| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| K Andersen, T Liljefors, J Hyttel, J Perregaar. Serotonin 5-HT2 receptor, dopamine D2 receptor, and alpha 1 adrenoceptor antagonists. Conformationally flexible analogues of the atypical antipsychotic sertindole. Journal of medicinal chemistry. vol 39. issue 19. 1996-11-04. PMID:8809161. |
replacement of the basic amino group by nitrogen-containing six-membered rings has led to 5-chloro-1-(4-fluorophenyl)-3-[(4-methylpiperazinyl)-ethoxy]-1h-in dole, which has high affinity for dopamine d2, versus low affinity for serotonin 5-ht2a receptors and alpha 1 adrenoceptors. |
1996-11-04 |
2023-08-12 |
Not clear |
| N A Darman. Differential potentiation of L-tryptophan-induced head-twitch response in mice by cocaine and sertraline. Life sciences. vol 59. issue 14. 1996-10-31. PMID:8831798. |
using selective monoamine uptake blockers and appropriate selective monoamine receptor antagonists, we have previously shown that cocaine enhances the frequency of 5-ht2a receptor-mediated 5-hydroxytryptophan (5-htp)-induced head-twitch response (htr) in mice via inhibition of serotonin uptake. |
1996-10-31 |
2023-08-12 |
mouse |
| J P Huidobro-Toro, R A Harri. Brain lipids that induce sleep are novel modulators of 5-hydroxytrypamine receptors. Proceedings of the National Academy of Sciences of the United States of America. vol 93. issue 15. 1996-10-29. PMID:8755606. |
cis-9,10-octadecenamide (oda) markedly potentiated the action of 5-hydroxytryptamine (5-ht) on 5-ht2a and 5-ht2c receptors, but this action was not shared by related compounds such as oleic acid and trans-9,10-octacenamide. |
1996-10-29 |
2023-08-12 |
rat |
| M J Piera, M Beaughard, M T Michelin, E Winslow, R Massingha. Lack of efficacy of 5-HT2A receptor antagonists to reduce brain damage after 3 minutes of transient global cerebral ischaemia in gerbils. Fundamental & clinical pharmacology. vol 9. issue 6. 1996-10-29. PMID:8808177. |
stimulation of the 5-ht2a receptors by serotonin has been reported to exert an excitatory effect on neocortical neurons in rats and mice, to facilitate ischaemia-induced release of excitatory amino acids and to mediate the vasomotor constrictor component of the response of blood vessels to 5-ht. |
1996-10-29 |
2023-08-12 |
mouse |
| F G Graeff, F S Guimarães, T G De Andrade, J F Deaki. Role of 5-HT in stress, anxiety, and depression. Pharmacology, biochemistry, and behavior. vol 54. issue 1. 1996-10-23. PMID:8728550. |
in healthy volunteers, d-fenfluramine and the 5-ht agonist mcpp (mainly 5-ht2c) increased, while the antagonists ritanserin (5-ht2a/2c) and sr 46349b (5-ht2a) decreased skin conductance responses to an aversively conditioned stimulus (tone). |
1996-10-23 |
2023-08-12 |
human |
| C Reist, D Helmeste, L Albers, H Chhay, S W Tan. Serotonin indices and impulsivity in normal volunteers. Psychiatry research. vol 60. issue 2-3. 1996-10-17. PMID:8723308. |
the calcium response to serotonin (5-hydroxytryptamine, 5ht), mediated by platelet 5ht2a, was also measured. |
1996-10-17 |
2023-08-12 |
human |
| S A Doggrel. Increase in affinity and loss of 5-hydroxytryptamine2A-receptor reserve for 5-hydroxytryptamine on the aorta of spontaneously hypertensive rats. Journal of autonomic pharmacology. vol 15. issue 5. 1996-10-16. PMID:8744977. |
on the wky and wa rat aortae, 5-ht caused 50 and 95% maximal responses by occupying 10-20 and 45-60%, whereas on the shr aorta 5-ht produced 50 and 95% maximal responses by occupying 20-30 and 75-85% of the available 5-ht2a receptors, respectively. |
