![]() Overall, the study reinforces the conclusion that species differences detected for native 5-HT 3 receptors extend to, and appear largely explained by, differences in the properties of homo-oligomeric receptors formed from 5-HT(3A) subunit orthologues.Ībstract = "1. The data are discussed in the context of results previously obtained with the human and mouse orthologues of the 5-HT(3A) subunit. Responses evoked by 5-HT at EC 50 were blocked by the 5-HT 3 receptor selective antagonist ondansetron (IC 50 = 231 ± 22 pM) and by the less selective agents (+)-tubocurarine (IC 50 = 31.9 ± 0.01 nM) and cocaine (IC 50 = 2.1 ± 0.2 μM). With the exception of 2-methyl-5-HT, all of the agonists tested elicited maximal current responses comparable to those produced by a saturating concentration (10 μM) of 5-HT. The response to 5-HT was mimicked by the 5-HT, receptor selective agonists 2-methyl-5-HT (EC 50 = 4.1 ± 0.2 μM), 1-phenylbiguanide (EC 50 = 3.0 ± 0.1 μM), 3-chlorophenylbiguanide (EC 50 = 140 ± 10 nM, 3,5-dichlorophenylbiguanide (EC 50 = 14.5 ± 0.4 nM) and 2,5-dichlorophenylbiguanide (EC 50 = 10.2 ± 0.6 nM). The response reversed in sign at a holding potential of -2.1 ± 1.6 mV. at negative holding potentials, bath applied 5-HT (300 nM-10 μM) evoked a transient, concentration-dependent (EC 50 = 1.1 ± 0.1 μM). ![]() The present study has utilized the two electrode voltage-clamp technique to examine the pharmacological profile of a splice variant of the rat orthologue of the 5-hydroxytryptamine type 3A subunit ((5-HT(3A(b)) heterologously expressed in Xenopus laevis oocytes.
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