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)

Radioligand binding studies were performed to characterize serotonin 5HT1D binding sites in porcine and bovine brain. 3H-5HT binding, in the presence of 1 microM (+/-)pindolol (to block 5HT1A and 5HT1B receptors) and 100 nM mesulergine (to block 5HT1C receptors), was specific, saturable, and of high affinity. In porcine and bovine cortex and striatum the majority of 5HT1 sites (80%-90%) were of the 5HT1D subtype. In competition experiments 8-OH-DPAT, TFMPP, mesulergine, DOB, and ICS 205-930 had low affinity for 3H-5HT-labeled 5HT1D sites, indicating that the pharmacology of the 5HT1D site is distinct from previously identified 5HT1A, 5HT1B, 5HT1C, 5HT2, and 5HT3 sites. Guanyl nucleotides, GTPgammaS, and Gpp(NH)p, and divalent cations potently modulated the binding of 3H-5HT to 5HT1D sites in porcine and bovine striatum. Mg++ ions increased the number and affinity of 3H-5HT-labeled 5HT1D sites, while guanyl nucleotides decreased the number of 3H-5HT-labeled 5HT1D sites. These results demonstrate the presence of the 5HT1D receptors in porcine striatum and bovine cortex and provide direct demonstration that the radioligand binding assay for the 5HT1D receptor can monitor the interaction of this receptor with a GTP-binding protein.
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PMID:Detection and characterization of a 5HT1D serotonin receptor-GTP binding protein interaction in porcine and bovine brain. 252 22

The effects of local application of 5-HT2- and 5-HT3-receptor agonists in the nucleus tractus solitarius (NTS) on the cardiovascular parameters were investigated in anaesthetized spontaneously hypertensive (SH) rats and their genetically normotensive precursors (WKY). Unilateral microinjection of picomolar doses of a 5HT2 receptor agonist, 2,5-dimethoxy-3-bromo-amphetamine (DOB, 0.025-0.5 pmol), produced a dose-dependent hypotension and bradycardia in both SH and WKY rats. These effects could be prevented by prior local microinjection of a 5-HT2 receptor antagonist, ketanserin (10 pmol). However, for both cardiovascular parameters, DOB was more potent in SH than in WKY rats. Thus, the dose-related responses to DOB were shifted to the left in SH as compared to WKY rats. Bilateral microinjection of the 5-HT3 receptor agonist, phenylbiguanide (1.7-5 nmol), produced an increase in blood pressure and reduced the cardiovagal component of the baroreflex. These effects were not significantly different in SH and WKY rats. These data suggest that 5-HT2 receptors, but not 5-HT3 receptors, are supersensitive in the NTS of SH rats.
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PMID:Cardiovascular effects of 5HT2 and 5HT3 receptor stimulation in the nucleus tractus solitarius of spontaneously hypertensive rats. 771 56