| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| R E Solomon, G F Gebhar. Mechanisms of effects of intrathecal serotonin on nociception and blood pressure in rats. The Journal of pharmacology and experimental therapeutics. vol 245. issue 3. 1988-07-29. PMID:2455040. |
the 5-ht1a agonist 8-hydroxy-n,n-dipropyl-2-aminotetralin and the 5ht1b agonist 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indole (ru-24969) also produced depressor effects but, in contrast to 5-ht, facilitated the tail-flick reflex, whereas the 5-ht2 agonists 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane, 6-chloro-2-(1-piperazinyl)-pyrazine (mk-212) and quipazine produced dose-dependent antinociception and had little or no effect on blood pressure. |
1988-07-29 |
2023-08-11 |
rat |
| H Shimizu, N Karai, A Hirose, T Tatsuno, H Tanaka, Y Kumasaka, M Nakamur. Interaction of SM-3997 with serotonin receptors in rat brain. Japanese journal of pharmacology. vol 46. issue 3. 1988-07-25. PMID:2898033. |
sm-3997 possessed a high affinity towards 5-ht1a receptors, low affinity towards dopamine (d2) and 5-ht2 receptors, and no affinity towards benzodiazepine (bz), gaba, 5-ht1b and adrenergic receptors. |
1988-07-25 |
2023-08-11 |
rat |
| D Hoyer, C Waeber, A Pazos, A Probst, J M Palacio. Identification of a 5-HT1 recognition site in human brain membranes different from 5-HT1A, 5-HT1B and 5-HT1C sites. Neuroscience letters. vol 85. issue 3. 1988-06-02. PMID:2966310. |
in contrast, these sites showed low affinity for drugs with high affinity and/or selectivity for 5-ht1a (8-oh-dpat, buspirone), 5-ht1b (21-009, ru 24969), 5-ht1c (mesulergine, mianserin) and 5-ht2 sites (ketanserin, cinanserin). |
1988-06-02 |
2023-08-11 |
human |
| M R Pranzatell. The comparative pharmacology of the behavioral syndromes induced by TRH and by 5-HT in the rat. General pharmacology. vol 19. issue 2. 1988-05-12. PMID:2895033. |
a 5-ht1a agonist (8-oh-dpat) blocked wds, but like putative 5-ht1b (ru 24969) and 5-ht2 (doi) agonists and the 5-ht antagonists methysergide (non-selective), ritanserin (5-ht2 selective), and l-propranolol (5-ht1 selective), it did not block other antagonists behavioural effects of mk-771. |
1988-05-12 |
2023-08-11 |
rat |
| G Gross, G Hanft, N Kolass. Urapidil and some analogues with hypotensive properties show high affinities for 5-hydroxytryptamine (5-HT) binding sites of the 5-HT1A subtype and for alpha 1-adrenoceptor binding sites. Naunyn-Schmiedeberg's archives of pharmacology. vol 336. issue 6. 1988-05-03. PMID:2832770. |
in the present study, the affinities of these urapidil derivatives (5-acetyl, 5-formyl- and 5-methyl-urapidil) for 5-ht receptors were investigated using 3h-8-hydroxy-2-(di-n-propyl-amino)tetralin (3h-8-oh-dpat), 125i-iodocyanopindolol (125i-icyp) and 3h-ketanserin for labelling 5-ht1a, 5-ht1b and 5-ht2 binding sites, respectively. |
1988-05-03 |
2023-08-11 |
Not clear |
| M Titeler, R A Lyon, R A Glenno. Radioligand binding evidence implicates the brain 5-HT2 receptor as a site of action for LSD and phenylisopropylamine hallucinogens. Psychopharmacology. vol 94. issue 2. 1988-05-03. PMID:3127847. |
in order to test the hypothesis that the mechanism of action of lsd and phenylisopropylamine hallucinogens is through stimulation of a specific brain serotonin receptor sub-type, the affinities of these compounds for radiolabelled 5-ht2, 5-ht1a, 5-ht1b, and 5-ht1c receptors have been determined using recently developed in vitro radioligand binding methodologies. |
1988-05-03 |
2023-08-11 |
Not clear |
| J R Ieni, L R Meyerso. The 5-HT1A receptor probe [3H]8-OH-DPAT labels the 5-HT transporter in human platelets. Life sciences. vol 42. issue 3. 1988-02-23. PMID:2961966. |
