Abstract
Long-term (18 h) activation of 5-HT1A receptors alters 5-HT1A receptor-G protein coupling and leads to heterologous sensitization of adenylate cyclase. In contrast, the effects of short-term (2 h) 5-HT1A receptor activation on subsequent adenylate cyclase activity have not been determined. The present study examined and characterized 5-HT1A receptor-induced heterologous sensitization following short-term activation in CHO-5-HT1A cells. Short-term activation of 5-HT1A receptors with full agonists, as well as the partial agonist, buspirone, markedly enhanced subsequent forskolin-stimulated cyclic AMP accumulation. This heterologous sensitization was evident after 30 min treatment with 5HT and appeared to be near maximal following 2 h agonist treatment. Sensitization was characterized by a dose-dependent increase in forskolin-stimulated cyclic AMP accumulation and was prevented by WAY 100635 or by pertussis toxin treatment. The ability of the 5-HT1A agonists to induce heterologous sensitization was not significantly altered by agents shown previously to modulate 5-HT1A-mediated inhibition of cyclic AMP accumulation.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
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Adenylyl Cyclases / metabolism*
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Animals
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Arachidonic Acid / pharmacology
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Buspirone / pharmacology
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CHO Cells
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Calcimycin / pharmacology
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Colforsin / pharmacology
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Cricetinae
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Cricetulus
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Cyclic AMP / metabolism
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Cycloheximide / pharmacology
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Dose-Response Relationship, Drug
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Flavonoids / pharmacology
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Humans
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Indoles / pharmacology
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Indomethacin / pharmacology
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Maleimides / pharmacology
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Pertussis Toxin / pharmacology
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Phorbol Esters / pharmacology
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Piperazines / pharmacology
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Pyridines / pharmacology
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Receptor, Serotonin, 5-HT1A / physiology*
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Serotonin / pharmacology
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Serotonin 5-HT1 Receptor Agonists
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Serotonin 5-HT1 Receptor Antagonists
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Time Factors
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Tryptamines / pharmacology
Substances
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Flavonoids
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Indoles
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Maleimides
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Phorbol Esters
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Piperazines
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Pyridines
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Serotonin 5-HT1 Receptor Agonists
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Serotonin 5-HT1 Receptor Antagonists
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Tryptamines
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Receptor, Serotonin, 5-HT1A
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LY 293284
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Colforsin
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phorbol-12-myristate
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Arachidonic Acid
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Serotonin
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Calcimycin
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N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide
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8-Hydroxy-2-(di-n-propylamino)tetralin
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Cycloheximide
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Cyclic AMP
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Pertussis Toxin
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Adenylyl Cyclases
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bisindolylmaleimide
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2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
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Buspirone
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Indomethacin