| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Claire Scott, Ellen M Soffin, Matthew Hill, Peter J Atkinson, Christopher J Langmead, Paul B Wren, Stefania Faedo, Laurie J Gordon, Gary W Price, Steve Bromidge, Christopher N Johnson, James J Hagan, Jeannette Watso. SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue. European journal of pharmacology. vol 536. issue 1-2. 2006-07-25. PMID:16571351. |
sb-649915, a novel, potent 5-ht1a and 5-ht1b autoreceptor antagonist and 5-ht re-uptake inhibitor in native tissue. |
2006-07-25 |
2023-08-12 |
mouse |
| Claire Scott, Ellen M Soffin, Matthew Hill, Peter J Atkinson, Christopher J Langmead, Paul B Wren, Stefania Faedo, Laurie J Gordon, Gary W Price, Steve Bromidge, Christopher N Johnson, James J Hagan, Jeannette Watso. SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue. European journal of pharmacology. vol 536. issue 1-2. 2006-07-25. PMID:16571351. |
it has been proven that selective serotonin re-uptake inhibitors are effective antidepressants but the delay to therapeutic onset of these agents is thought to be due to the time required for 5-ht1a, and possibly 5-ht1b, autoreceptor desensitisation. |
2006-07-25 |
2023-08-12 |
mouse |
| Claire Scott, Ellen M Soffin, Matthew Hill, Peter J Atkinson, Christopher J Langmead, Paul B Wren, Stefania Faedo, Laurie J Gordon, Gary W Price, Steve Bromidge, Christopher N Johnson, James J Hagan, Jeannette Watso. SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue. European journal of pharmacology. vol 536. issue 1-2. 2006-07-25. PMID:16571351. |
therefore an agent incorporating 5-ht re-uptake inhibition coupled with 5-ht1a and/or 5-ht1b autoreceptor antagonism may provide a fast acting clinical agent. |
2006-07-25 |
2023-08-12 |
mouse |
| Claire Scott, Ellen M Soffin, Matthew Hill, Peter J Atkinson, Christopher J Langmead, Paul B Wren, Stefania Faedo, Laurie J Gordon, Gary W Price, Steve Bromidge, Christopher N Johnson, James J Hagan, Jeannette Watso. SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue. European journal of pharmacology. vol 536. issue 1-2. 2006-07-25. PMID:16571351. |
the current studies describe the in vitro profile of sb-649915 (6-[(1-{2-[(2-methylquinolin-5-yl)oxy]ethyl}piperidin-4-yl)methyl]-2h-1,4-benzoxazin-3(4h)-one), a novel compound which has high affinity for human recombinant 5-ht1a, 5-ht1b and 5-ht1d receptors (pki values of 8.6, 8.0, 8.8, respectively) and the human recombinant 5-ht transporter (pki value of 9.3). |
2006-07-25 |
2023-08-12 |
mouse |
| Claire Scott, Ellen M Soffin, Matthew Hill, Peter J Atkinson, Christopher J Langmead, Paul B Wren, Stefania Faedo, Laurie J Gordon, Gary W Price, Steve Bromidge, Christopher N Johnson, James J Hagan, Jeannette Watso. SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue. European journal of pharmacology. vol 536. issue 1-2. 2006-07-25. PMID:16571351. |
sb-649915 also displays high affinity for rat, guinea pig, mouse and marmoset native tissue 5-ht1a, 5-ht1b and 5-ht1d receptors and rat native tissue 5-ht transporters (pki values>or=7.5). |
2006-07-25 |
2023-08-12 |
mouse |
| Claire Scott, Ellen M Soffin, Matthew Hill, Peter J Atkinson, Christopher J Langmead, Paul B Wren, Stefania Faedo, Laurie J Gordon, Gary W Price, Steve Bromidge, Christopher N Johnson, James J Hagan, Jeannette Watso. SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue. European journal of pharmacology. vol 536. issue 1-2. 2006-07-25. PMID:16571351. |
in functional [35s]gtpgammas binding studies, sb-649915 (up to 1 microm) does not display intrinsic activity in hek293 cells expressing human recombinant 5-ht1a receptors but acts as a partial agonist at human recombinant 5-ht1b and 5-ht1d receptors with intrinsic activity values of 0.3 and 0.7, respectively, as compared to the full agonist 5-ht. |
2006-07-25 |
