Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P46098 (5-HT3 receptor)
 2,290 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The interactions of serotonin 5-HT1A, 5-HT1C/2 and 5-HT3 receptor subtypes with apomorphine-induced locomotor activity (AILA) were investigated in Sprague-Dawley rats. The 5-HT3 antagonists ondansetron and ICS 205-930 had no significant effects on AILA. The 5-HT1A agonist 8-hydroxy-2-(di-N-propylamino) tetralin (8-OH-DPAT) produced an increase in locomotor activity that was independent of DA neurotransmission. The locomotor activity induced by co-administration of apomorphine (APO; 0.25 mg/kg) and 8-OH-DPAT (0.25-1.0 mg/kg) was not significantly higher than those induced by APO alone during the peak period of APO stimulation of locomotor activity, nor were they higher than activity induced by 8-OH-DPAT alone during the same time intervals. The 5-HT1 antagonist (1)-propranolol had a depressant effect on AILA, but only at high doses. Coadministration of (1)-propranolol (5 mg/kg) and 8-OH-DPAT (1.0 mg/kg) elevated spontaneous locomotor activity for the first 10 min of the session when compared to 8-OH-DPAT (1.0 mg/kg) alone. The 5-HT2 antagonist ketanserin along with moderate and high doses of mesulergine depressed AILA, effects which may be mediated by the 5-HT2 antagonist properties of these drugs, by nonspecific sedation or by direct effects of these compounds on DA D2 receptors. In contrast to the high-dose mesulergine depression of AILA, a low dose (0.1 mg/kg) of mesulergine elevated AILA, an effect which was blocked by the 5-HT1C/2 agonist 1-(2,-5-dimethoxy-4-iodophenyl) -2-aminopropane (DOI; 1 mg/kg). Neither of these compounds at the doses tested had significant effects on spontaneous locomotor activity.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Effects of serotonergic agents on apomorphine-induced locomotor activity. 787 Sep 5

Direct effects of the enantiomers of the classical dopamine receptor ligand apomorphine on 5-HT3 receptors were examined in NIE-115 neuroblastoma cells in whole-cell voltage clamp mode. R(-)-apomorphine (R(-)APO; 3-300 microM) evokes a small, transient inward ion current. At 30 microM, R(-)APO induces its maximum inward current, which is approximately 3% of the amplitude of the inward current induced by 10 microM 5-HT. The R(-)APO-induced current is completely and reversibly inhibited after superfusion of 50 nM of the selective 5-HT3 receptor antagonist MDL 72222 and after desensitization of the 5-HT3 receptors by 10 microM 5-HT. The results indicate that R(-)APO is a partial agonist at the 5-HT3 receptor. R(-)APO (30 microM) evokes a depolarization of the membrane potential with an amplitude which is 26% of the 10 microM 5-HT-induced depolarization. In addition, the 5-HT-induced depolarization is reduced (from 29 to 15 mV) after prolonged exposure of the cell to R(-)APO. S(+)-apomorphine (S(+)APO; 3-300 microM) does not evoke an ion current. Instead, S(+)APO antagonizes the 5-HT3 receptor with an IC50 of 32 microM. The combined results indicate that enantiomers of apomorphine act directly on 5-HT3 receptors, and suggest that the in vivo effects of apomorphine are partially attributable to a direct interaction with 5-HT3 receptors.
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PMID:Agonist and antagonist effects of apomorphine enantiomers on 5-HT3 receptors. 968 Feb 51