| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| R M Eglen, K Bley, D W Bonhaus, R D Clark, S S Hegde, L G Johnson, E Leung, E H Won. RS 23597-190: a potent and selective 5-HT4 receptor antagonist. British journal of pharmacology. vol 110. issue 1. 1993-12-14. PMID:8220871. |
at 5-ht1a, 5-ht2,muscarinic m1, m2, m3, m4 and dopamine d1 and d2 receptors, rs 23597-190 exhibited low apparent affinities, with all - log ki values less than 5.5.6. |
1993-12-14 |
2023-08-12 |
rat |
| C E Johanson, J E Barret. The discriminative stimulus effects of cocaine in pigeons. The Journal of pharmacology and experimental therapeutics. vol 267. issue 1. 1993-11-29. PMID:8229735. |
the drugs included other psychomotor stimulants, antidepressants, clonidine, yohimbine, other dopamine (1-(2-[bis(4-fluoro-phenyl)-methoxy]ethyl)4-3-phenylpropyl piperazine, gbr 12909) and serotonin (5-ht, sertraline) reuptake blockers, a d1 (skf 75670), d2 (quinpirole), and 5-ht1a (8-hydroxy-2-(di-n-propylamino)tetralin, 8-oh-dpat) agonist as well as the 5-ht3 antagonists, mdl 72222, ly 278584 and ondansetron. |
1993-11-29 |
2023-08-12 |
Not clear |
| D Curtis, R Sherrington, P Brett, D S Holmes, G Kalsi, J Brynjolfsson, H Petursson, L Rifkin, P Murphy, E Molone. Genetic linkage analysis of manic depression in Iceland. Journal of the Royal Society of Medicine. vol 86. issue 9. 1993-11-02. PMID:8105081. |
candidate genes excluded include those for tyrosine hydroxylase, the dopamine type 2 receptor, proenkephalin, the 5ht1a receptor and dopamine beta hydroxylase. |
1993-11-02 |
2023-08-12 |
Not clear |
| M B Assié, A J Sleight, W Koe. Biphasic displacement of [3H]YM-09151-2 binding in the rat brain by thioridazine, risperidone and clozapine, but not by other antipsychotics. European journal of pharmacology. vol 237. issue 2-3. 1993-10-04. PMID:7689973. |
biphasic displacement did not appear to result from interactions with either the dopamine d3, dopamine d4, 5-ht2, 5-ht1c or the 5-ht1a receptor binding sites. |
1993-10-04 |
2023-08-12 |
rat |
| S Bourgoin, M Pohl, A Mauborgne, J J Benoliel, E Collin, M Hamon, F Cesseli. Monoaminergic control of the release of calcitonin gene-related peptide- and substance P-like materials from rat spinal cord slices. Neuropharmacology. vol 32. issue 7. 1993-09-24. PMID:7689707. |
further studies with selective ligands of other monoamine receptors indicated that neither alpha 1- and beta-adrenergic receptors, dopamine d-2, nor serotonin 5-ht1a and 5-ht3 receptors are apparently involved in some control of the spinal release of cgrplm and splm. |
1993-09-24 |
2023-08-12 |
rat |
| A M Ismaiel, J De Los Angeles, M Teitler, S Ingher, R A Glenno. Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist. Journal of medicinal chemistry. vol 36. issue 17. 1993-09-23. PMID:8355253. |
although the neuroleptic agent spiperone binds at d2 dopamine receptors and 5-ht1a serotonin receptors, (a) it displays about a 1000-fold selectivity for 5-ht2 versus 5-ht1c sites and (b) it has been used as a "5-ht2-selective" antagonist. |
1993-09-23 |
2023-08-12 |
rat |
| R Corbett, H Hartman, L L Kerman, A T Woods, J T Strupczewski, G C Helsley, P C Conway, R W Dun. Effects of atypical antipsychotic agents on social behavior in rodents. Pharmacology, biochemistry, and behavior. vol 45. issue 1. 1993-07-19. PMID:7685916. |
further, our data suggests that a compound's effectiveness for the treatment of social withdrawal is at least in part due to its relative affinity for binding to dopamine d1 and serotonin 5-ht1a receptors. |
1993-07-19 |
2023-08-12 |
rat |
| L Arborelius, K Chergui, S Murase, G G Nomikos, B B Höök, G Chouvet, U Hacksell, T H Svensso. The 5-HT1A receptor selective ligands, (R)-8-OH-DPAT and (S)-UH-301, differentially affect the activity of midbrain dopamine neurons. Naunyn-Schmiedeberg's archives of pharmacology. vol 347. issue 4. 1993-07-15. PMID:8510763. |
the 5-ht1a receptor selective ligands, (r)-8-oh-dpat and (s)-uh-301, differentially affect the activity of midbrain dopamine neurons. |
1993-07-15 |
2023-08-12 |
rat |
| L Arborelius, K Chergui, S Murase, G G Nomikos, B B Höök, G Chouvet, U Hacksell, T H Svensso. The 5-HT1A receptor selective ligands, (R)-8-OH-DPAT and (S)-UH-301, differentially affect the activity of midbrain dopamine neurons. Naunyn-Schmiedeberg's archives of pharmacology. vol 347. issue 4. 1993-07-15. PMID:8510763. |
the effects of the selective 5-ht1a receptor agonist (r)-8-hydroxy-2(di-n-propylamino)tetralin [(r)-8-oh-dpat] and the novel 5-ht1a antagonist (s)-5-fluoro-8-hydroxy-2-(dipropylamino)-tetralin [(s)-uh-301] were studied with regard to the firing pattern of single mesencephalic dopamine (da) neurons with extracellular recording techniques in chloral hydrate anesthetized male rats. |
