Serotonin 5-HT1D and 5-HT1A receptors respectively mediate inhibition of glutamate release and inhibition of cyclic GMP production in rat cerebellum in vitro
The K(+)-evoked overflow of endogenous glutamate from cerebellar synaptosomes was inhibited by serotonin [5-hydroxytryptamine (5-HT); pD2 = 8.95], 8-hydroxy-2-(di-n- propylamino)tetralin (8-OH-DPAT; pD2 = 7.35), and sumatriptan (pD2 = 8.43). These inhibitions were prevented by the selective 5-HT1D receptor antagonist N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1, 2,4 - oxadiazol-3-yl) (1,1-biphenyl)-4-carboxamide (GR-127935). The three agonists tested also inhibited the cyclic GMP (cGMP) response provoked in slices by K+ depolarization; pD2 values were 9.37 (5-HT), 9.00 (8-OH-DPAT), and 8.39 (sumatriptan). When cGMP formation was elevated by directly activating glutamate receptors with NMDA or alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA), the inhibition of the cGMP responses displayed the following pattern: 5-HT (pD2 values of 8.68 and 8.72 against NMDA and AMPA, respectively); 8-OH-DPAT (respective pD2 values of 9.15 and 9.00); sumatriptan (0.1 microM) was ineffective. The 5-HT1A receptor antagonist (S)-(+)N-tert-butyl-3-[4-(2- methoxyphenyl)piperazin-1-yl]-2-phenylpropionamide dihydrochloride [(+)-WAY 100135] did not prevent the inhibition of glutamate release by 5-HT but blocked the inhibition by 8-OH-DPAT of the NMDA/AMPA-evoked cGMP responses. It is suggested that presynaptic 5-HT1D receptors mediate inhibition directly of glutamate release and indirectly of the cGMP responses to the released glutamate; on the other hand, activation of (postsynaptic) 5-HT1A receptors causes inhibition of the cGMP responses linked to stimulation of NMDA/AMPA receptors.
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
1996 |
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| Erschienen: |
1996 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:66 |
|---|---|
| Enthalten in: |
Journal of neurochemistry - 66(1996), 1 vom: 18. Jan., Seite 203-9 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Maura, G [VerfasserIn] |
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| Anmerkungen: |
Date Completed 24.01.1996 Date Revised 30.06.2019 published: Print Citation Status MEDLINE |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM084973498 |
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| 041 | |a eng | ||
| 100 | 1 | |a Maura, G |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Serotonin 5-HT1D and 5-HT1A receptors respectively mediate inhibition of glutamate release and inhibition of cyclic GMP production in rat cerebellum in vitro |
| 264 | 1 | |c 1996 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ohne Hilfsmittel zu benutzen |b n |2 rdamedia | ||
| 338 | |a Band |b nc |2 rdacarrier | ||
| 500 | |a Date Completed 24.01.1996 | ||
| 500 | |a Date Revised 30.06.2019 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a The K(+)-evoked overflow of endogenous glutamate from cerebellar synaptosomes was inhibited by serotonin [5-hydroxytryptamine (5-HT); pD2 = 8.95], 8-hydroxy-2-(di-n- propylamino)tetralin (8-OH-DPAT; pD2 = 7.35), and sumatriptan (pD2 = 8.43). These inhibitions were prevented by the selective 5-HT1D receptor antagonist N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1, 2,4 - oxadiazol-3-yl) (1,1-biphenyl)-4-carboxamide (GR-127935). The three agonists tested also inhibited the cyclic GMP (cGMP) response provoked in slices by K+ depolarization; pD2 values were 9.37 (5-HT), 9.00 (8-OH-DPAT), and 8.39 (sumatriptan). When cGMP formation was elevated by directly activating glutamate receptors with NMDA or alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA), the inhibition of the cGMP responses displayed the following pattern: 5-HT (pD2 values of 8.68 and 8.72 against NMDA and AMPA, respectively); 8-OH-DPAT (respective pD2 values of 9.15 and 9.00); sumatriptan (0.1 microM) was ineffective. The 5-HT1A receptor antagonist (S)-(+)N-tert-butyl-3-[4-(2- methoxyphenyl)piperazin-1-yl]-2-phenylpropionamide dihydrochloride [(+)-WAY 100135] did not prevent the inhibition of glutamate release by 5-HT but blocked the inhibition by 8-OH-DPAT of the NMDA/AMPA-evoked cGMP responses. It is suggested that presynaptic 5-HT1D receptors mediate inhibition directly of glutamate release and indirectly of the cGMP responses to the released glutamate; on the other hand, activation of (postsynaptic) 5-HT1A receptors causes inhibition of the cGMP responses linked to stimulation of NMDA/AMPA receptors | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 7 | |a Oxadiazoles |2 NLM | |
| 650 | 7 | |a Piperazines |2 NLM | |
| 650 | 7 | |a Receptor, Serotonin, 5-HT1D |2 NLM | |
| 650 | 7 | |a Receptors, AMPA |2 NLM | |
| 650 | 7 | |a Receptors, N-Methyl-D-Aspartate |2 NLM | |
| 650 | 7 | |a Receptors, Serotonin |2 NLM | |
| 650 | 7 | |a Receptors, Serotonin, 5-HT1 |2 NLM | |
| 650 | 7 | |a Serotonin Agents |2 NLM | |
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| 650 | 7 | |a Serotonin |2 NLM | |
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| 650 | 7 | |a Glutamic Acid |2 NLM | |
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| 650 | 7 | |a N-Methylaspartate |2 NLM | |
| 650 | 7 | |a 6384-92-5 |2 NLM | |
| 650 | 7 | |a alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid |2 NLM | |
| 650 | 7 | |a 77521-29-0 |2 NLM | |
| 650 | 7 | |a 8-Hydroxy-2-(di-n-propylamino)tetralin |2 NLM | |
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| 650 | 7 | |a Sumatriptan |2 NLM | |
| 650 | 7 | |a 8R78F6L9VO |2 NLM | |
| 650 | 7 | |a Cyclic GMP |2 NLM | |
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| 650 | 7 | |a Potassium |2 NLM | |
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| 700 | 1 | |a Raiteri, M |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Journal of neurochemistry |d 1956 |g 66(1996), 1 vom: 18. Jan., Seite 203-9 |w (DE-627)NLM000006211 |x 1471-4159 |7 nnns |
| 773 | 1 | 8 | |g volume:66 |g year:1996 |g number:1 |g day:18 |g month:01 |g pages:203-9 |
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