Publication

CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS

BODDEKE, HWGM., HOFFMAN, BJ., PALACIOS, JM. & HOYER, D., Sep-1993, In : Naunyn-Schmiedebergs Archives of Pharmacology. 348, 3, p. 221-224 4 p.

Research output: Contribution to journalArticleAcademicpeer-review

APA

BODDEKE, HWGM., HOFFMAN, BJ., PALACIOS, JM., & HOYER, D. (1993). CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS. Naunyn-Schmiedebergs Archives of Pharmacology, 348(3), 221-224.

Author

BODDEKE, HWGM ; HOFFMAN, BJ ; PALACIOS, JM ; HOYER, D. / CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS. In: Naunyn-Schmiedebergs Archives of Pharmacology. 1993 ; Vol. 348, No. 3. pp. 221-224.

Harvard

BODDEKE, HWGM, HOFFMAN, BJ, PALACIOS, JM & HOYER, D 1993, 'CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS', Naunyn-Schmiedebergs Archives of Pharmacology, vol. 348, no. 3, pp. 221-224.

Standard

CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS. / BODDEKE, HWGM; HOFFMAN, BJ; PALACIOS, JM; HOYER, D.

In: Naunyn-Schmiedebergs Archives of Pharmacology, Vol. 348, No. 3, 09.1993, p. 221-224.

Research output: Contribution to journalArticleAcademicpeer-review

Vancouver

BODDEKE HWGM, HOFFMAN BJ, PALACIOS JM, HOYER D. CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS. Naunyn-Schmiedebergs Archives of Pharmacology. 1993 Sep;348(3):221-224.


BibTeX

@article{d77723e3450f47a294b6e46c5c33f73e,
title = "CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS",
abstract = "Functional responses to stimulation of rat 5-HT1C receptors expressed in A9 cells were studied using whole cell voltage clamp recording technique. Stimulation of 5-HT1C receptors with serotonin (5-HT) evoked calcium-dependent outward currents of 109 pA in cells clamped at -50 mV. Pretreatment with the protein kinase C (PKC) activator phorbol myristic acetate (PMA) reduced the 5-HT-induced current amplitude by 46% of the control value. Inclusion of inositol triphosphate (IP3) in the pipette solution induced an outward current of 84 pA. The IP3-induced response was not affected by 60 min pretreatment with PMA. In the presence of the PKC antagonist calphostin C, 60 min treatment with PMA (10(-6) mol/1) reduced the 5-HT response only by 8%. In cells preincubated with PMA, injection of the calcium/calmodulin dependent serine proteinphosphatase calcineurin gradually increased the 5-HT-induced responses by 34%. In A9 cells which were incubated 24 h with the 5-HT1C receptor agonist meta chlorophenylpiperazine hydrochloride (mCPP), 5-HT-induced responses were reduced by 23% of the vehicle pretreated control value. Injection of calcineurin in mCPP treated cells enhanced the 5-HT-induced response by 24%.The results suggest that in A9 cells rat 5-HT1c receptors are desensitized after phosphorylation by PKC. This desensitization can be counteracted by calcineurin-induced dephosphorylation.",
keywords = "RAT 5-HT(1C)RECEPTORS, A9-CELLS, DESENSITIZATION, CALCINEURIN, PROTEIN-KINASE-C, XENOPUS OOCYTES, RECEPTORS, RESPONSES, BRAIN, BETA",
author = "HWGM BODDEKE and BJ HOFFMAN and JM PALACIOS and D HOYER",
year = "1993",
month = sep,
language = "English",
volume = "348",
pages = "221--224",
journal = "Naunyn-Schmiedebergs Archives of Pharmacology",
issn = "0028-1298",
publisher = "SPRINGER",
number = "3",

}

RIS

TY - JOUR

T1 - CALCINEURIN INHIBITS DESENSITIZATION OF CLONED RAT 5-HT(1C)RECEPTORS

AU - BODDEKE, HWGM

AU - HOFFMAN, BJ

AU - PALACIOS, JM

AU - HOYER, D

PY - 1993/9

Y1 - 1993/9

N2 - Functional responses to stimulation of rat 5-HT1C receptors expressed in A9 cells were studied using whole cell voltage clamp recording technique. Stimulation of 5-HT1C receptors with serotonin (5-HT) evoked calcium-dependent outward currents of 109 pA in cells clamped at -50 mV. Pretreatment with the protein kinase C (PKC) activator phorbol myristic acetate (PMA) reduced the 5-HT-induced current amplitude by 46% of the control value. Inclusion of inositol triphosphate (IP3) in the pipette solution induced an outward current of 84 pA. The IP3-induced response was not affected by 60 min pretreatment with PMA. In the presence of the PKC antagonist calphostin C, 60 min treatment with PMA (10(-6) mol/1) reduced the 5-HT response only by 8%. In cells preincubated with PMA, injection of the calcium/calmodulin dependent serine proteinphosphatase calcineurin gradually increased the 5-HT-induced responses by 34%. In A9 cells which were incubated 24 h with the 5-HT1C receptor agonist meta chlorophenylpiperazine hydrochloride (mCPP), 5-HT-induced responses were reduced by 23% of the vehicle pretreated control value. Injection of calcineurin in mCPP treated cells enhanced the 5-HT-induced response by 24%.The results suggest that in A9 cells rat 5-HT1c receptors are desensitized after phosphorylation by PKC. This desensitization can be counteracted by calcineurin-induced dephosphorylation.

AB - Functional responses to stimulation of rat 5-HT1C receptors expressed in A9 cells were studied using whole cell voltage clamp recording technique. Stimulation of 5-HT1C receptors with serotonin (5-HT) evoked calcium-dependent outward currents of 109 pA in cells clamped at -50 mV. Pretreatment with the protein kinase C (PKC) activator phorbol myristic acetate (PMA) reduced the 5-HT-induced current amplitude by 46% of the control value. Inclusion of inositol triphosphate (IP3) in the pipette solution induced an outward current of 84 pA. The IP3-induced response was not affected by 60 min pretreatment with PMA. In the presence of the PKC antagonist calphostin C, 60 min treatment with PMA (10(-6) mol/1) reduced the 5-HT response only by 8%. In cells preincubated with PMA, injection of the calcium/calmodulin dependent serine proteinphosphatase calcineurin gradually increased the 5-HT-induced responses by 34%. In A9 cells which were incubated 24 h with the 5-HT1C receptor agonist meta chlorophenylpiperazine hydrochloride (mCPP), 5-HT-induced responses were reduced by 23% of the vehicle pretreated control value. Injection of calcineurin in mCPP treated cells enhanced the 5-HT-induced response by 24%.The results suggest that in A9 cells rat 5-HT1c receptors are desensitized after phosphorylation by PKC. This desensitization can be counteracted by calcineurin-induced dephosphorylation.

KW - RAT 5-HT(1C)RECEPTORS

KW - A9-CELLS

KW - DESENSITIZATION

KW - CALCINEURIN

KW - PROTEIN-KINASE-C

KW - XENOPUS OOCYTES

KW - RECEPTORS

KW - RESPONSES

KW - BRAIN

KW - BETA

M3 - Article

VL - 348

SP - 221

EP - 224

JO - Naunyn-Schmiedebergs Archives of Pharmacology

JF - Naunyn-Schmiedebergs Archives of Pharmacology

SN - 0028-1298

IS - 3

ER -

ID: 14146121