PMID- 1409010 OWN - NLM STAT- MEDLINE DCOM- 19921026 LR - 20190818 IS - 0196-9781 (Print) IS - 0196-9781 (Linking) VI - 13 IP - 2 DP - 1992 Mar-Apr TI - Pharmacological characterization of angiotensin II binding sites in the canine pancreas. PG - 313-8 AB - High affinity 125I-angiotensin II (Ang II) binding sites were characterized in the canine pancreas. Total binding increased with protein concentration and equilibrium was reached within 60-90 min at 22 degrees C. Specific binding was saturable and averaged 70% of total. Scatchard analysis of binding yielded a KD of 0.48 +/- 0.18 nM with a Bmax of 32.8 +/- 6.5 fmol/mg protein (mean +/- SEM, n = 6). The addition of the reducing agent dithiothreitol increased specific binding two-fold. The rank order of displacement of 125I-Ang II binding by native angiotensin peptides was Ang II greater than or equal to Ang III greater than AngI greater than Ang(1-7) much greater than Ang(1-6). The use of the specific Ang II antagonists CGP 42112A, PD 123177, and DuP 753 revealed that the pancreas expresses two receptor subtypes. The majority of Ang II binding sites in the pancreas could be classified as type 2 (AT2), although type 1 (AT1) sites were also detected. In vitro autoradiography revealed binding sites localized over islet cells, acinar and duct cells, as well as the pancreatic vasculature. In addition, the autoradiographic studies confirmed the predominance of the AT2 receptor subtype throughout the pancreas. FAU - Chappell, M C AU - Chappell MC AD - Department of Brain and Vascular Research, Cleveland Clinic Foundation, OH 44195-5286. FAU - Diz, D I AU - Diz DI FAU - Jacobsen, D W AU - Jacobsen DW LA - eng GR - HL-38535/HL/NHLBI NIH HHS/United States GR - HL-6835/HL/NHLBI NIH HHS/United States PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Research Support, U.S. Gov't, P.H.S. PL - United States TA - Peptides JT - Peptides JID - 8008690 RN - 0 (Angiotensin Receptor Antagonists) RN - 0 (Biphenyl Compounds) RN - 0 (Imidazoles) RN - 0 (Oligopeptides) RN - 0 (Pyridines) RN - 0 (Receptors, Angiotensin) RN - 0 (Tetrazoles) RN - 11128-99-7 (Angiotensin II) RN - 114785-12-5 (PD 123177) RN - 127060-75-7 (CGP 42112A) RN - 9041-90-1 (Angiotensin I) RN - JMS50MPO89 (Losartan) RN - T8ID5YZU6Y (Dithiothreitol) SB - IM MH - Angiotensin I/antagonists & inhibitors/chemistry/drug effects MH - Angiotensin II/antagonists & inhibitors/*chemistry/drug effects MH - Angiotensin Receptor Antagonists MH - Animals MH - Binding, Competitive MH - Biphenyl Compounds/pharmacology MH - Dithiothreitol/pharmacology MH - Dogs MH - Imidazoles/pharmacology MH - Kinetics MH - Losartan MH - Male MH - Oligopeptides/pharmacology MH - Pancreas/*chemistry/drug effects/metabolism MH - Pyridines/pharmacology MH - Receptors, Angiotensin/*chemistry/classification/drug effects MH - Tetrazoles/pharmacology EDAT- 1992/03/01 00:00 MHDA- 1992/03/01 00:01 CRDT- 1992/03/01 00:00 PHST- 1992/03/01 00:00 [pubmed] PHST- 1992/03/01 00:01 [medline] PHST- 1992/03/01 00:00 [entrez] AID - 0196-9781(92)90114-I [pii] AID - 10.1016/0196-9781(92)90114-i [doi] PST - ppublish SO - Peptides. 1992 Mar-Apr;13(2):313-8. doi: 10.1016/0196-9781(92)90114-i.