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Research ArticleNEUROPHARMACOLOGY

A Subtype of the γ-Aminobutyric AcidB Receptor Regulates Cholinergic Twitch Response in the Guinea Pig Ileum

Manuela Marcoli, Simona Scarrone, Guido Maura, Giambattista Bonanno and Maurizio Raiteri
Journal of Pharmacology and Experimental Therapeutics April 2000, 293 (1) 42-47;
Manuela Marcoli
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Simona Scarrone
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Guido Maura
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Giambattista Bonanno
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Maurizio Raiteri
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Abstract

The pharmacological profile of the γ-aminobutyric acid (GABA)B receptor regulating cholinergic twitch contraction in the guinea pig ileum myenteric plexus-longitudinal muscle preparation was investigated. GABA and (−)-baclofen inhibited the contraction, exhibiting quite close potencies (pD2 for GABA = 5.70; pD2 for (−)-baclofen = 5.33). The compound CGP 47656 also reduced the cholinergic twitch concentration (pD2 = 5.42), but its efficacy was significantly lower than that of (−)-baclofen or GABA. Added at varying concentrations, CGP 47656 modified the concentration-response curve of (−)-baclofen as expected for a partial agonist. Phaclofen, CGP 36742, CGP 35348, and CGP 52432 behaved as competitive antagonists of (−)-baclofen, exhibiting the following pA2 values: 3.90, 4.88, 5.02, and 7.82, respectively. The compound CGP 56999 behaved as a potent noncompetitive GABAB receptor antagonist. In comparing the pharmacological profile of the ileal receptor with those of the previously characterized pharmacological subtypes of the GABAB receptor present in the central nervous system, it can be seen that the GABAB receptor inhibiting cholinergic twitch contraction in guinea pig ileum myenteric plexus-longitudinal muscle mostly resembles the receptor located on somatostatin human neocortex nerve terminals.

Footnotes

  • Send reprint requests to: Dr. Manuela Marcoli, Dipartimento di Medicina Sperimentale, Sezione Farmacologia e Tossicologia, Viale Cembrano 4-16148 Genova, Italy. E-mail:marcoli{at}pharmatox.unige.it

  • ↵1 This work was supported by an Italian MURST Network grant (1997).

  • Abbreviations:
    GABA
    γ-aminobutyric acid
    CNS
    central nervous system
    CGP 35348
    3-aminopropyl(diethoxymethyl)phosphinic acid
    CGP 36742
    3-aminopropyl-n butyl phosphinic acid
    CGP 47656
    3-aminopropyl-(difluoromethyl)phosphinic acid
    CGP 52432
    [3-[[(3,4-dichlorophenyl)methyl]amino]propyl](diethoxymethyl) phosphinic acid
    CGP 56999
    [3{[1-(R)-(3-carboxyphenyl)ethyl]amino}-2-(S)-hydroxy-propyl]cyclohexyl-methyl-phosphinic acid
    MP-LM
    myenteric plexus-longitudinal muscle
    SRIF
    somatostatin
    CCK
    cholecystokinin
    • Received October 21, 1999.
    • Accepted January 6, 2000.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 293 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 293, Issue 1
1 Apr 2000
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Research ArticleNEUROPHARMACOLOGY

A Subtype of the γ-Aminobutyric AcidB Receptor Regulates Cholinergic Twitch Response in the Guinea Pig Ileum

Manuela Marcoli, Simona Scarrone, Guido Maura, Giambattista Bonanno and Maurizio Raiteri
Journal of Pharmacology and Experimental Therapeutics April 1, 2000, 293 (1) 42-47;

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Research ArticleNEUROPHARMACOLOGY

A Subtype of the γ-Aminobutyric AcidB Receptor Regulates Cholinergic Twitch Response in the Guinea Pig Ileum

Manuela Marcoli, Simona Scarrone, Guido Maura, Giambattista Bonanno and Maurizio Raiteri
Journal of Pharmacology and Experimental Therapeutics April 1, 2000, 293 (1) 42-47;
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