5-Hydroxytryptamine uptake

Anand M, Gopal K, Agrawal C, et al. 1986. Endosulfan induced inhibition of 3H 5-hydroxytryptamine uptake in platelets. Toxicol Lett 32 203-208. 

Ross, S.B. Ogren, S.O. and Renyi, L. Antagonism of the acute and longterm biochemical effects of 4-chloroamphetamine on the 5-HT neurons in rat brain by inhibitors of the 5-hydroxytryptamine uptake. Acta Pharmacol Toxicol [Copenh] 39 456-476, 1976. 

Nalepa I, Vetulani J Enhancement of the responsiveness of cortical adrenergic receptors by chronic administration of the 5-hydroxytryptamine uptake inhibitor citalopram. J Neurochem 60 2029-2035, 1993 Nalepa I, Vetulani J The responsiveness of cerebral cortical adrenergic receptors after chronic administration of atypical antidepressant mianserin. J Psychiatry Neurosci 19 (2) 120, 1994... 

Ogren S-O, Ross SB, Holm AC, et al 5-Hydroxytryptamine and avoidance performance in the rat antagonism of the acute effect of p-chloroamphetamine by zimetidine, an inhibitor of 5-hydroxytryptamine uptake. Neurosci Lett 7 331-336, 1977... 

The dopamine uptake and the 5-hydroxytryptamine uptake systems are very similar to the noradrenaline uptake... 

Aral, Y. Kim, S.Y. Kinemuchi, H. Tadano, T. Satoh, S. and Satoh, N. Inhibition of brain type A monoamine oxidase and 5-hydroxytryptamine uptake by two amphetamine metabolites, p-hydroxyamphetamine and p-hydroxynorephedrine. JNeurochem 55 403-408, 1990. 

Affects noradrenaline (norepinephrine), dopamine and serotonin (5-hydroxytryptamine) uptake and release... 

Hetey, L. and Quirling, K., Synaptosomal uptake and release of dopamine and 5-hydroxytryptamine in the nucleus accumbens in vitro following in vivo administration of lysergic acid diethlamide in rats, Acta Biol. Med. Ger., 39, 889, 1980. 

F. Martel and E. Keating. Uptake of 1-methyl-4-phenylpyridinium (MPP+) by the JAR human placental choriocarcinoma cell line Comparison with 5-hydroxytryptamine. Placenta. 24 361-369 (2003). 

Sertraline (Zoloft, Pfizer) selective serotonin (5-hydroxytryptamine 5HT) uptake inhibitor for treating major depression and obsessive compulsive disorder... 

Ramassamy C, Christen Y, Clostre F, Costentin J. (1992). The Ginkgo biloba extract, EGb 761, increases synaptosomal uptake of 5-hydroxytryptamine in-vitro and ex-vivo studies. J Pharm Pharmacol. 44(11) 943-45. 

It should be possible to treat the disease by increasing the concentration of the neurotransmitter in the synaptic cleft. There are, in principle, three ways in which this could be achieved, (i) Neurotransmitter synthesis could be increased, (ii) The rate of exocytosis could be increased, (iii) Removal of neurotransmitter from the synapse could be inhibited. Drugs that affect process (iii) have been developed. The tricyclic antidepressants and the specific serotonin (5-hydroxytryptamine) reuptake inhibitors (abbreviated to SSRIs) inhibit uptake of the neurotransmitter into the presynaptic on postsynaptic neurone. The most prescribed SSRI is fluoxetine (Prozac). 

PHARMACOLOGICAL ACTIVITIES AND CLINICAL TRIALS 5-Hydroxytryptamine inhibition. Ethanol (80%) extract of the dried stem hark, in cell culture at a dose of 10 pg/mL, inhibited the uptake of serotonin (5HT) in rat brainstem neurons L... 

Nicholson AN, Pascoe PA 5-Hydroxytryptamine and noradrenaline uptake inhibition studies on sleep in man. Neuropharmacology 25 1079-1083, 1986 Nicholson AN, Pascoe PA Studies on the modulation of the sleep-wakefulness continuum in man by fluoxetine, a 5-HT uptake inhibitor. Neuropharmacology 27 597-602, 1988... 

Tuomisto J, Tukiainen E. Decreased uptake of 5-hydroxytryptamine in blood platelets from depressed patients. Nature 1976 262 596-598. 

EGb inhibits the uptake of [3H]norepinephrine ([3H]NE) and [3H]dopamine and [3H]5-hydroxytryptamine ([3H]5-HT) into in vitro synaptosomes prepared from the striatum and cortex in a concentration-dependent manner. The rank order of potency for the inhibition of amine uptake is NE > dopamine > 5-HT [173]. Similar results were obtained by Ramassamy et al. [174]. These workers showed that EGb decreased the specific uptakes of [3H]dopamine, [3H]5-HT and [3H]choline by synaptosomes prepared from the striatum of mice in a concentration-dependent manner. The IC,0 values were 637 pg/rol for [3H]dopamine uptake, 803 pg/ml for [3H]5-HT uptake, >2000 pg/ml for [3H]choline uptake. However, they concluded that the inhibition of amine uptake caused by EGb appears to be non-specific, since EGb also prevents the specific binding of the dopamine uptake inhibitor [3H]GBR12783 to membranes prepared from striatum. 

