Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
3
|
| pubmed:dateCreated |
1993-10-14
|
| pubmed:abstractText |
Specific binding of [3H]bradykinin (BK) to guinea pig gall bladder (GPGB) membranes was protein dependent, rapid (Kon = 0.067 min-1) with high affinity (Kd = 0.45 +/- 0.02; n = 3), saturable (Bmax = 546 +/- 56 fmol/mg of protein) and showed no cooperativity (nH = 1.19 +/- 0.08). A BK B2 receptor type was indicated by the rank order of potency for inhibition of binding by B2 antagonists, [(D)Arg-[Hyp3,Thi5,(D)Tic7-Oic8]-bradykinin (HOE140) > (D)Arg-[Hyp3,(D)HypE(transpropyl)7-Oic8]-bradykinin (NPC17731) > (D)Arg-[Hyp3,Thi5, (D)Tic7-Tic8]-bradykinin (NPC16731) > (D)Arg-[Hyp3,(D)Phe7]-bradykinin (NPC567)] and agonists (BK = kallidin = Tyr(Me)8-BK > Tyr8-BK,> Hyp4-kallidin) as well as inactivity of the B1 agonist des(Arg9)-BK. Nonhydrolyzable GTP analogs (GTP-gamma-S and guanylyl-5'-imido-diphosphate) produced 80% inhibition of specific binding suggesting receptor coupling to guanine nucleotide-binding proteins. BK increased polyphosphoinositide hydrolysis in chopped GPGB in a concentration-dependent manner (0.01-300 microM; EC50 = 414 +/- 171 nM; n = 3-9 tissues/concentration). HOE140 and NPC16731, inhibited BK-induced polyphosphoinositide hydrolysis but only the latter appeared competitive (pKb 8.09 +/- 0.19, n = 3). U73122, an inhibitor of phospholipase C pathway, also inhibited BK-induced turnover in GPGB (IC50 = 46.9 +/- 17.3 nM). BK produced a concentration-related contraction of isolated strips of GPGB. Indomethacin significantly decreased both the potency and efficacy of BK whereas thiorphan, a neutral endopeptidase inhibitor, and/or captopril, an angiotensin-converting enzyme inhibitor, enhanced potency.(ABSTRACT TRUNCATED AT 250 WORDS)
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Bradykinin,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphatidylinositols,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Bradykinin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurotransmitter,
http://linkedlifedata.com/resource/pubmed/chemical/Tritium
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Sep
|
| pubmed:issn |
0022-3565
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
266
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1291-9
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:8396632-Amino Acid Sequence,
pubmed-meshheading:8396632-Animals,
pubmed-meshheading:8396632-Bradykinin,
pubmed-meshheading:8396632-Drug Stability,
pubmed-meshheading:8396632-Gallbladder,
pubmed-meshheading:8396632-Guinea Pigs,
pubmed-meshheading:8396632-Hydrolysis,
pubmed-meshheading:8396632-Male,
pubmed-meshheading:8396632-Membranes,
pubmed-meshheading:8396632-Molecular Sequence Data,
pubmed-meshheading:8396632-Muscle, Smooth,
pubmed-meshheading:8396632-Muscle Contraction,
pubmed-meshheading:8396632-Peptides,
pubmed-meshheading:8396632-Phosphatidylinositols,
pubmed-meshheading:8396632-Radioligand Assay,
pubmed-meshheading:8396632-Receptors, Bradykinin,
pubmed-meshheading:8396632-Receptors, Neurotransmitter,
pubmed-meshheading:8396632-Tritium
|
| pubmed:year |
1993
|
| pubmed:articleTitle |
Characterization of bradykinin receptors in guinea pig gall bladder.
|
| pubmed:affiliation |
Department of Pharmacology, Zeneca Pharmaceuticals Group, Business Unit of ZENECA Inc., Wilmington, Delaware.
|
| pubmed:publicationType |
Journal Article,
In Vitro
|