| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Jesper Bornø Jensen, Kristian Gaarn du Jardin, Dekun Song, David Budac, Gennady Smagin, Connie Sanchez, Alan Lars Pehrso. Vortioxetine, but not escitalopram or duloxetine, reverses memory impairment induced by central 5-HT depletion in rats: evidence for direct 5-HT receptor modulation. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. vol 24. issue 1. 2014-09-12. PMID:24284262. |
the investigational multimodal acting antidepressant vortioxetine is a 5-ht3, 5-ht7 and 5-ht1d receptor antagonist, 5-ht1b receptor partial agonist, 5-ht1a receptor agonist and 5-ht transporter (sert) inhibitor that enhances memory in normal rats in novel object recognition (nor) and conditioned fear (mørk et al., 2013). |
2014-09-12 |
2023-08-12 |
rat |
| C Cervantes-Durán, H I Rocha-González, V Granados-Sot. Peripheral and spinal 5-HT receptors participate in the pronociceptive and antinociceptive effects of fluoxetine in rats. Neuroscience. vol 252. 2014-06-11. PMID:23994595. |
the peripheral pronociceptive effect of fluoxetine was prevented by the 5-ht2a (ketanserin, 3-10 pmol/paw), 5-ht2b (3-(2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl)-2,4(1h,3h)-quinazolinedione(+) tartrate, rs-127445, 3-10 pmol/paw), 5-ht2c (8-[5-(2,4-dimethoxy-5-(4-trifluoromethylphenylsulphonamido) phenyl-5-oxopentyl]1,3,8-triazaspiro[4.5] decane-2,4-dione hydrochloride, rs-102221, 3-10 pmol/paw), 5-ht3 (ondansetron, 3-10 nmol/paw), 5-ht4 ([1-[2-methylsulphonylamino ethyl]-4-piperidinyl]methyl 1-methyl-1h-indole-3-carboxylate, gr-113808, 3-100 fmol/paw), 5-ht6 (4-iodo-n-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]benzene-sulfonamide hydrochloride, sb-258585, 3-10 pmol/paw) and 5-ht7 ((r)-3-(2-(2-(4-methylpiperidin-1-yl) ethyl) pyrrolidine-1-sulfonyl) phenol hydrochloride, sb-269970, 0.3-1 nmol/paw), but not by the 5-ht1a (n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-2-pyridinylcyclohexanecarboxamide maleate, way-100635, 0.3-1 nmol/paw), 5-ht1b/1d (n-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1'-biphenyl-4-carboxamide hydrochloride hydrate, gr-127935, 0.3-1 nmol/paw), 5-ht1b (1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine hydrochloride, sb-224289, 0.3-1 nmol/paw), 5-ht1d (4-(3-chlorophenyl)-α-(diphenylmethyl)-1-piperazineethanol hydrochloride, brl-15572, 0.3-1nmol/paw) nor 5-ht5a ((n-[2-(dimethylamino)ethyl]-n-[[4'-[[(2-phenylethyl)amino]methyl][1,1'-biphenyl]-4-yl]methyl]cyclopentanepropanamide dihydrochloride, sb-699551, 1-3 nmol/paw), receptor antagonists. |
2014-06-11 |
2023-08-12 |
rat |
| C Cervantes-Durán, H I Rocha-González, V Granados-Sot. Peripheral and spinal 5-HT receptors participate in the pronociceptive and antinociceptive effects of fluoxetine in rats. Neuroscience. vol 252. 2014-06-11. PMID:23994595. |
in marked contrast, the spinal antinociceptive effect of fluoxetine was prevented by the 5-ht1a (way-100635, 0.3-1 nmol/rat), 5-ht1b/1d (gr-127935, 0.3-1 nmol/rat), 5-ht1b (sb-224289, 0.3-1 nmol/rat), 5-ht1d (brl-15572, 0.3-1 nmol/rat) and 5-ht5a (sb-699551, 1-3 nmol/rat), but not by the 5-ht2a (ketanserin, 3-10 pmol/rat), 5-ht2b (rs-127445, 3-10 pmol/rat), 5-ht2c (rs-102221, 3-10 pmol/rat), 5-ht3 (ondansetron, 3-10 nmol/rat), 5-ht4 (gr-113808, 3-100 fmol/rat), 5-ht6 (sb-258585, 3-10 pmol/rat) nor 5-ht7 (sb-269970, 0.3-1 nmol/rat), receptor antagonists. |
2014-06-11 |
2023-08-12 |
rat |
| Colin P Leslie, Matteo Biagetti, Silvia Bison, Steven M Bromidge, Romano Di Fabio, Daniele Donati, Alessandro Falchi, Martine J Garnier, Albert Jaxa-Chamiec, Gary Manchee, Giancarlo Merlo, Domenica A Pizzi, Luigi P Stasi, Jessica Tibasco, Antonio Vong, Simon E Ward, Laura Zonzin. Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist. Journal of medicinal chemistry. vol 53. issue 23. 2014-04-15. PMID:21053897. |