1996-10-16 |
2023-08-12 |
rat |
| D D Mousseau, V L Rao, R F Butterwort. Alterations in serotonin parameters in brain of thiamine-deficient rats are evident prior to the appearance of neurological symptoms. Journal of neurochemistry. vol 67. issue 3. 1996-10-02. PMID:8752118. |
these binding changes, which appear to represent changes in the density of the postsynaptic 5-ht2a receptor population rather than the "tetrabenazine-sensitive" vesicular monoamine transporter, are evident before the appearance of histopathologic lesions and coincide with altered tissue concentrations of 5-ht. |
1996-10-02 |
2023-08-12 |
rat |
| S Graf, S K Sarn. 5-HT-induced jejunal motor activity: enteric locus of action and receptor subtypes. The American journal of physiology. vol 270. issue 6 Pt 1. 1996-09-26. PMID:8764207. |
we conclude that in the conscious state, 5-ht acts on 5-ht2a and 5-ht2c receptors located on postsynaptic cholinergic neurons in the canine jejunum to stimulate phasic contractions and phase iii activity. |
1996-09-26 |
2023-08-12 |
Not clear |
| J E Audia, D A Evrard, G R Murdoch, J J Droste, J S Nissen, K W Schenck, P Fludzinski, V L Lucaites, D L Nelson, M L Cohe. Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus. Journal of medicinal chemistry. vol 39. issue 14. 1996-09-10. PMID:8709108. |
these high-affinity tetrahydro-beta-carboline antagonists are able to discriminate among the 5ht2 family of serotonin receptors, with members of the series showing selectivities of more than 100-fold versus both the 5ht2a and 5ht2c receptors based upon radioligand binding and functional assays. |
1996-09-10 |
2023-08-12 |
rat |
| N Almaula, B J Ebersole, J A Ballesteros, H Weinstein, S C Sealfo. Contribution of a helix 5 locus to selectivity of hallucinogenic and nonhallucinogenic ligands for the human 5-hydroxytryptamine2A and 5-hydroxytryptamine2C receptors: direct and indirect effects on ligand affinity mediated by the same locus. Molecular pharmacology. vol 50. issue 1. 1996-09-03. PMID:8700116. |
furthermore, this analysis shows that the higher affinity of 5-ht and tryptamine for the 5-ht2c receptor than for the 5-ht2a receptors is not due to the difference at this locus. |
1996-09-03 |
2023-08-12 |
human |
| F V Abbott, Y Hong, P Blie. Activation of 5-HT2A receptors potentiates pain produced by inflammatory mediators. Neuropharmacology. vol 35. issue 1. 1996-08-19. PMID:8684602. |
these data imply that 5-ht2a antagonists may be effective peripherally acting analgesics or analgesic adjuncts in pain associated with 5-ht release from platelets, such acute injury and, perhaps, some chronic pain states. |
1996-08-19 |
2023-08-12 |
rat |
| N Almaula, B J Ebersole, D Zhang, H Weinstein, S C Sealfo. Mapping the binding site pocket of the serotonin 5-Hydroxytryptamine2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin. The Journal of biological chemistry. vol 271. issue 25. 1996-08-13. PMID:8663249. |
like other amine neurotransmitters that activate g-protein-coupled receptors, 5-hydroxytryptamine (5-ht) binds to the 5-ht2a receptor through the interaction of its cationic primary amino group with the conserved asp3.32(155) in transmembrane helix 3. |
1996-08-13 |
2023-08-12 |
Not clear |
| N Almaula, B J Ebersole, D Zhang, H Weinstein, S C Sealfo. Mapping the binding site pocket of the serotonin 5-Hydroxytryptamine2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin. The Journal of biological chemistry. vol 271. issue 25. 1996-08-13. PMID:8663249. |
