NDLI: Pharmacological profile of the novel mammalian tachykinin, hemokinin 1

Content Provider	PubMed Central
Author	Bellucci, Francesca Carini, Francesca Catalani, Claudio Cucchi, Paola Alessandro, Lecci Meini, Stefania Riccardo, Patacchini Laura, Quartara Ricci, Renzo Tramontana, Manuela Giuliani, Sandro Maggi, Carlo Alberto
Copyright Year	2002
Abstract	The effects of the novel mammalian tachykinin, hemokinin 1 (HEK-1), have been investigated by radioligand binding and functional in vitro and in vivo experiments. Similar to SP (Ki =0.13 nM), HEK-1 inhibited in a concentration-dependent manner and with high affinity [3H]-substance P (SP) binding to human NK1 receptor (Ki =0.175 nM) while its affinity for [125I]-neurokinin A (NKA) binding at human NK2 receptor was markedly lower (Ki =560 nM). In isolated bioassays HEK-1 was a full agonist at tachykinin NK1, NK2 and NK3 receptors. In the rat urinary bladder (RUB) HEK-1 was about 3 fold less potent than SP. In the rabbit pulmonary artery (RPA) HEK-1 and in the guinea-pig ileum (GPI), HEK-1 was about 500 fold less potent than NKA and NKB, respectively. The responses to HEK-1 were antagonized by GR 82334 in RUB (pKB=5.6±0.07), by nepadutant in RPA (pKB=8.6±0.04) and by SR 142801 in GPI (pKB=9.0±0.2) with apparent affinities comparable to that measured against tachykinin NK1, NK2 and NK3 receptor-selective agonists, respectively. Intravenous HEK-1 produced dose-related decrease of blood pressure in anaesthetized guinea-pigs (ED50=0.1 nmol kg−1) and salivary secretion in anaesthetized rats (ED50=6 nmol kg−1) with potencies similar to that of SP. All these effects were blocked by the selective tachykinin NK1 receptor antagonist, SR 140333. We conclude that HEK-1 is a full agonist at tachykinin NK1, NK2 and NK3 receptors, possesses a remarkable selectivity for NK1 as compared to NK2 or NK3 receptors and acts in vivo experiments with potency similar to that of SP.
Related Links	http://dx.doi.org/10.1038/sj.bjp.0704443
Ending Page	274
Page Count	9
Starting Page	266
File Format	PDF
ISSN	00071188
Journal	British Journal of Pharmacology
Issue Number	1
Volume Number	135
Language	English
Publisher Date	2002-01-01
Access Restriction	Open
Subject Keyword	Pharmacology Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Pharmacology

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