| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| J Martínez-Esparza, A M Oficialdegui, S Pérez-Silanes, B Heras, L Orús, J A Palop, B Lasheras, J Roca, M Mourelle, A Bosch, J C Del Castillo, R Tordera, J Del Río, A Mong. New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. Journal of medicinal chemistry. vol 44. issue 3. 2001-08-02. PMID:11462981. |
in a search toward new and efficient antidepressants, 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives were designed, synthesized, and evaluated for 5-ht reuptake inhibition and 5-ht1a receptor antagonism. |
2001-08-02 |
2023-08-12 |
mouse |
| J Martínez-Esparza, A M Oficialdegui, S Pérez-Silanes, B Heras, L Orús, J A Palop, B Lasheras, J Roca, M Mourelle, A Bosch, J C Del Castillo, R Tordera, J Del Río, A Mong. New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. Journal of medicinal chemistry. vol 44. issue 3. 2001-08-02. PMID:11462981. |
the design was based on coupling structural moieties related to inhibition of serotonin reuptake, such as gamma-phenoxypropylamines, to arylpiperazines, typical 5-ht1a ligands. |
2001-08-02 |
2023-08-12 |
mouse |
| J Martínez-Esparza, A M Oficialdegui, S Pérez-Silanes, B Heras, L Orús, J A Palop, B Lasheras, J Roca, M Mourelle, A Bosch, J C Del Castillo, R Tordera, J Del Río, A Mong. New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. Journal of medicinal chemistry. vol 44. issue 3. 2001-08-02. PMID:11462981. |
in binding studies, several compounds showed affinity at the 5-ht transporter and 5-ht1a receptors. |
2001-08-02 |
2023-08-12 |
mouse |
| J Martínez-Esparza, A M Oficialdegui, S Pérez-Silanes, B Heras, L Orús, J A Palop, B Lasheras, J Roca, M Mourelle, A Bosch, J C Del Castillo, R Tordera, J Del Río, A Mong. New 1-aryl-3-(4-arylpiperazin-1-yl)propane derivatives, with dual action at 5-HT1A serotonin receptors and serotonin transporter, as a new class of antidepressants. Journal of medicinal chemistry. vol 44. issue 3. 2001-08-02. PMID:11462981. |
among these three compounds, 28b (1-benzo[b]thiophene-3-yl)-3-[4-(2-methoxyphenyl)-1-ylpropan-1-ol) showed the higher affinity at both the 5-ht transporter and 5-ht1a receptors (ki = 20 nm in both cases) and was also active in the other pharmacological tests. |
2001-08-02 |
2023-08-12 |
mouse |
| B N Smith, P J Sollars, F E Dudek, G E Pickar. Serotonergic modulation of retinal input to the mouse suprachiasmatic nucleus mediated by 5-HT1B and 5-HT7 receptors. Journal of biological rhythms. vol 16. issue 1. 2001-07-26. PMID:11220775. |
this effect of 8-oh-dpat was minimally attenuated by the selective 5-ht1a receptor antagonist way 100635 but was reversibly and significantly reduced in the presence of ritanserin, a mixed 5-ht(2/7) receptor antagonist. |
2001-07-26 |
2023-08-12 |
mouse |
| Y Zhang, Z Yang, X Gao, G W. The role of 5-hydroxytryptamine1A and 5-hydroxytryptamine1B receptors in modulating spinal nociceptive transmission in normal and carrageenan-injected rats. Pain. vol 92. issue 1-2. 2001-07-26. PMID:11323141. |
intrathecal injection of the 5-hydroxytryptamine(1a) (5-ht1a) receptor agonist 8-hydroxy-dpat hydroxybromide (8-oh-dpat) (0.305, 1.525, 3.05, and 15.25 mm) dose-dependently increased adelta- and c-responses and post-discharge in most of the wdr neurons. |
2001-07-26 |
2023-08-12 |
rat |
| Y Zhang, Z Yang, X Gao, G W. The role of 5-hydroxytryptamine1A and 5-hydroxytryptamine1B receptors in modulating spinal nociceptive transmission in normal and carrageenan-injected rats. Pain. vol 92. issue 1-2. 2001-07-26. PMID:11323141. |
these data suggest that 5-ht1a and 5-ht1b receptor subtypes mediate the facilitatory effect of 5-ht on nociceptive processing in the spinal cord of rats. |
2001-07-26 |
2023-08-12 |
rat |
| M M Fernández, E Calama, A Morán, M L Martín, L San Romá. Characterization of mechanisms involved in presynaptic inhibition of sympathetic pressor effects induced by some 5-HT1 receptor antagonists. Journal of autonomic pharmacology. vol 20. issue 5-6. 2001-07-26. PMID:11350497. |
in a previous study, we showed that the presynaptic inhibitory action of 5-hydroxytryptamine receptor agonists on sympathetic pressor effects obtained in the pithed rats were mainly mediated by activation of 5-ht1a and 5-ht1d receptor subtypes. |
2001-07-26 |
2023-08-12 |
rat |
| P Blie. Pharmacology of rapid-onset antidepressant treatment strategies. The Journal of clinical psychiatry. vol 62 Suppl 15. 2001-07-26. PMID:11444761. |
the increase in synaptic 5-ht activates feedback mechanisms mediated by 5-ht1a (cell body) and 5-ht1b (terminal) autoreceptors, which, respectively, reduce the firing in 5-ht neurons and decrease the amount of 5-ht released per action potential resulting in attenuated 5-ht neurotransmission. |
2001-07-26 |
2023-08-12 |
Not clear |
| P Blie. Pharmacology of rapid-onset antidepressant treatment strategies. The Journal of clinical psychiatry. vol 62 Suppl 15. 2001-07-26. PMID:11444761. |
