Smooth muscle cells were isolated from the dog gallbladder and used to examine whether bombesin-14 and substance P cause direct contraction and whether this effect is mediated by the same or different receptors. Both peptides caused concentration-dependent contraction that was inhibited by two substance P derivatives, [D-Pro2, D-Trp7,9]SP ([PTT]SP) and [D-Arg1, D-Pro2, D-Trp7,9, Leu11]SP ([APTTL]SP). In nonmuscle cells, these substance P derivatives exhibit preferential antagonism of responses to substance P and bombesin, respectively; accordingly, these properties were used to demonstrate the presence of separate bombesin and substance P receptors. Estimates of the apparent K(i) showed that [PTT]SP was 40 times more potent than [APTTL]SP as an antagonist of the response to substance P, whereas [APTTL]SP was 85 times more potent than [PTT]SP as an antagonist of the response to bombesin-14. Estimates of median inhibitory concentration obtained from inhibition curves for the effect of various concentrations of each antagonist on the responses to substance P and bombesin-14 confirmed that [PTT]SP was a preferential antagonist of the response to substance P and [APTTL]SP, a preferential antagonist of the response to bombesin-14. The results demonstrate the presence of separate bombesin and substance P receptors mediating contraction of smooth muscle cells of the dog gallbladder.
IDENTIFICATION OF SEPARATE BOMBESIN AND SUBSTANCE-P RECEPTORS ON ISOLATED MUSCLE-CELLS FROM CANINE GALLBLADDER / Severi, Carola; J. R., Grider; G. M., Makhlouf. - In: JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS. - ISSN 0022-3565. - STAMPA. - 245:1(1988), pp. 195-198.
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Titolo: | IDENTIFICATION OF SEPARATE BOMBESIN AND SUBSTANCE-P RECEPTORS ON ISOLATED MUSCLE-CELLS FROM CANINE GALLBLADDER | |
Autori: | ||
Data di pubblicazione: | 1988 | |
Rivista: | ||
Citazione: | IDENTIFICATION OF SEPARATE BOMBESIN AND SUBSTANCE-P RECEPTORS ON ISOLATED MUSCLE-CELLS FROM CANINE GALLBLADDER / Severi, Carola; J. R., Grider; G. M., Makhlouf. - In: JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS. - ISSN 0022-3565. - STAMPA. - 245:1(1988), pp. 195-198. | |
Handle: | http://hdl.handle.net/11573/43006 | |
Appartiene alla tipologia: | 01a Articolo in rivista |