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• W2079267119 abstract "5-Hydroxytryptamine (5-HT) and 2,5-dimethoxy-4-methyl-amphetamine (DOM) produced a concentration-dependent contraction in isolated umbilical veins obtained from fetal lambs within 2 weeks of term. Contractions to 5-HT were antagonized by ketanserin, mianserin and methiothepin with the dissociation constants (KB) being 2.17 ± 0.36, 1.37 ± 0.55 and 1.98 ± 0.48 nM, respectively. The order of potency of serotonergic agonists in this tissue was: DOM > 5-HT > α-methyl-5-HT > 1(3-chlorophenyl) piperazine (mCPP) . m-trifluoromethyl-phenylpiperazine (TFMPP) > 8-hydroxy-dipropylaminotetralin (8-OH-DPAT) = 2-methyl-5-HT. α-Methyl-5-HT was a full agonist compared to 5-HT. DOM possesses greater affinity but less efficacy than that of 5-HT. The affinities and efficacies of the other agonists studied were lower than those of 5-HT. Variation in the sensitivity and potency of agonist is primarily due to variations in their affinity for 5-HT receptors. Assessment of receptor occupancy vs. functional response demonstrated very little, if any, receptor reserve for 5-HT receptors in this tissue. Contractile responses to DOM, 8-OH-DPAT, mCPP and 2-methyl-5-HT were effectively blocked by ketanserin. The dissociation constants (KB) of ketanserin against these agonists were as follows: DOM, 2.78 ± 0.85 nM; 8-OH-DPAT-, 3.47 ± 1.12 nM; mCPP, 1.45 ± 0.51 nM; 2-methyl-5-HT, 1.99 ± 0.74 nM. The dissociation constant of MDL 72222 (3-tropanyl-3,5-dichlorobenzoate) vs. 5-HT was 13833 nM. No antagonism by prazosin (10−7 M) or yohimbine (10−7 M) of the responses to 5-HT was observed. These results indicate that 5-HT2 receptors are present in the ovine umbilical vein. 5-HT3 receptors were not present in this tissue. Activation of α-adrenoceptors was not involved in the contractions to 5-HT." @default.
• W2079267119 created "2016-06-24" @default.
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• W2079267119 date "1990-08-01" @default.
• W2079267119 modified "2023-09-24" @default.
• W2079267119 title "Receptor mechanisms for 5-hydroxytryptamine (5-HT) in isolated ovine umbilical vein" @default.
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• W2079267119 doi "https://doi.org/10.1016/0014-2999(90)90620-l" @default.
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