| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Dahui Zhou, Gary P Stack, Jennifer Lo, Amedeo A Failli, Deborah A Evrard, Boyd L Harrison, Nicole T Hatzenbuhler, Megan Tran, Susan Croce, Soo Yi, Jeannette Golembieski, Geoffrey A Hornby, Margaret Lai, Qian Lin, Lee E Schechter, Deborah L Smith, Adam D Shilling, Christine Huselton, Paul Mitchell, Chad E Beyer, Terrance H Andre. Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. Journal of medicinal chemistry. vol 52. issue 15. 2009-09-21. PMID:19719241. |
on the basis of the previously reported clinical candidate, ssa-426 (1), a series of related 2-piperazin-1-ylquinoline derivatives 3-16 were synthesized and evaluated as dual-acting serotonin (5-ht) reuptake inhibitors and 5-ht1a receptor antagonists. |
2009-09-21 |
2023-08-12 |
Not clear |
| Dahui Zhou, Gary P Stack, Jennifer Lo, Amedeo A Failli, Deborah A Evrard, Boyd L Harrison, Nicole T Hatzenbuhler, Megan Tran, Susan Croce, Soo Yi, Jeannette Golembieski, Geoffrey A Hornby, Margaret Lai, Qian Lin, Lee E Schechter, Deborah L Smith, Adam D Shilling, Christine Huselton, Paul Mitchell, Chad E Beyer, Terrance H Andre. Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists. Journal of medicinal chemistry. vol 52. issue 15. 2009-09-21. PMID:19719241. |
in particular, compound 7 exhibits potent functional activities at both the 5-ht transporter and 5-ht1a receptor, good selectivity over the alpha1-adrenergic and dopaminergic receptors, acceptable pharmacokinetic properties, and a favorable in vivo profile. |
2009-09-21 |
2023-08-12 |
Not clear |
| Nathalie M Goodfellow, Madhurima Benekareddy, Vidita A Vaidya, Evelyn K Lamb. Layer II/III of the prefrontal cortex: Inhibition by the serotonin 5-HT1A receptor in development and stress. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 29. issue 32. 2009-09-08. PMID:19675243. |
layer ii/iii of the prefrontal cortex: inhibition by the serotonin 5-ht1a receptor in development and stress. |
2009-09-08 |
2023-08-12 |
human |
| Amélie Lothe, Claudette Boni, Nicolas Costes, Philip Gorwood, Sandrine Bouvard, Didier Le Bars, Franck Lavenne, Philippe Ryvli. Association between triallelic polymorphism of the serotonin transporter and [18F]MPPF binding potential at 5-HT1A receptors in healthy subjects. NeuroImage. vol 47. issue 2. 2009-09-03. PMID:19409499. |
association between triallelic polymorphism of the serotonin transporter and [18f]mppf binding potential at 5-ht1a receptors in healthy subjects. |
2009-09-03 |
2023-08-12 |
human |
| Amélie Lothe, Claudette Boni, Nicolas Costes, Philip Gorwood, Sandrine Bouvard, Didier Le Bars, Franck Lavenne, Philippe Ryvli. Association between triallelic polymorphism of the serotonin transporter and [18F]MPPF binding potential at 5-HT1A receptors in healthy subjects. NeuroImage. vol 47. issue 2. 2009-09-03. PMID:19409499. |
the greater [(18)f]mppf bp(nd) observed in women homozygote carriers of the s allele could either reflect a greater 5-ht1a receptor density or a lower extracellular concentration of 5-ht. |
2009-09-03 |
2023-08-12 |
human |
| T G Noskova, A V Kazantseva, A E Gareeva, D A Gaĭsina, S U Tuktarova, E K Khusnutdinov. [Association of several polymorphic loci of serotoninergic genes with unipolar depression]. Genetika. vol 45. issue 6. 2009-08-28. PMID:19639876. |
using pcr-rflp analysis, we have conducted a study of polymorphic loci of several genes of this system: c1019g of serotonin receptor 1a gene, (htr1a); a438g of serotonin receptor 2a gene, (htr2a); g861c of serotonin receptor 1b gene, (htr1b); stin2vntr and 5-httlpr of serotonin transporter gene (slc6a4) in patients with unipolar depression among ethnic tatars and russians. |
2009-08-28 |
2023-08-12 |