Driessen, B. and Reimann, W. Interaction of the central analgesic, tramadol, with the uptake and release of 5-hydroxytryptamine in the rat brain in vitro, Br. J. Pharmacol. 1992, 105, 147-151. 

Synaptic serotonin (5-hydroxytryptamine) transporters are inhibited by amphetamines, the tropane alkaloids cocaine and ecgonine [194] and by the indole alkaloid ibogaine (12-methoxyibogamine) and its demethylation product ibogamine [191, 195]. Hyperforin is a major antidepressant constituent of St. John s Wort (Hypericum perforatum) and inhibits serotonin uptake by elevating cytosolic Na+ [196]. The additional... 

Sanderson G, Scholfield CN (1986) Effects of adenosine uptake blockers and adenosine on evoked potentials of guinea-pig olfactory cortex. Pflugers Arch 406(l) 25-30 Sattin A, Rail TW (1970) The effect of adenosine and adenine nucleotides on the cyclic adenosine 3, 5 -phosphate content of guinea pig cerebral cortex slices. Mol Pharmacol 6(1) 13-23 Sawynok J, Zarrindast MR, Reid AR, Doak GJ (1997) Adenosine A3 receptor activation produces nociceptive behaviour and edema by release of histamine and 5-hydroxytryptamine. Eur J Pharmacol 333(1) 1-7... 

Feuerstein TJ, Seeger W (1997) Modulation of acetylcholine release in human cortical slices possible implications for Alzheimer s disease. Pharmacol Ther 74 333 17 Feuerstein TJ, Hertting G, Lupp A, Neufang B (1986) False labelling of dopaminergic terminals in the rabbit caudate nucleus uptake and release of [3H]-5-hydroxytryptamine. Br J Pharmacol 88 677-84... 

A molecule such as cyclic AMP, cyclic GMP or phosphatidylinositol that regulates intracellular processes in response to an extracellular signal. Uncontrolled or paroxysmal brain activity that is usually expressed through the motor system. Antidepressants such as fluoxetine and fluvoxamine that show specificity in inhibiting the uptake of 5-hydroxytryptamine into platelets or brain tissue in vitro and in vivo. 

Quinaux N, Scuvee-Moreau J, Dresse A. Inhibition of in vitro and ex vivo uptake of noradrenaline and 5-hydroxytryptamine by five antidepressants correlation with reduction of spontaneous firing rate of central monoaminergic neurones. Naunyn-Schmiedebergs Arch Pharmacol 1982 319 66-70. 

Differential scanning calorimetry has also been used to study the interaction of DPPC liposomes with the neuromediators norepinephrine and 5-hydroxytryptamine and four antidepressant drugs (imipramine, indalpine, citalopram, and milnacipran) known to inhibit uptake of these neurotransmitters [39]. Changes in the thermograms, transition temperature maximum, Tt, and ATt were determined as a function... 

Cyr, D., Gruner, S. Mettrick, D. F. (1983). Uptake of 5-hydroxytryptamine (serotonin), glucose and changes in worm glycogen levels. Canadian Journal of Zoology, 61 1469-74. 

Uptake of 5-hydroxytryptamine by Mesocestoides corti (Cestoda). Journal of Parasitology, 61 440-8. 

Rahman, M. S., Mettrick, D. F. Podesta, R. B. (1982). 5-Hydroxytryptamine, glucose uptake, glycogen utilization and carbon dioxide fixation in Hymenolepis microstoma (Cestoda). Comparative Biochemistry and Physiology, 73B 901-6. 

Simansky KJ, Vaidya AH (1990) Behavioral mechanisms for the anorectic action of the serotonin (5-HT) uptake inhibitor sertaline in rats comparison with directly acting 5-HT agonists. Brain Res Bull 25 953-960 Simmons RD, Blosser JC, Rosamond JR (1994) FPL 14294 A novel CCK-8 agonist with potent intranasal anorectic activity in the rat. Pharmacol Biochem Behav 47 701-708 Stevens R, Edwards S (1996) Effect of a 5-HT3 antagonist on peripheral 5-hydroxytryptamine-induced anorexia. Psychobiology 24 67-70... 

Serotonin or 5-hydroxytryptamine (5-HT), a monoamine, is widely distributed in many cells of the body and about 1-2% of the entire serotonin body content is found in the CNS. Serotonin is synthesized by the enzyme amino acid decarboxylase from 5-hydroxytryptophan (which is derived from tryptophan via tryptophan hydroxylase). The rate-limiting step is the production of 5-hydroxytryptophan by tryptophan hydroxylase. Serotonin is removed from the synapse by a high-affinity serotonin uptake site that is capable of transporting serotonin in either direction, depending on the concentration. 

BIMU 8 is a benzimidazole-carboxamide derivative, a selective (5-HT4-subtype) 5-hydroxytryptamine receptor AGONIST. It has experimental GASTRIC motility stimulant (gastroprokinetic) activity used as a pharmacological tool, binedaline [inn] (Scha 1659) is a phenylindole, a noradrenaline uptake inhibitor and antidepressant. Never marketed. 

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