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Titolo:
CHARACTERIZATION OF MUSCARINIC RECEPTOR SUBTYPES IN PIG AIRWAYS - RADIOLIGAND BINDING AND NORTHERN BLOTTING STUDIES
Autore:
HADDAD EB; MAK JCW; HISLOP A; HAWORTH SG; BARNES PJ;
Indirizzi:
NATL HEART & LUNG INST,DEPT THORAC MED,DOVEHOUSE ST LONDON SW3 6LY ENGLAND NATL HEART & LUNG INST,DEPT THORAC MED LONDON SW3 6LY ENGLAND INST CHILD HLTH,DIV PHYSIOL & PHARMACOL LONDON SW3 6LY ENGLAND
Titolo Testata:
The American journal of physiology
fascicolo: 6, volume: 266, anno: 1994,
parte:, 1
pagine: 120000642 - 120000648
SICI:
0002-9513(1994)266:6<120000642:COMRSI>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG; SMOOTH-MUSCLE; MESSENGER-RNAS; ACETYLCHOLINE-RECEPTOR; SELECTIVE ANTAGONISTS; PERIPHERAL LUNG; LIGAND-BINDING; HIGH-AFFINITY; RAT LUNG; CELLS;
Keywords:
LUNG; TRACHEA; MUSCARINIC ANTAGONISTS; MESSENGER RIBONUCLEIC ACID;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
38
Recensione:
Indirizzi per estratti:
Citazione:
E.B. Haddad et al., "CHARACTERIZATION OF MUSCARINIC RECEPTOR SUBTYPES IN PIG AIRWAYS - RADIOLIGAND BINDING AND NORTHERN BLOTTING STUDIES", The American journal of physiology, 266(6), 1994, pp. 120000642-120000648

Abstract

This study was under-taken to characterize the muscarinic receptor subtypes present in adult pig peripheral lung and airway smooth muscle. The binding of the nonselective muscarinic antagonist [N-methyl-H-3]scopolamine ([H-3]NMS) to pig airways showed a single class of binding sites with a maximum density of 172 and 450 fmol/mg protein in peripheral lung and airway smooth muscle, respectively. Unlike [H-3]NMS, the M(1)-selective antagonist, [H-3]telenzepine, recognized two populationsof binding sites in peripheral lung. Approximately 14% of total [H-3]telenzepine binding sites displayed high affinity [dissociation constant (K-d) = 0.95 nM], whereas the remaining sites showed low affinity (K-d = 14.2 nM). The high- and the low-affinity [H-3]telenzepine binding sites displayed the pharmacological profile of M(1) and M(2) receptors, respectively. Heterogeneity of pig airways muscarinic receptor wasalso revealed by competitive binding experiments against [H-3]NMS with the M(2)-selective antagonist methoctramine. This compound recognized 70 and 90% of total receptors with high affinity in airway smooth muscle (K-i = 4.44 nM) and peripheral lung (K-i = 9.82 nM), respectively. This result suggests that the dominant muscarinic receptor in pig airways is of the M(2) subtype. Northern blot analysis demonstrated the presence of m(1) and m(2) mRNAs transcripts in peripheral lung and m(2) and m(3) mRNAs in airway smooth muscle with no evidence for m(4) mRNA.

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Documento generato il 25/11/20 alle ore 01:28:19