Not clear |
| M A Cooper, M S Grober, C R Nicholas, K L Huhma. Aggressive encounters alter the activation of serotonergic neurons and the expression of 5-HT1A mRNA in the hamster dorsal raphe nucleus. Neuroscience. vol 161. issue 3. 2009-08-24. PMID:19362123. |
our results support the hypothesis that social stress can activate 5-ht neurons in the drn, reduce 5-ht1a autoreceptor-mediated inhibition, and lead to hyperactivity of 5-ht neurons. |
2009-08-24 |
2023-08-12 |
Not clear |
| Eduard Badarau, Franck Suzenet, Andrzej J Bojarski, Adriana-Luminiţa Fînaru, Gérald Guillaume. Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation. Bioorganic & medicinal chemistry letters. vol 19. issue 6. 2009-08-20. PMID:19237285. |
benzimidazolone-based serotonin 5-ht1a or 5-ht7r ligands: synthesis and biological evaluation. |
2009-08-20 |
2023-08-12 |
Not clear |
| Eleonora Calcagno, Sara Guzzetti, Alessandro Canetta, Claudia Fracasso, Silvio Caccia, Luigi Cervo, Roberto W Invernizz. Enhancement of cortical extracellular 5-HT by 5-HT1A and 5-HT2C receptor blockade restores the antidepressant-like effect of citalopram in non-responder mice. The international journal of neuropsychopharmacology. vol 12. issue 6. 2009-08-18. PMID:19123962. |
enhancement of cortical extracellular 5-ht by 5-ht1a and 5-ht2c receptor blockade restores the antidepressant-like effect of citalopram in non-responder mice. |
2009-08-18 |
2023-08-12 |
mouse |
| Eleonora Calcagno, Sara Guzzetti, Alessandro Canetta, Claudia Fracasso, Silvio Caccia, Luigi Cervo, Roberto W Invernizz. Enhancement of cortical extracellular 5-HT by 5-HT1A and 5-HT2C receptor blockade restores the antidepressant-like effect of citalopram in non-responder mice. The international journal of neuropsychopharmacology. vol 12. issue 6. 2009-08-18. PMID:19123962. |
we employed intracerebral microdialysis, fst and selective antagonists of 5-ht1a and 5-ht2c receptors to investigate whether enhancing the increase in extracellular 5-ht reinstated the anti-immobility effect of citalopram in the fst. |
2009-08-18 |
2023-08-12 |
mouse |
| Eleonora Calcagno, Sara Guzzetti, Alessandro Canetta, Claudia Fracasso, Silvio Caccia, Luigi Cervo, Roberto W Invernizz. Enhancement of cortical extracellular 5-HT by 5-HT1A and 5-HT2C receptor blockade restores the antidepressant-like effect of citalopram in non-responder mice. The international journal of neuropsychopharmacology. vol 12. issue 6. 2009-08-18. PMID:19123962. |
way 100635 (0.3 mg/kg s.c.) or sb 242084 (1 mg/kg s.c.), respectively a selective 5-ht1a and 5-ht2c receptor antagonist, raised the effect of citalopram (5 mg/kg) on extracellular 5-ht in the medial prefrontal cortex of dba/2n mice (citalopram alone 5.2+/-0.3 fmol/20 microl, way 100635+citalopram 9.9+/-2.1 fmol/20 microl, sb 242084+ citalopram 7.6+/-1.0 fmol/20 microl) to the level reached in 'responder' mice given citalopram alone. |
2009-08-18 |
2023-08-12 |
mouse |
| Eleonora Calcagno, Sara Guzzetti, Alessandro Canetta, Claudia Fracasso, Silvio Caccia, Luigi Cervo, Roberto W Invernizz. Enhancement of cortical extracellular 5-HT by 5-HT1A and 5-HT2C receptor blockade restores the antidepressant-like effect of citalopram in non-responder mice. The international journal of neuropsychopharmacology. vol 12. issue 6. 2009-08-18. PMID:19123962. |
the results confirm that impaired 5-ht transmission accounts for the lack of effect of citalopram in the fst and suggest that enhancing the effect of ssris on extracellular 5-ht, through selective blockade of 5-ht1a and 5-ht2c receptors, could be a useful strategy to restore the response in treatment-resistant depression. |
2009-08-18 |
2023-08-12 |
mouse |