for example, 8-oh-dpat 5ht1a had an ic50 of 117 nm; tfmpp 5ht1b (2.3 microm0 and papp 1a + 5ht2 (9 microm); ipsapirone 5ht1a (21.1 microm) and buspirone 5ht1a (greater than 100 microm); ketanserin 5ht2 (greater than 100 microm); 5-ht uptake inhibitors: paroxetine (13 nm); chlorimipramine (73 nm) and fluoxetine (653 nm). |
1988-02-23 |
2023-08-11 |
human |
| G J Molderings, K Fink, E Schlicker, M Göther. Inhibition of noradrenaline release via presynaptic 5-HT1B receptors of the rat vena cava. Naunyn-Schmiedeberg's archives of pharmacology. vol 336. issue 3. 1988-01-11. PMID:3683595. |
ketanserin, a 5-ht2 receptor antagonist, and spiperone, which blocks 5-ht2 and 5-ht1a but not 5-ht1b or 5-ht1c receptors, failed to antagonize the effect of 5-ht. |
1988-01-11 |
2023-08-11 |
rat |
| M R Pranzatelli, E Jappay, S R Snodgras. Effects of 5-HT receptor subtype-selective drugs on locomotor activity and motor habituation in the DHT adult rat model. Pharmacology, biochemistry, and behavior. vol 27. issue 3. 1987-10-27. PMID:3116560. |
the non-neuroleptic ritanserin, however, did not reduce lma stimulated by the 5-ht1b agonist ru24969 but did reverse transient suppression of lma induced by high dose 5-htp and by the putative 5-ht2 agonist doi. |
1987-10-27 |
2023-08-11 |
rat |
| B S Alexander, M D Woo. Stereoselective blockade of central [3H]5-hydroxytryptamine binding to multiple sites (5-HT1A, 5-HT1B and 5-HT1C) by mianserin and propranolol. The Journal of pharmacy and pharmacology. vol 39. issue 8. 1987-10-26. PMID:2888864. |
the interaction of the enantiomers of mianserin and propranolol with the binding of [3h]5-hydroxytryptamine ([3h]5-ht) to the 5-ht1a, 5-ht1b and 5-ht1c sites, and with the binding of [3h]ketanserin to the 5-ht2 site, has been evaluated in rat brain membranes. |
1987-10-26 |
2023-08-11 |
rat |
| B L Roth, D M Chuan. Multiple mechanisms of serotonergic signal transduction. Life sciences. vol 41. issue 9. 1987-09-23. PMID:2441225. |
recent findings suggest that the distinct types of pharmacologically defined serotonergic receptors (5ht1a, 5ht1b, 5ht1c, 5ht2) may be coupled to one or more signal transduction systems. |
1987-09-23 |
2023-08-11 |
Not clear |
| G A Kennett, C T Dourish, G Curzo. Antidepressant-like action of 5-HT1A agonists and conventional antidepressants in an animal model of depression. European journal of pharmacology. vol 134. issue 3. 1987-05-28. PMID:2883013. |
evidence suggests that the above action of 8-oh-dpat is mediated by 5-ht1a receptors since it was antagonised by the 5-ht1a antagonist spiperone but not by the 5-ht2 antagonist ketanserin and was not mimicked by the 5-ht1b agonist ru 24969. |
1987-05-28 |
2023-08-11 |
rat |
| R E Heuring, S J Peroutk. Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 7. issue 3. 1987-04-29. PMID:2951504. |
these data therefore demonstrate the presence of a homogeneous class of 5-ht1 binding sites in bovine caudate that is pharmacologically distinct from previously defined 5-ht1a, 5-ht1b, 5-ht1c, 5-ht2, and 5-ht3 receptor subtypes. |
1987-04-29 |
2023-08-11 |
rat |
| G M Goodwin, R J DeSouza, A J Wood, A R Gree. Lithium decreases 5-HT1A and 5-HT2 receptor and alpha 2-adrenoceptor mediated function in mice. Psychopharmacology. vol 90. issue 4. 1987-03-20. PMID:3027734. |
by contrast with this reduction of 5-hydroxytryptamine (5-ht) function mediated by the 5-ht1a and 5-ht2 receptor sub-types, repeated lithium administration had no effect on the motor response to a putative 5-ht1b receptor agonist 5-methoxy-3(1,2,3,6-tetrahydropyridin-4-yl)1h indole (ru 24969, 3 mg/kg ip). |