computational experiments with a 5-ht2a receptor model suggest that the same functional group of 5-hydroxytryptamine also forms a hydrogen bond with the side chain of ser3.36(159), which is adjacent in space to asp3.32(155). |
1996-08-13 |
2023-08-12 |
Not clear |
| N Almaula, B J Ebersole, D Zhang, H Weinstein, S C Sealfo. Mapping the binding site pocket of the serotonin 5-Hydroxytryptamine2A receptor. Ser3.36(159) provides a second interaction site for the protonated amine of serotonin but not of lysergic acid diethylamide or bufotenin. The Journal of biological chemistry. vol 271. issue 25. 1996-08-13. PMID:8663249. |
however, other 5-ht2a receptor ligands like lysergic acid diethylamide (lsd), in which the amine nitrogen is embedded in a heterocycle, or n,n-dimethyl 5-ht, in which the side chain is a tertiary amine, are found in the computational simulations to interact with the aspartate but not with the serine, due mainly to steric hindrance. |
1996-08-13 |
2023-08-12 |
Not clear |
| N Laprade, F Radja, T A Reader, J J Soghomonia. Dopamine receptor agonists regulate levels of the serotonin 5-HT2A receptor and its mRNA in a subpopulation of rat striatal neurons. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 16. issue 11. 1996-07-12. PMID:8642415. |
dopamine receptor agonists regulate levels of the serotonin 5-ht2a receptor and its mrna in a subpopulation of rat striatal neurons. |
1996-07-12 |
2023-08-12 |
rat |
| N Laprade, F Radja, T A Reader, J J Soghomonia. Dopamine receptor agonists regulate levels of the serotonin 5-HT2A receptor and its mRNA in a subpopulation of rat striatal neurons. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 16. issue 11. 1996-07-12. PMID:8642415. |
the effects of dopamine receptor agonists on the levels of the striatal serotonin 5-ht2a receptor and its mrna were investigated in rats lesioned with 6-ohda as neonates. |
1996-07-12 |
2023-08-12 |
rat |
| S W Watts, M Baez, R C Web. The 5-hydroxytryptamine2B receptor and 5-HT receptor signal transduction in mesenteric arteries from deoxycorticosterone acetate-salt hypertensive rats. The Journal of pharmacology and experimental therapeutics. vol 277. issue 2. 1996-06-27. PMID:8627522. |
in arteries from sham rats, ketanserin (5-ht2a/5-ht2c selective), ly53857 (5-ht2 selective) and spiperone (5-ht2a/5-ht2c selective) shifted contraction to 5-ht (pkb = 8.58, 8.35 and 9.52, respectively) indicating that a 5-ht2a receptor mediates contraction in arteries from normotensive rats. |
1996-06-27 |
2023-08-12 |
rat |
| D A Cox, S W Watts, M L Cohe. Neomycin selectively inhibits 5-hydroxytryptamine-induced contraction in the guinea pig trachea. The Journal of pharmacology and experimental therapeutics. vol 277. issue 2. 1996-06-27. PMID:8627578. |
neomycin (3 mm) inhibited maximal 5-ht-induced contraction by approximately 50% without inhibiting [3h]5-ht binding to 5-ht2a receptors. |
1996-06-27 |
2023-08-12 |
Not clear |
| D A Cox, S W Watts, M L Cohe. Neomycin selectively inhibits 5-hydroxytryptamine-induced contraction in the guinea pig trachea. The Journal of pharmacology and experimental therapeutics. vol 277. issue 2. 1996-06-27. PMID:8627578. |
although bradykinin stimulated phospholipase d (pld) activity, 5-ht did not activate pld, suggesting that the 5-ht2a receptor is not coupled to this enzyme in the guinea pig trachea. |
1996-06-27 |
2023-08-12 |
Not clear |