a novel series of compounds was identified showing low intrinsic activities and potent affinities across the 5-ht1a, 5-ht1b, and 5-ht1d receptors as well as high selectivity against the serotonin transporter. |
2014-04-15 |
2023-08-12 |
Not clear |
| A Dhi. Vortioxetine for the treatment of major depression. Drugs of today (Barcelona, Spain : 1998). vol 49. issue 12. 2014-03-10. PMID:24524096. |
it inhibits the activity of serotonin transporters and is an agonist of serotonin 5-ht1a receptor, partial agonist of 5-ht1b and antagonist of 5-ht3a, 5-ht7 and 5-ht1d receptors. |
2014-03-10 |
2023-08-12 |
Not clear |
| Jean-François Perrier, Hanne Borger Rasmussen, Rasmus Kordt Christensen, Anders Victor Peterse. Modulation of the intrinsic properties of motoneurons by serotonin. Current pharmaceutical design. vol 19. issue 24. 2014-01-27. PMID:23360270. |
the somato-dendritic compartments of motoneurons are densely innervated by serotonergic synaptic boutons and several receptors are expressed in the membrane of motoneurons including 5-ht1a, 5-ht1b, 5-ht1d, 5-ht2a, 5-ht2b, 5-ht2c and 5-ht5a. |
2014-01-27 |
2023-08-12 |
Not clear |
| Stephen D Silberstein, Shashidhar H Kor. Dihydroergotamine: a review of formulation approaches for the acute treatment of migraine. CNS drugs. vol 27. issue 5. 2013-10-28. PMID:23620146. |
dhe is a potent agonist at serotonin 5-ht1b and 5-ht1d receptors. |
2013-10-28 |
2023-08-12 |
Not clear |
| Arne Mørk, Liliana P Montezinho, Silke Miller, Crista Trippodi-Murphy, Niels Plath, Yan Li, Maria Gulinello, Connie Sanche. Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacology, biochemistry, and behavior. vol 105. 2013-10-23. PMID:23380522. |
vortioxetine (lu aa21004) in development as a novel multimodal antidepressant is a 5-ht3, 5-ht7 and 5-ht1d receptor antagonist, a 5-ht1b receptor partial agonist, a 5-ht1a receptor agonist and a 5-ht transporter (5-htt) inhibitor in vitro. |
2013-10-23 |
2023-08-12 |
rat |
| Dimos D Mitsikostas, Peer Tfelt-Hanse. Targeting to 5-HT1F receptor subtype for migraine treatment: lessons from the past, implications for the future. Central nervous system agents in medicinal chemistry. vol 12. issue 4. 2013-06-06. PMID:22934751. |
the effective anti-migraine drugs triptans, all bind with high affinity to three serotonin (5-ht) subtypes, the 5-ht1b, 5-ht1d and 5-ht1f. |
2013-06-06 |
2023-08-12 |
human |
| Khanum Ridler, Christophe Plisson, Eugenii A Rabiner, Roger N Gunn, Balu Easwaramoorthy, Anissa Abi-Dargham, Marc Laruelle, Mark Slifstei. Characterization of in vivo pharmacological properties and sensitivity to endogenous serotonin of [11C] P943: a positron emission tomography study in Papio anubis. Synapse (New York, N.Y.). vol 65. issue 11. 2012-06-18. PMID:21538549. |
we characterized a number of its in vivo pharmacokinetic properties, including the evaluation of its two stereo-isomers, saturability of specific binding, selectivity for 5-ht1b and 5-ht1d receptors, and vulnerability to pharmacologically induced increases in endogenous 5-ht levels. |
2012-06-18 |
2023-08-12 |
human |
| Khanum Ridler, Christophe Plisson, Eugenii A Rabiner, Roger N Gunn, Balu Easwaramoorthy, Anissa Abi-Dargham, Marc Laruelle, Mark Slifstei. Characterization of in vivo pharmacological properties and sensitivity to endogenous serotonin of [11C] P943: a positron emission tomography study in Papio anubis. Synapse (New York, N.Y.). vol 65. issue 11. 2012-06-18. PMID:21538549. |
the interventions included the administration of pharmacological doses of p943, sb-616234-s (a 5-ht1b selective antagonist), sb-714786 (a 5-ht1d selective antagonist), as well as the administration of 5-ht releasing agents (fenfluramine, amphetamine) and 5-ht reuptake inhibitor (citalopram). |