1987-03-20 |
2023-08-11 |
mouse |
| H O Kalkman, G Engel, D Hoye. Inhibition of 5-carboxamidotryptamine-induced relaxation of guinea-pig ileum correlates with [125I]LSD binding. European journal of pharmacology. vol 129. issue 1-2. 1986-12-11. PMID:3770071. |
the results suggest that the 5-ht receptor-mediating relaxation in the guinea-pig ileum can be labelled with [125i]lsd and that this receptor does not belong to the 5-ht2, 5-ht1a, 5-ht1b or 5-ht1c receptor subtypes. |
1986-12-11 |
2023-08-11 |
Not clear |
| M L Cohen, W E Colber. Relationship between receptors mediating serotonin (5-HT) contractions in the canine basilar artery to 5-HT1, 5-HT2 and rat stomach fundus 5-HT receptors. The Journal of pharmacology and experimental therapeutics. vol 237. issue 3. 1986-07-16. PMID:3712277. |
similarity of the contractile effects of 5-ht in the rat stomach fundus and in the basilar artery coupled to the previous observations that receptors mediating 5-ht-induced contractions in the fundus were not 5-ht1, 5-ht1a, 5-ht1b or 5-ht2 led us to consider the possibility that 5-ht receptors in the canine basilar artery may resemble those in the rat stomach fundus. |
1986-07-16 |
2023-08-11 |
rat |
| G Engel, M Göthert, D Hoyer, E Schlicker, K Hillenbran. Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites. Naunyn-Schmiedeberg's archives of pharmacology. vol 332. issue 1. 1986-04-22. PMID:2936965. |
the affinities of the compounds for 5-ht1b and 5-ht2 binding sites in rat brain cortex membranes (labelled by [125i]cyanopindolol = [125i]-cyp in the presence of 30 mumol/l isoprenaline and [3h]ketanserin, respectively), for 5-ht1a binding sites in pig and rat brain cortex membranes (labelled by [3h]8-hydroxy-2-(di-n-propylamino)tetralin = [3h]8-oh-dpat) and for 5-ht1c binding sites in pig choroid plexus membranes (labelled by [3h]mesulergine) were also determined. |
1986-04-22 |
2023-08-11 |
rat |
| E W Taylor, S P Duckles, D L Nelso. Dissociation constants of serotonin agonists in the canine basilar artery correlate to Ki values at the 5-HT1A binding site. The Journal of pharmacology and experimental therapeutics. vol 236. issue 1. 1986-02-20. PMID:2934545. |
logs of these ka values did not correlate with log ki values for the inhibition of binding of the 5-ht2 ligand [3h] ketanserin (r = 0.2253, p greater than .05) or log ic50 values for inhibition of [3h]5-ht binding (r = 0.5732, p greater than 0.05), which labels both 5-ht1a and 5-ht1b sites. |
1986-02-20 |
2023-08-11 |
Not clear |
| K A Yagaloff, P R Harti. 125I-lysergic acid diethylamide binds to a novel serotonergic site on rat choroid plexus epithelial cells. The Journal of neuroscience : the official journal of the Society for Neuroscience. vol 5. issue 12. 1986-02-07. PMID:4078623. |
the choroid plexus site exhibits a novel pharmacology that does not match the properties of 5-hydroxytryptamine-1a (5-ht1a), 5-ht1b, or 5-ht2 serotonergic sites. |
1986-02-07 |
2023-08-11 |
rat |
| D N Middlemis. The putative 5-HT1 receptor agonist, RU 24969, inhibits the efflux of 5-hydroxytryptamine from rat frontal cortex slices by stimulation of the 5-HT autoreceptor. The Journal of pharmacy and pharmacology. vol 37. issue 6. 1985-09-16. PMID:2862270. |
moreover, since ru 24969 potently displaced ligand binding to the 5-ht1 and 5-ht1b recognition sites but was only weakly active at the 5-ht2 receptor, the results lend support to the claim for a pharmacological resemblance between the 5-ht autoreceptor and the 5-ht1 recognition site and in particular the low affinity 5-ht1b subtype. |
1985-09-16 |
2023-08-11 |
rat |