PMID- 9570477
OWN - NLM
STAT- MEDLINE
DCOM- 19980609
LR  - 20190624
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 343
IP  - 2-3
DP  - 1998 Feb 19
TI  - Identification of a unique ligand which has high affinity for all four bombesin 
      receptor subtypes.
PG  - 275-87
AB  - Four subtypes of bombesin receptors are identified (gastrin-releasing peptide 
      receptor, neuromedin B receptor, the orphan receptor bombesin receptor subtype 3 
      (BB3 or BRS-3) and bombesin receptor subtype 4 (BB4)), however, only the 
      pharmacology of the gastrin-releasing peptide receptor has been well studied. 
      This lack of data is due in part to the absence of a general ligand. Recently we 
      have discovered a ligand, 125I-[D-Tyr6,betaAla11,Phe13,Nle14]bombesin-(6-1 4) 
      that binds to BRS-3 receptors. In this study we investigate its ability to 
      interact with all four bombesin receptor subtypes. In rat pancreatic acini 
      containing only gastrin-releasing peptide receptor and in BB4 transfected BALB 
      cells, this ligand and 125I-[Tyr4]bombesin, the conventional gastrin-releasing 
      peptide receptor ligand, gave similar results for receptor number, affinity for 
      bombesin and affinity for the unlabeled ligand. In neuromedin B receptor 
      transfected BALB cells, this ligand and 125I-[D-Tyr0]neuromedin B, the generally 
      used neuromedin B receptor ligand, gave similar results for receptor number, 
      neuromedin B affinity or the unlabeled ligand affinity. Lastly, in BRS-3 
      transfected BALB cells, only this ligand had high affinity. For all four bombesin 
      receptors this ligand had an affinity of 1-8 nM and was equal or greater in 
      affinity than any other specific ligands for any receptor. The unlabeled ligand 
      is specific for gastrin-releasing peptide receptors on rat pancreatic acini and 
      did not inhibit binding of 125I-cholecystokinin octapeptide (125I-CCK-8), 
      125I-vasoactive intestinal peptide (125I-VIP) or 125I-endothelin to their 
      receptors. The unlabeled ligand was an agonist only at the gastrin-releasing 
      peptide receptor in rat acini and did not interact with CCK(A) receptors or 
      muscarinic M3 acetylcholine receptors to increase [3H]inositol phosphates. These 
      results demonstrate 125I-[D-Tyr6,betaAla11,Phe13,Nle14]bombesin-(6-1 4) is a 
      unique ligand with high affinity for all subtypes of bombesin receptors. Because 
      of the specificity for bombesin receptors, this ligand will be a valuable 
      addition for such pharmacological studies as screening for bombesin receptor 
      agonists or antagonists and, in particular, for investigating BRS-3 cell biology, 
      a receptor for which no ligand currently exists.
FAU - Pradhan, T K
AU  - Pradhan TK
AD  - Digestive Diseases Branch, National Institute of Diabetes and Digestive and 
      Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-1804, USA.
FAU - Katsuno, T
AU  - Katsuno T
FAU - Taylor, J E
AU  - Taylor JE
FAU - Kim, S H
AU  - Kim SH
FAU - Ryan, R R
AU  - Ryan RR
FAU - Mantey, S A
AU  - Mantey SA
FAU - Donohue, P J
AU  - Donohue PJ
FAU - Weber, H C
AU  - Weber HC
FAU - Sainz, E
AU  - Sainz E
FAU - Battey, J F
AU  - Battey JF
FAU - Coy, D H
AU  - Coy DH
FAU - Jensen, R T
AU  - Jensen RT
LA  - eng
PT  - Journal Article
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Iodine Radioisotopes)
RN  - 0 (Ligands)
RN  - 0 (Receptors, Bombesin)
RN  - PX9AZU7QPK (Bombesin)
SB  - IM
MH  - 3T3 Cells
MH  - Animals
MH  - Bombesin/analogs & derivatives/*metabolism
MH  - CHO Cells
MH  - Cricetinae
MH  - Iodine Radioisotopes
MH  - Ligands
MH  - Male
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Pancreas/cytology/metabolism
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Receptors, Bombesin/classification/*metabolism
EDAT- 1998/05/07 00:00
MHDA- 1998/05/07 00:01
CRDT- 1998/05/07 00:00
PHST- 1998/05/07 00:00 [pubmed]
PHST- 1998/05/07 00:01 [medline]
PHST- 1998/05/07 00:00 [entrez]
AID - S0014-2999(97)01527-6 [pii]
AID - 10.1016/s0014-2999(97)01527-6 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 1998 Feb 19;343(2-3):275-87. doi: 10.1016/s0014-2999(97)01527-6.