2012-06-18 |
2023-08-12 |
human |
| Rosa I Caamaño Tubío, Jorge Pérez-Maceira, Manuel Aldegund. Homeostasis of glucose in the rainbow trout (Oncorhynchus mykiss Walbaum): the role of serotonin. The Journal of experimental biology. vol 213. issue 11. 2010-08-17. PMID:20472767. |
administration of tfmpp (a 5-ht1b agonist) did not increase the plasma levels of glucose, and the hyperglycaemic action of 5-ht was not blocked by antagonists of 5-ht1a (way 100635), 5-ht1d (brl 15572), 5-ht2b (sb 204741) or 5-ht7 (pimozide) receptors. |
2010-08-17 |
2023-08-12 |
Not clear |
| V Granados-Soto, C F Argüelles, H I Rocha-González, B Godínez-Chaparro, F J Flores-Murrieta, C M Villaló. The role of peripheral 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F serotonergic receptors in the reduction of nociception in rats. Neuroscience. vol 165. issue 2. 2010-02-24. PMID:19837141. |
the role of peripheral 5-ht1a, 5-ht1b, 5-ht1d, 5-ht1e and 5-ht1f serotonergic receptors in the reduction of nociception in rats. |
2010-02-24 |
2023-08-12 |
rat |
| Enriqueta Muñoz-Islas, Jair Lozano-Cuenca, Abimael González-Hernández, Martha B Ramírez-Rosas, Araceli Sánchez-López, David Centurión, Antoinette Maassenvandenbrink, Carlos M Villaló. Spinal sumatriptan inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors. European journal of pharmacology. vol 615. issue 1-3. 2009-11-10. PMID:19460365. |
spinal sumatriptan inhibits capsaicin-induced canine external carotid vasodilatation via 5-ht1b rather than 5-ht1d receptors. |
2009-11-10 |
2023-08-12 |
Not clear |
| E Muñoz-Islas, S Gupta, L R Jiménez-Mena, J Lozano-Cuenca, A Sánchez-López, D Centurión, S Mehrotra, A MaassenVanDenBrink, C M Villaló. Donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors. British journal of pharmacology. vol 149. issue 1. 2006-10-24. PMID:16880765. |
donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-ht1b rather than 5-ht1d receptors. |
2006-10-24 |
2023-08-12 |
dog |
| 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 |
| E Calama, A V Ortíz de Urbina, A Morán, M L Martín, L San Romá. Effect of 5-hydroxytryptamine on neurogenic vasoconstriction in the isolated, autoperfused hindquarters of the rat. Clinical and experimental pharmacology & physiology. vol 32. issue 10. 2006-01-05. PMID:16173953. |
the effects of 5-ht were mimicked by 5-carboxamidotryptamine (a 5-ht1 receptor agonist) and l-694 247 (a selective 5-ht1d receptor agonist), but not by 8-hydroxy-2-dipropylaminotetralin (a 5-ht1a receptor agonist), cgs-12066b (a 5-ht1b receptor agonist), alpha-methyl-5-ht (a 5-ht2 receptor agonist), 1-(3-chlorophenyl) piperazine (a 5-ht2c receptor agonist) or 1-phenylbiguanide (a 5-ht3 receptor agonist). |
2006-01-05 |
2023-08-12 |
rat |
| Tom D Heightman, Laramie M Gaster, Sarah L Pardoe, Jean-Pierre Pilleux, Michael S Hadley, Derek N Middlemiss, Gary W Price, Claire Roberts, Claire M Scott, Jeannette M Watson, Laurie J Gordon, Vicky A Holland, Jenifer Powles, Graham J Riley, Tania O Stean, Brenda K Trail, Neil Upton, Nigel E Austin, Andrew D Ayrton, Tanya Coleman, Leanne Cutle. 8-Piperazinyl-2,3-dihydropyrrolo[3,2-g]isoquinolines: potent, selective, orally bioavailable 5-HT1 receptor ligands. Bioorganic & medicinal chemistry letters. vol 15. issue 19. 2005-12-20. PMID:16039851. |
the template was n-substituted to give a series of compounds showing binding to human cloned 5-ht1a, 5-ht1b and 5-ht1d receptors with pki's greater than 9 and selectivities up to 1000-fold against other serotonin, dopamine and adrenergic receptors. |
2005-12-20 |
2023-08-12 |
human |