PMID- 12047904
OWN - NLM
STAT- MEDLINE
DCOM- 20030123
LR  - 20190901
IS  - 0167-0115 (Print)
IS  - 0167-0115 (Linking)
VI  - 106
IP  - 1-3
DP  - 2002 Jun 15
TI  - Pharmacological comparison of rat and human melanocortin 3 and 4 receptors in 
      vitro.
PG  - 7-12
AB  - The melanocortin 3 and 4 receptors are G-protein-coupled receptors found in the 
      hypothalamus with important role in regulation of the energy balance. In this 
      study, we performed pharmacological comparison of the rat and human melancortin 
      (MC) 3 and MC4 receptors. We transiently expressed the genes for these receptors 
      individually in a mammalian cell line and determined the binding affinities to 
      several MSH peptides. The results showed no major difference between the rat and 
      human MC3 receptors while the rat MC4 receptor had higher affinity to several 
      peptides compared with the human MC4 receptor. NDP-, alpha-, beta-, gamma-MSH, 
      ACTH(1-24), HS014 and MTII had from 5- to 34-fold higher affinity for the rat MC4 
      receptor, while SHU9119, HS024 and HS028 had similar affinity for both the MC4 
      receptors. Pharmacological species difference have earlier been reported for the 
      MC1 and MC5 receptors but this is the first report showing important differences 
      between the rat and human MC4 receptors.
FAU - Schioth, Helgi B
AU  - Schioth HB
AD  - Department of Neuroscience, Biomedical Center, Box 593, 751 24 Uppsala 
      University, Uppsala, Sweden. helgis@bmc.uu.se
FAU - Bouifrouri, Amin A
AU  - Bouifrouri AA
FAU - Rudzish, Richard
AU  - Rudzish R
FAU - Muceniece, Ruta
AU  - Muceniece R
FAU - Watanobe, Hajime
AU  - Watanobe H
FAU - Wikberg, Jarl E S
AU  - Wikberg JE
FAU - Larhammar, Dan
AU  - Larhammar D
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 (Receptor, Melanocortin, Type 3)
RN  - 0 (Receptor, Melanocortin, Type 4)
RN  - 0 (Receptors, Corticotropin)
RN  - 581-05-5 (alpha-MSH)
RN  - E0399OZS9N (Cyclic AMP)
SB  - IM
MH  - Animals
MH  - Binding, Competitive
MH  - COS Cells
MH  - Cyclic AMP/metabolism
MH  - Humans
MH  - Hypothalamus/cytology/drug effects/metabolism
MH  - Ligands
MH  - Protein Binding
MH  - Rats
MH  - Receptor, Melanocortin, Type 3
MH  - Receptor, Melanocortin, Type 4
MH  - Receptors, Corticotropin/genetics/*metabolism
MH  - alpha-MSH/metabolism/pharmacology
EDAT- 2002/06/06 10:00
MHDA- 2003/01/24 04:00
CRDT- 2002/06/06 10:00
PHST- 2002/06/06 10:00 [pubmed]
PHST- 2003/01/24 04:00 [medline]
PHST- 2002/06/06 10:00 [entrez]
AID - S0167011502000253 [pii]
AID - 10.1016/s0167-0115(02)00025-3 [doi]
PST - ppublish
SO  - Regul Pept. 2002 Jun 15;106(1-3):7-12. doi: 10.1016/s0167-0115(02)00025-3.