-C) has been reported. This gene codes for a novel peptide named hemokinin 1 (HK-1). In contrast with the known tachykinins, which are exclusively expressed in neuronal tissues, PPT-C mRNA was detected primarily in hematopoietic cells. In this study, we pharmacologically characterised the effects of HK-1 using three tachykinin monoreceptor systems, namely the rabbit jugular vein (rbJV) for NK 1, the rabbit pulmonary artery (rbPA) for NK 2, and rat portal vein (rPV) for NK 3 receptors. In all these preparations substance P (SP), neurokinin A (NKA) and neurokinin B (NKB) elicited concentration dependent contractions showing similar maximal effects and the following rank order of potency: SP > NKA = NKB in the rbJV, NKA > NKB ≫ SP in the rbPA, and NKB > NKA > SP in the rPV. In those vessels HK-1 behaved as a full agonist displaying potencies similar (rbPA and rPV) or slightly higher (rbJV) than those of SP. In the rbJV, SR 140333, a selective NK 1 receptor antagonist, antagonised the effects of HK-1 and SP with similar high potencies (pK B 9.3 and 9.5, respectively). Similar results were obtained with the pseudopeptide NK 1 antagonist, MEN 11467 (pK B 8.8 and 8.6, respectively). Taken together, these data indicate that HK-1 behaves as a NK 1 preferring receptor agonist.
ISSN:0024-3205
1879-0631
DOI:10.1016/S0024-3205(02)01682-X