| Jacqueline Borg, Susanne Henningsson, Tomoyuki Saijo, Makoto Inoue, Jessica Bah, Lars Westberg, Johan Lundberg, Hristina Jovanovic, Bengt Andrée, Anna-Lena Nordstrom, Christer Halldin, Elias Eriksson, Lars Fard. Serotonin transporter genotype is associated with cognitive performance but not regional 5-HT1A receptor binding in humans. The international journal of neuropsychopharmacology. vol 12. issue 6. 2009-08-18. PMID:19126263. |
serotonin transporter genotype is associated with cognitive performance but not regional 5-ht1a receptor binding in humans. |
2009-08-18 |
2023-08-12 |
human |
| M Catalina Cervantes, Yvon Delvill. Serotonin 5-HT1A and 5-HT3 receptors in an impulsive-aggressive phenotype. Behavioral neuroscience. vol 123. issue 3. 2009-08-13. PMID:19485565. |
serotonin 5-ht1a and 5-ht3 receptors in an impulsive-aggressive phenotype. |
2009-08-13 |
2023-08-12 |
Not clear |
| M Catalina Cervantes, Yvon Delvill. Serotonin 5-HT1A and 5-HT3 receptors in an impulsive-aggressive phenotype. Behavioral neuroscience. vol 123. issue 3. 2009-08-13. PMID:19485565. |
as serotonin 1a (5-ht1a) receptors participate in the inhibition of aggression, whereas 5-ht3 receptor activation facilitates aggression, the authors hypothesized that differences in their expression are associated with differences in behavior. |
2009-08-13 |
2023-08-12 |
Not clear |
| M Catalina Cervantes, Yvon Delvill. Serotonin 5-HT1A and 5-HT3 receptors in an impulsive-aggressive phenotype. Behavioral neuroscience. vol 123. issue 3. 2009-08-13. PMID:19485565. |
although the authors observed a greater density of 5-ht1a receptor immunoreactivity in h-agg hamsters within several areas, it appears to be related to a lack of serotonin release, as supported by further observations of decreased immunoreactive perikarya and 5-ht1a receptors in fluoxetine-treated hamsters. |
2009-08-13 |
2023-08-12 |
Not clear |
| M Catalina Cervantes, Yvon Delvill. Serotonin 5-HT1A and 5-HT3 receptors in an impulsive-aggressive phenotype. Behavioral neuroscience. vol 123. issue 3. 2009-08-13. PMID:19485565. |
the data indicate a convergence of impulsive and aggressive characteristics to one phenotype that is associated with various aspects of serotonin function, such as serotonin release and differential expression of 5-ht1a and 5-ht3 receptors. |
2009-08-13 |
2023-08-12 |
Not clear |
| Taku Nagai, Rina Murai, Kanae Matsui, Hiroyuki Kamei, Yukihiro Noda, Hiroshi Furukawa, Toshitaka Nabeshim. Aripiprazole ameliorates phencyclidine-induced impairment of recognition memory through dopamine D1 and serotonin 5-HT1A receptors. Psychopharmacology. vol 202. issue 1-3. 2009-08-05. PMID:18679658. |
aripiprazole ameliorates phencyclidine-induced impairment of recognition memory through dopamine d1 and serotonin 5-ht1a receptors. |
2009-08-05 |
2023-08-12 |
Not clear |
| Anh Dzung Lê, Douglas Funk, Stephen Harding, Walter Juzytsch, Paul J Fletche. The role of noradrenaline and 5-hydroxytryptamine in yohimbine-induced increases in alcohol-seeking in rats. Psychopharmacology. vol 204. issue 3. 2009-08-05. PMID:19229522. |
yohimbine also acts as an agonist of 5-hydroxytryptamine (5-ht) 5-ht1a receptors, which have been shown to be involved in alcohol seeking. |
2009-08-05 |
2023-08-12 |
rat |
| R Iceta, J E Mesonero, J J Aramayona, A I Alcald. Expression of 5-HT1A and 5-HT7 receptors in Caco-2 cells and their role in the regulation of serotonin transporter activity. Journal of physiology and pharmacology : an official journal of the Polish Physiological Society. vol 60. issue 1. 2009-07-20. PMID:19439818. |
expression of 5-ht1a and 5-ht7 receptors in caco-2 cells and their role in the regulation of serotonin transporter activity. |
2009-07-20 |
2023-08-12 |
human |