2023-08-12 |
mouse |
| Adrian Newman-Tancredi, Marie-Bernadette Assié, Nathalie Leduc, Anne-Marie Ormière, Nathalie Danty, Cristina Cos. Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia. The international journal of neuropsychopharmacology. vol 8. issue 3. 2006-07-19. PMID:15707540. |
novel antipsychotics activate recombinant human and native rat serotonin 5-ht1a receptors: affinity, efficacy and potential implications for treatment of schizophrenia. |
2006-07-19 |
2023-08-12 |
human |
| Adrian Newman-Tancredi, Marie-Bernadette Assié, Nathalie Leduc, Anne-Marie Ormière, Nathalie Danty, Cristina Cos. Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia. The international journal of neuropsychopharmacology. vol 8. issue 3. 2006-07-19. PMID:15707540. |
serotonin 5-ht1a receptors are promising targets in the management of schizophrenia but little information exists about affinity and efficacy of novel antipsychotics at these sites. |
2006-07-19 |
2023-08-12 |
human |
| Adrian Newman-Tancredi, Marie-Bernadette Assié, Nathalie Leduc, Anne-Marie Ormière, Nathalie Danty, Cristina Cos. Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia. The international journal of neuropsychopharmacology. vol 8. issue 3. 2006-07-19. PMID:15707540. |
e(max) values (% effect induced by 10 microm of 5-ht) for g-protein activation at rat brain 5-ht1a receptors: sarizotan (66.5), bifeprunox (35.9), ssr181507 (25.8), nemonapride (25.7), ziprasidone (20.6), slv313 (19), aripiprazole (15), tiospirone (8.9). |
2006-07-19 |
2023-08-12 |
human |
| Youichirou Ootsuka, William W Blessin. Activation of 5-HT1A receptors in rostral medullary raphé inhibits cutaneous vasoconstriction elicited by cold exposure in rabbits. Brain research. vol 1073-1074. 2006-07-19. PMID:16455061. |
in both conscious and anesthetized rabbits, we determined whether microinjection of a 5-hydroxytryptamine (5-ht) 1a receptor agonist 8-hydroxy-2-(di-n-propylaminio) tetralin (8-oh-dpat) into the medullary raphé/parapyramidal region inhibits thermoregulatory vasoconstriction and whether microinjection of a 5-ht1a receptor antagonist (n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)-n-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride) (way-100635) into the raphé reverses the cutaneous vasomotor changes induced by intravenous administration of 8-oh-dpat. |
2006-07-19 |
2023-08-12 |
Not clear |
| Hye-Jung Kim, Hyunah Choo, Yong Seo Cho, Hun Yeong Koh, Kyoung Tai No, Ae Nim Pa. Classification of dopamine, serotonin, and dual antagonists by decision trees. Bioorganic & medicinal chemistry. vol 14. issue 8. 2006-07-11. PMID:16387502. |
data set containing 1135 dopamine antagonists (d2, d3, and d4), 1251 serotonin antagonists (5-ht1a, 5-ht2a, and 5-ht2c), and 386 serotonin-dopamine dual antagonists was collected from the mddr database. |
2006-07-11 |
2023-08-12 |
Not clear |
| Elaine M Jagoda, Lixin Lang, Joji Tokugawa, Ashlie Simmons, Ying Ma, Carlo Contoreggi, Dale Kiesewetter, William C Eckelma. Development of 5-HT1A receptor radioligands to determine receptor density and changes in endogenous 5-HT. Synapse (New York, N.Y.). vol 59. issue 6. 2006-06-28. PMID:16440292. |
development of 5-ht1a receptor radioligands to determine receptor density and changes in endogenous 5-ht. |
2006-06-28 |
2023-08-12 |
mouse |
| Gabina Calderón-Rosete, Gonzalo Flores, Leonardo Rodríguez-Sos. Diurnal rhythm in the levels of the serotonin 5-HT1A receptors in the crayfish eyestalk. Synapse (New York, N.Y.). vol 59. issue 6. 2006-06-28. PMID:16447179. |
diurnal rhythm in the levels of the serotonin 5-ht1a receptors in the crayfish eyestalk. |
2006-06-28 |
2023-08-12 |
Not clear |
