PMID- 11600206
OWN - NLM
STAT- MEDLINE
DCOM- 20020115
LR  - 20190901
IS  - 0167-0115 (Print)
IS  - 0167-0115 (Linking)
VI  - 102
IP  - 1
DP  - 2001 Oct 15
TI  - Characterisation of a new chimeric ligand for galanin receptors: 
      galanin(1-13)-[D-Trp(32)]-neuropeptide Y(25-36)amide.
PG  - 15-9
AB  - In this work, we studied a novel chimeric peptide, M242, 
      galanin(1-13)-[D-Trp(32)]-neuropeptide Y(25-36)amide, and examined its properties 
      in comparison with its parent peptide, M32, galanin(1-13)-neuropeptide 
      Y(25-36)amide, a previously known high-affinity ligand for galanin receptors, and 
      galanin itself. Binding assays performed in Bowes cells known to express human 
      galanin receptor type 1 (hGalR1) and in Chinese hamster ovary cells 
      overexpressing human galanin receptor type 2 (hGalR2) revealed that all three 
      ligands had comparable affinities: at hGalR1<1 nM and at hGalR2<10 nM. However, 
      in rat hippocampal membranes M242 had a 24-fold lower affinity than galanin (9.4 
      vs. 0.4 nM) and 134-fold lower affinity than M32 (9.4 vs. 0.07 nM). In the same 
      tissue, we also examined the effects of these peptides on adenylate cyclase 
      activity. M32 showed a weak antagonistic behaviour but M242 acted as a potent 
      biphasic regulator of adenylate cyclase. In conclusion, we present and 
      characterise a new peptide M242, which could be a useful tool in studies of 
      galaninergic signalling.
FAU - Saar, K
AU  - Saar K
AD  - Department of Neurochemistry and Neurotoxicology, SvanteArrhenius vag 21A, 
      Stockholm University, S-10691, Stockholm, Sweden.
FAU - Mahlapuu, R
AU  - Mahlapuu R
FAU - Laidmae, E
AU  - Laidmae E
FAU - Valkna, A
AU  - Valkna A
FAU - Kahl, U
AU  - Kahl U
FAU - Karelson, E
AU  - Karelson E
FAU - Langel U
AU  - Langel U
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - Regul Pept
JT  - Regulatory peptides
JID - 8100479
RN  - 0 (Ligands)
RN  - 0 (Neuropeptide Y)
RN  - 0 (Peptide Fragments)
RN  - 0 (Receptor, Galanin, Type 1)
RN  - 0 (Receptor, Galanin, Type 2)
RN  - 0 (Receptors, Galanin)
RN  - 0 (Receptors, Neuropeptide)
RN  - 0 (Recombinant Fusion Proteins)
RN  - 0 (galanin-NPY chimeric peptide M32)
RN  - 88813-36-9 (Galanin)
RN  - EC 4.6.1.1 (Adenylyl Cyclases)
SB  - IM
MH  - Adenylyl Cyclases/metabolism
MH  - Animals
MH  - CHO Cells
MH  - Cricetinae
MH  - Galanin/antagonists & inhibitors/*chemistry/metabolism
MH  - Hippocampus/metabolism
MH  - Humans
MH  - Ligands
MH  - Neuropeptide Y/*analogs & derivatives/antagonists & 
      inhibitors/*chemistry/metabolism
MH  - Peptide Fragments/antagonists & inhibitors/*chemistry/metabolism
MH  - Protein Binding
MH  - Rats
MH  - Receptor, Galanin, Type 1
MH  - Receptor, Galanin, Type 2
MH  - Receptors, Galanin
MH  - Receptors, Neuropeptide/*metabolism
MH  - Recombinant Fusion Proteins/chemistry/metabolism
EDAT- 2001/10/16 10:00
MHDA- 2002/01/16 10:01
CRDT- 2001/10/16 10:00
PHST- 2001/10/16 10:00 [pubmed]
PHST- 2002/01/16 10:01 [medline]
PHST- 2001/10/16 10:00 [entrez]
AID - S0167011501002981 [pii]
AID - 10.1016/s0167-0115(01)00298-1 [doi]
PST - ppublish
SO  - Regul Pept. 2001 Oct 15;102(1):15-9. doi: 10.1016/s0167-0115(01)00298-1.