the addition of pindolol, which blocks 5-ht1a receptors, to ssri treatment decouples the feedback inhibition of 5-ht neuron firing and accelerates and enhances the antidepressant response. |
2001-07-26 |
2023-08-12 |
Not clear |
| C Cidis Meltzer, W C Drevets, J C Price, C A Mathis, B Lopresti, P J Greer, V L Villemagne, D Holt, N S Mason, P R Houck, C F Reynolds, S T DeKosk. Gender-specific aging effects on the serotonin 1A receptor. Brain research. vol 895. issue 1-2. 2001-07-19. PMID:11259754. |
of particular interest is the serotonin type-1a (5-ht1a) receptor, due to its putative role in mediating the therapeutic efficacy of antidepressant treatment. |
2001-07-19 |
2023-08-12 |
human |
| H Sánchez, D N Velázquez-Martíne. Discriminative stimulus properties of indorenate, a 5-HT1A, 5-HT1B and 5-HT2C agonist: a study in rats. Journal of psychopharmacology (Oxford, England). vol 15. issue 1. 2001-07-19. PMID:11277605. |
generalization to the discriminative stimulus properties of indo was observed with the 5-ht1a receptor agonist 8-oh-dpat (1.0 mg/kg produced 90% generalization) and the 5-ht(1b/2c) receptor agonist 1-(3-trifluoromethylphenyl) piperazine (tfmpp) (3.0 mg/kg produced up to 75% generalization). |
2001-07-19 |
2023-08-12 |
rat |
| H Sánchez, D N Velázquez-Martíne. Discriminative stimulus properties of indorenate, a 5-HT1A, 5-HT1B and 5-HT2C agonist: a study in rats. Journal of psychopharmacology (Oxford, England). vol 15. issue 1. 2001-07-19. PMID:11277605. |
the results suggest that indo acts as an agonist at 5-ht1a receptor sites, but its activity at 5-ht(1b/2c) receptor sites also contributes to its discriminative function. |
2001-07-19 |
2023-08-12 |
rat |
| F Borsini, A Brambilla, R Cesana, N Gripp. Lack of interaction between flibanserin and antidepressants in inducing serotonergic syndrome in rats. The international journal of neuropsychopharmacology. vol 4. issue 1. 2001-07-19. PMID:11343624. |
this study was aimed at evaluating the ability of flibanserin, a 5-ht1a receptor full agonist with antidepressant potential, to induce the 5-ht syndrome (flat body posture, hindlimb abduction and forepaw treading) in rats previously administered with clinically active antidepressants imipramine, fluoxetine or paroxetine. |
2001-07-19 |
2023-08-12 |
rat |
| J Tauscher, N P Verhoeff, B K Christensen, D Hussey, J H Meyer, A Kecojevic, M Javanmard, S Kasper, S Kapu. Serotonin 5-HT1A receptor binding potential declines with age as measured by [11C]WAY-100635 and PET. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. vol 24. issue 5. 2001-07-12. PMID:11282252. |
serotonin 5-ht1a receptor binding potential declines with age as measured by [11c]way-100635 and pet. |
2001-07-12 |
2023-08-12 |
human |
| M D Doherty, V M Picke. Targeting of serotonin 1A receptors to dopaminergic neurons within the parabrachial subdivision of the ventral tegmental area in rat brain. The Journal of comparative neurology. vol 433. issue 3. 2001-07-12. PMID:11298363. |
serotonin (5-hydroxytryptamine [5-ht]) modulates dopamine-related cognitive functions and motor activity through activation of selective receptor subtypes including 5-ht1a. |
2001-07-12 |
2023-08-12 |
rat |
| M I Granoff, C R Ashb. Effect of the repeated administration of (+/-)-3,4-methylenedioxymethamphetamine on the behavioral response of rats to the 5-HT1A receptor agonist (+/-)-8-hydroxy-(di-n-propylamino)tetralin. Neuropsychobiology. vol 43. issue 1. 2001-07-05. PMID:11150898. |
overall, our results suggest that the depletion of 5-ht levels by the repeated administration of mdma does not produce a supersensitivity of central 5-ht1a receptors in the rat as determined via our approach. |
2001-07-05 |
2023-08-12 |
rat |
| Q Lei, E M Talley, D A Baylis. Receptor-mediated inhibition of G protein-coupled inwardly rectifying potassium channels involves G(alpha)q family subunits, phospholipase C, and a readily diffusible messenger. The Journal of biological chemistry. vol 276. issue 20. 2001-07-05. PMID:11279027. |
in cells transiently or stably cotransfected with 5-ht1a (g(alpha)i/o-coupled) and trh-r1 (g(alpha)q-coupled) receptors, 5-ht (5-hydroxytryptamine; serotonin) enhanced girk channel currents, whereas thyrotropin-releasing hormone (trh) inhibited both basal and 5-ht-activated girk channel currents. |
2001-07-05 |
2023-08-12 |
Not clear |
| U Laban, D Kurrasch-Orbaugh, D Marona-Lewicka, D E Nichol. A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties. Bioorganic & medicinal chemistry letters. vol 11. issue 6. 2001-06-28. PMID:11277522. |
a novel fluorinated tryptamine with highly potent serotonin 5-ht1a receptor agonist properties. |
2001-06-28 |
2023-08-12 |
Not clear |
| U Laban, D Kurrasch-Orbaugh, D Marona-Lewicka, D E Nichol. A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties. Bioorganic & medicinal chemistry letters. vol 11. issue 6. 2001-06-28. PMID:11277522. |
this new compound 1-(4-fluoro-5-methoxyindol-3-yl)pyrrolidine (2) was found to be a potent serotonin 5-ht1a agonist. |
2001-06-28 |
2023-08-12 |
Not clear |