| Kumiko Takeuchi, Todd J Kohn, Nicholas A Honigschmidt, Vincent P Rocco, Patrick G Spinazze, Susan K Hemrick-Luecke, Linda K Thompson, David C Evans, Kurt Rasmussen, Deanna Koger, David Lodge, Laura J Martin, Janice Shaw, Penny G Threlkeld, David T Won. Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5. Bioorganic & medicinal chemistry letters. vol 16. issue 9. 2006-06-26. PMID:16298130. |
a series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-ht1a receptor antagonism and serotonin reuptake inhibition was discovered. |
2006-06-26 |
2023-08-12 |
Not clear |
| Kumiko Takeuchi, Todd J Kohn, Nicholas A Honigschmidt, Vincent P Rocco, Patrick G Spinazze, Susan K Hemrick-Luecke, Linda K Thompson, David C Evans, Kurt Rasmussen, Deanna Koger, David Lodge, Laura J Martin, Janice Shaw, Penny G Threlkeld, David T Won. Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5. Bioorganic & medicinal chemistry letters. vol 16. issue 9. 2006-06-26. PMID:16298130. |
1-(1h-indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high affinities at the 5-ht1a receptor and serotonin reuptake site in vitro. |
2006-06-26 |
2023-08-12 |
Not clear |
| Kumiko Takeuchi, Todd J Kohn, Nicholas A Honigschmidt, Vincent P Rocco, Patrick G Spinazze, Susan K Hemrick-Luecke, Linda K Thompson, David C Evans, Kurt Rasmussen, Deanna Koger, David Lodge, Laura J Martin, Janice Shaw, Penny G Threlkeld, David T Won. Advances toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT1A receptor antagonism/SSRI activities. Part 5. Bioorganic & medicinal chemistry letters. vol 16. issue 9. 2006-06-26. PMID:16298130. |
in vivo evaluation of this series of compounds demonstrated elevated extracellular serotonin levels from the basal and quick recovery of neuron firing that was presumably suppressed by the initial acute activation of 5-ht1a somatodendritic autoreceptors. |
2006-06-26 |
2023-08-12 |
Not clear |
| Jeanne Lanoir, Gerard Hilaire, Isabelle Sei. Reduced density of functional 5-HT1A receptors in the brain, medulla and spinal cord of monoamine oxidase-A knockout mouse neonates. The Journal of comparative neurology. vol 495. issue 5. 2006-06-26. PMID:16498683. |
abnormally high brain 5-ht levels in monoamine oxidase-a knockout (mao-a ko) mouse neonates raise the question of whether the distribution and density of the 5-ht1a receptors (5-ht1ar) expressed in the brain by postnatal day p7 are affected and, if so, whether the 5-ht1a autoreceptors in the dorsal raphe are modified in the same way as the postsynaptic 5-ht1ar present in raphe target structures. |
2006-06-26 |
2023-08-12 |
mouse |
| A C E Linthors. Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handbook of experimental pharmacology. issue 169. 2006-06-13. PMID:16594259. |
although the picture is far from complete yet--partly due to the large number of serotonin (5-ht) receptors and the often-disparate effects of receptor agonists and antagonists in animal models of anxiety--ssris and the 5-ht1a agonist buspirone have now earned their place in the treatment of anxiety disorders. |
2006-06-13 |
2023-08-12 |
Not clear |
| Helen Rosengarten, Gerd D Bartoszyk, David Quartermain, Yan Li. The effect of chronic administration of sarizotan, 5-HT1A agonist/D3/D4 ligand, on haloperidol-induced repetitive jaw movements in rat model of tardive dyskinesia. Progress in neuro-psychopharmacology & biological psychiatry. vol 30. issue 2. 2006-06-08. PMID:16229932. |
sarizotan, a serotonin 5-ht1a receptor agonist and dopamine receptor ligand. |
2006-06-08 |
2023-08-12 |
rat |
| Scott M Rawls, Alan Cowa. Modulation of delta opioid-evoked hypothermia in rats by WAY 100635 and fluoxetine. Neuroscience letters. vol 398. issue 3. 2006-06-08. PMID:16483716. |
the present data reveal that 5-ht1a receptor activation mediates a significant proportion of the hypothermic response to delta opioid receptor activation and that a 5-ht uptake blockade potentiates delta receptor-induced hypothermia. |
2006-06-08 |
2023-08-12 |
rat |