PMID- 17920583
OWN - NLM
STAT- MEDLINE
DCOM- 20080205
LR  - 20131121
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 577
IP  - 1-3
DP  - 2007 Dec 22
TI  - Senktide-induced gerbil foot tapping behaviour is blocked by selective tachykinin 
      NK1 and NK3 receptor antagonists.
PG  - 78-86
AB  - Intracerebroventricular (i.c.v.) administration of tachykinin NK(1) receptor 
      agonists induces tapping of the hind legs in gerbils, so-called gerbil foot 
      tapping, which is thought to reflect a fear-related response. The aim of the 
      present study was to examine how ligands selective for NK(1), NK(2) and NK(3) 
      receptors affect the gerbil foot tap response. Agonists selective for NK receptor 
      subtypes were administered i.c.v. and the gerbil foot tap response was monitored. 
      The effect of systemically administered antagonists was also studied. The 
      interaction of ligands with gerbil NK(1) receptors was evaluated using 
      autoradiography on gerbil brain slices with [(3)H]-Sar,Met(O(2))-substance P or 
      [(3)H]GR205171 as radioligand. The effects of ligands on NK(1) and NK(3) 
      receptor-mediated increases in intracellular calcium in vitro were studied in 
      Chinese hamster ovary cells expressing the cloned gerbil receptors. The selective 
      NK(1) receptor agonist ASMSP and the selective NK(3) receptor agonist senktide 
      induced dose-dependent increases in gerbil foot tapping with similar potency. The 
      maximal effect of senktide was approximately 40% of the maximal response evoked 
      by ASMSP. The effects of ASMSP and senktide were blocked by administration of the 
      selective NK(1) receptor antagonist CP99,994 (10 micromol/kg s.c.). The effects 
      of senktide, but not ASMSP, were blocked by administration of the selective NK(3) 
      receptor antagonist SB223412 (50 micromol/kg i.p.). Senktide did not displace 
      NK(1) receptor radioligand binding and was >1000-fold less potent than ASMSP at 
      activating gerbil NK(1) receptors. The selective NK(3) receptor agonist senktide 
      evokes fear-related gerbil foot tapping, an effect which probably involves 
      indirect enhancement of NK(1) receptor signalling.
FAU - Sundqvist, Monika
AU  - Sundqvist M
AD  - AstraZeneca R&D, Molndal, Sweden.
FAU - Kristensson, Elin
AU  - Kristensson E
FAU - Adolfsson, Rebecka
AU  - Adolfsson R
FAU - Leffler, Agnes
AU  - Leffler A
FAU - Ahlstedt, Ingela
AU  - Ahlstedt I
FAU - Engberg, Susanna
AU  - Engberg S
FAU - Drmota, Tomas
AU  - Drmota T
FAU - Sigfridsson, Kalle
AU  - Sigfridsson K
FAU - Jussila, Rainer
AU  - Jussila R
FAU - de Verdier, Jennie
AU  - de Verdier J
FAU - Noven, Anna
AU  - Noven A
FAU - Johansson, Anders
AU  - Johansson A
FAU - Pahlman, Ingrid
AU  - Pahlman I
FAU - von Mentzer, Bengt
AU  - von Mentzer B
FAU - Lindstrom, Erik
AU  - Lindstrom E
LA  - eng
PT  - Journal Article
DEP - 20070911
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Neurokinin-1 Receptor Antagonists)
RN  - 0 (Peptide Fragments)
RN  - 0 (Piperidines)
RN  - 0 (Quinolines)
RN  - 0 (Receptors, Neurokinin-2)
RN  - 0 (Receptors, Neurokinin-3)
RN  - 0 (substance P(4-11), beta Ala(4)-Ser(9)-Met(O2)(11)-)
RN  - 106128-89-6 (senktide)
RN  - 133156-06-6 (GR 73632)
RN  - 136548-07-7 (neurokinin A (3-10), lysyl(3)-glycyl(8)-R-lactam-leucine(9)-)
RN  - 136982-36-0 (3-(2-methoxybenzylamino)-2-phenylpiperidine)
RN  - 174636-32-9 (SB 223412)
RN  - 33507-63-0 (Substance P)
RN  - 86933-74-6 (Neurokinin A)
RN  - SY7Q814VUP (Calcium)
SB  - IM
MH  - Animals
MH  - Autoradiography
MH  - Behavior, Animal/*drug effects
MH  - Brain/metabolism
MH  - CHO Cells
MH  - Calcium/metabolism
MH  - Cloning, Molecular
MH  - Cricetinae
MH  - Cricetulus
MH  - Dose-Response Relationship, Drug
MH  - Foot
MH  - Gerbillinae
MH  - Injections, Intraventricular
MH  - Male
MH  - Neurokinin A/analogs & derivatives/pharmacology
MH  - *Neurokinin-1 Receptor Antagonists
MH  - Peptide Fragments/*antagonists & inhibitors/*pharmacology
MH  - Piperidines/pharmacology
MH  - Quinolines/pharmacology
MH  - Receptors, Neurokinin-2/antagonists & inhibitors
MH  - Receptors, Neurokinin-3/*antagonists & inhibitors
MH  - Substance P/*analogs & derivatives/antagonists & inhibitors/pharmacology
EDAT- 2007/10/09 09:00
MHDA- 2008/02/06 09:00
CRDT- 2007/10/09 09:00
PHST- 2007/05/11 00:00 [received]
PHST- 2007/07/31 00:00 [revised]
PHST- 2007/08/28 00:00 [accepted]
PHST- 2007/10/09 09:00 [pubmed]
PHST- 2008/02/06 09:00 [medline]
PHST- 2007/10/09 09:00 [entrez]
AID - S0014-2999(07)00990-9 [pii]
AID - 10.1016/j.ejphar.2007.08.042 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2007 Dec 22;577(1-3):78-86. doi: 10.1016/j.ejphar.2007.08.042. 
      Epub 2007 Sep 11.