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Titolo:
MUSCARINIC M(2) RECEPTOR SYNTHESIS - STUDY OF RECEPTOR TURNOVER WITH PROPYLBENZILYLCHOLINE MUSTARD
Autore:
HADDAD EB; ROUSELL J; BARNES RJ;
Indirizzi:
NATL HEART & LUNG INST,DEPT THORAC MED,DOVEHOUSE ST LONDON ENGLAND NATL HEART & LUNG INST,DEPT THORAC MED LONDON ENGLAND
Titolo Testata:
European journal of pharmacology. Molecular pharmacology section
fascicolo: 3, volume: 290, anno: 1995,
pagine: 201 - 205
SICI:
0922-4106(1995)290:3<201:MMRS-S>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACETYLCHOLINE-RECEPTORS; SENSITIVITY; EXPRESSION; SUBTYPES; BRAIN; CELLS; RAT;
Keywords:
MUSCARINIC RECEPTOR SYNTHESIS; PROPYLBENZILYLCHOLINE MUSTARD; HEL 299 CELL; RECEPTOR INACTIVATION; RADIOLIGAND BINDING; CAMP ACCUMULATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
27
Recensione:
Indirizzi per estratti:
Citazione:
E.B. Haddad et al., "MUSCARINIC M(2) RECEPTOR SYNTHESIS - STUDY OF RECEPTOR TURNOVER WITH PROPYLBENZILYLCHOLINE MUSTARD", European journal of pharmacology. Molecular pharmacology section, 290(3), 1995, pp. 201-205

Abstract

We have investigated the rate and the functional responsiveness of the newly synthesised M(2) muscarinic receptors in HEL 299 cells following propylbenzilylcholine mustard treatment at 37 degrees C. Propylbenzilylcholine mustard induced a dose-dependent loss of the hydrophilic ligand [H-3]N-methylscopoiamine binding sites with 80% inactivation at 0.1 mu M. The rate of muscarinic receptor synthesis in these cells, estimated from wash-out experiments following propylbenzilylcholine mustard treatment, was very slow and returned to control values after 36 hof propylbenzilylcholine mustard removal. The recovery of muscarinic receptors was blocked by the cycloheximide pre-treatment, indicating the synthetic pathway for the new receptors. In control cells as well as in cells treated with propylbenzilylcholine mustard and allowed to recover for 12 h, carbachol still inhibited forskolin-induced cAMP accumulation. These results show that (i) the rate of M(2) muscarinic receptor synthesis is slow (ii) the recovery of receptors is mainly through increased synthesis and (iii) the newly synthesised receptors retaintheir full functional activity.

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Documento generato il 04/12/20 alle ore 13:12:57