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  • 1
    ISSN: 0014-5793
    Keywords: 5-Carboxamidotryptamine ; 5-Hydroxytryptamine ; CA1 pyramidal cell ; G-protein-coupled receptor ; Habenula ; Serotonin
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Biology , Chemistry and Pharmacology , Physics
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 353 (1995), S. 28-35 
    ISSN: 1432-1912
    Keywords: 5-HT4 receptors ; 5-Hydroxytryptamine ; SB 203186 ; Porcine sinoatrial tachycardia ; Porcine and human atria
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We investigated the blockade of the positive inotropic effects of 5-hydroxytryptamine (5-HT) by SB 203 186 (piperidinoethyl-indole-3-carboxylate hydrochloride) and its affinity for 5-HT4 receptors of human right atrium and piglet left atrium. We also compared the blocking effects of SB 203 186 against 5-HT-evoked tachycardia in anaesthetised adult Yucatan minipigs as well as new-born Camborough piglets. SB 203 186 caused competitive antagonism of the positive inotropic effects of 5-HT in electrically paced atrial preparations of man (pK B = 8.9) and piglet (pK B = 8.5) at concentrations (up to 0.3 μmo]/l) which were devoid of depressant or stimulant effects. The affinity of SB 203 186 for atrial 5-HT4 receptors was 30–160 times higher than that of tropisetron. 5-HT caused tachycardia with similar potency and efficacy in Yucatan minipigs and new-born Camborough piglets. SB 203 186 (0.1–3 mg/kg, i.v.) surmountably antagonised 5-HT-evoked tachycardia in anaesthetised Yucatan minipigs or new-born Camborough piglets with similar potency. The blocking potency of SB 203 186 in Yucatan minipigs was 17 times higher than that of tropisetron. Intraduodenally administered SB 203 186 (0.3–3 mg/kg) to new-born Camborough piglets produced blockade of 5-HT-evoked tachycardia which was maximal after 20 min and lasted for more than 3 h with 0.3 mg/kg. The antagonism produced by the SB 203 186 administration in new-born Camborough piglets was dose-related and threefold greater through the intravenous route than through the intraduodenal route. We conclude that SB 203 186 is an antagonist with nanomolar affinity for both human and porcine atrial 5-HT4 receptor. The in vivo results demonstrate that the sinoatrial 5-HT4 receptors function is similar in new-born Camborough piglets and adult Yucatan minipigs. Both porcine breeds are valid models for human atrial 5-HT4 receptors as demonstrated with the antagonist SB 203186.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 353 (1995), S. 28-35 
    ISSN: 1432-1912
    Keywords: Key words 5-HT4 receptors ; 5-Hydroxytryptamine ; SB 203186 ; Porcine sinoatrial tachycardia ; Porcine and human atria
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  We investigated the blockade of the positive inotropic effects of 5-hydroxytryptamine (5-HT) by SB 203 186 (piperidinoethyl-indole-3-carboxylate hydrochloride) and its affinity for 5-HT4 receptors of human right atrium and piglet left atrium. We also compared the blocking effects of SB 203 186 against 5-HT-evoked tachycardia in anaesthetised adult Yucatan minipigs as well as new-born Camborough piglets. SB 203 186 caused competitive antagonism of the positive inotropic effects of 5-HT in electrically paced atrial preparations of man (pK B=8.9) and piglet (pK B=8.5) at concentrations (up to 0.3 μmol/l) which were devoid of depressant or stimulant effects. The affinity of SB 203 186 for atrial 5-HT4 receptors was 30–160 times higher than that of tropisetron. 5-HT caused tachycardia with similar potency and efficacy in Yucatan minipigs and new-born Camborough piglets. SB 203 186 (0.1–3 mg/kg, i.v.) surmountably antagonised 5-HT-evoked tachycardia in anaesthetised Yucatan minipigs or new-born Camborough piglets with similar potency. The blocking potency of SB 203 186 in Yucatan minipigs was 17 times higher than that of tropisetron. Intraduodenally administered SB 203 186 (0.3–3 mg/kg) to new-born Camborough piglets produced blockade of 5-HT-evoked tachycardia which was maximal after 20 min and lasted for more than 3 h with 0.3 mg/kg. The antagonism produced by the SB 203 186 administration in new-born Camborough piglets was dose-related and threefold greater through the intravenous route than through the intraduodenal route. We conclude that SB 203 186 is an antagonist with nanomolar affinity for both human and porcine atrial 5-HT4 receptor. The in vivo results demonstrate that the sinoatrial 5-HT4 receptors function is similar in new-born Camborough piglets and adult Yucatan minipigs. Both porcine breeds are valid models for human atrial 5-HT4 receptors as demonstrated with the antagonist SB 203 186.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-2072
    Keywords: Activity ; Brain ; Catecholamines ; 5-Hydroxytryptamine ; Lithium ; Rubidium ; Tranylcypromine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract 1. The administration of 15 mg/kg tranylcypromine sulphate (Tc) to rats which have been given lithium chloride (LiCl) in the diet (30 mmol/kg dry food) for 14 days produces hyperactivity within 4 hrs, and this lasts for at least 4 further hours. 2. If LiCl is replaced by rubidium chloride (RbCl) at the same dose, the hyperactivity following Tc is increased and it appears within 2 hrs. 3. 5-Hydroxytryptamine (5HT) accumulation after a monoamine oxidase inhibitor (Tc) is increased 46% and 85% respectively above control values by LiCl and RbCl administration. 4. The hyperactivity produced by the above combinations is inhibited by α-methyl-p-tyrosine (αmpt). The inhibition is more effective following LiCl than RbCl treatment. 5. After sodium chloride (NaCl) and LiCl treatment, but not after RbCl treatment, the combination of αmpt and Tc produces rat brain concentrations of dopamine (DA) significantly below control values. 6. The smaller increase of brain noradrenaline (NA) after Tc and RbCl suggests that a lower percentage of NA is being metabolised by MAO. The greater decrease of NA after giving αmpt to RbCl and LiCl treated rats suggests an increased “turnover” rate of Na. 7. The hyperactivity syndrome seen in rats after the administration of LiCl or RbCl and Tc is dependent upon both 5HT and dopamine mechanisms.
    Type of Medium: Electronic Resource
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