1993-07-15 |
2023-08-12 |
rat |
| C G Chidester, C H Lin, R A Lahti, S R Haadsma-Svensson, M W Smit. Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands. Journal of medicinal chemistry. vol 36. issue 10. 1993-06-22. PMID:8496900. |
comparison of 5-ht1a and dopamine d2 pharmacophores. |
1993-06-22 |
2023-08-12 |
Not clear |
| C G Chidester, C H Lin, R A Lahti, S R Haadsma-Svensson, M W Smit. Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands. Journal of medicinal chemistry. vol 36. issue 10. 1993-06-22. PMID:8496900. |
conformational and molecular mechanics studies of a new series of tricyclic ligands with affinity for either the dopamine d2 receptor or the 5-ht1a receptor, or both, has enabled us to elaborate considerably on previous pharmacophore models for these receptors. |
1993-06-22 |
2023-08-12 |
Not clear |
| C G Chidester, C H Lin, R A Lahti, S R Haadsma-Svensson, M W Smit. Comparison of 5-HT1A and dopamine D2 pharmacophores. X-ray structures and affinities of conformationally constrained ligands. Journal of medicinal chemistry. vol 36. issue 10. 1993-06-22. PMID:8496900. |
suggestions are made for enhancing selectivity at the 5-ht1a receptor or at the dopamine d2 receptor. |
1993-06-22 |
2023-08-12 |
Not clear |
| C H Lin, S R Haadsma-Svensson, R A Lahti, R B McCall, M F Piercey, P J Schreur, P F Von Voigtlander, M W Smith, C G Chideste. Centrally acting serotonergic and dopaminergic agents. 1. Synthesis and structure-activity relationships of 2,3,3a,4,5,9b-hexahydro-1H-benz[e]indole derivatives. Journal of medicinal chemistry. vol 36. issue 8. 1993-05-24. PMID:8097537. |
analogs with 9-methoxy substitution (r1 in 3) showed mixed 5-ht1a agonist and dopamine antagonist activities whereas the corresponding 9-hydroxy analogs displayed selective 5-ht1a agonist activity. |
1993-05-24 |
2023-08-12 |
Not clear |
| C H Lin, S R Haadsma-Svensson, R A Lahti, R B McCall, M F Piercey, P J Schreur, P F VonVoigtlander, C G Chideste. Centrally acting serotonergic agents. Synthesis and structure-activity relationships of C-1- or C-3-substituted derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin. Journal of medicinal chemistry. vol 36. issue 6. 1993-04-28. PMID:8459396. |
interestingly, the 5-ome analogs were found to be inactive in both the 5-ht1a and dopamine d2 binding assays. |
1993-04-28 |
2023-08-12 |
Not clear |
| P Schoeffter, J R Fozard, A Stoll, H Siegl, M P Seiler, D Hoye. SDZ 216-525, a selective and potent 5-HT1A receptor antagonist. European journal of pharmacology. vol 244. issue 3. 1993-04-23. PMID:8384569. |
the affinity of the compound for alpha 1, alpha 2, beta 1 and beta 2 adrenoceptors, and dopamine d2 receptors was at least 50-100 times lower than for 5-ht1a sites. |
1993-04-23 |
2023-08-12 |
rat |
| B Cusack, E Richelso. A method for radioligand binding assays using a robotic workstation. Journal of receptor research. vol 13. issue 1-4. 1993-04-15. PMID:8450491. |
we have employed this method for the determination of equilibrium dissociation constants (kds) for drugs at the 5 human muscarinic acetylcholine receptor subtypes expressed in cultured cells, as well as histamine h1, dopamine d2, serotonin 5ht1a, alpha 1- and alpha 2-adrenergic receptors in human brain tissue homogenates. |
1993-04-15 |
2023-08-12 |
human |
| C M Brown, A C MacKinnon, W S Redfern, P E Hicks, A T Kilpatrick, C Small, M Ramcharan, R U Clague, R D Clark, C B MacFarlan. The pharmacology of RS-15385-197, a potent and selective alpha 2-adrenoceptor antagonist. British journal of pharmacology. vol 108. issue 2. 1993-04-09. PMID:8095420. |
rs-15385-197 was highly selective for alpha 2-adrenoceptors over other receptors: the compound showed low affinity for 5-ht1a (pki 6.50) and 5-ht1d (pki 7.00) receptor subtypes, and even lower affinity (pki < or = 5) for other 5-ht receptor subtypes, dopamine receptors, muscarinic cholinoceptors, beta-adrenoceptors and dihydropyridine binding sites. |
1993-04-09 |
2023-08-12 |
human |
| M J Millan, J M Rivet, H Canton, F Lejeune, A Gobert, P Widdowson, K Bervoets, M Brocco, J L Peglio. S 15535: a highly selective benzodioxopiperazine 5-HT1A receptor ligand which acts as an agonist and an antagonist at presynaptic and postsynaptic sites respectively. European journal of pharmacology. vol 230. issue 1. 1993-03-09. PMID:8381359. |
the novel benzodioxopiperazine, s 15535 (4-(benzodioxan-5-yl)1-(indan-2- yl)piperazine), displayed high affinity for 5-ht1a binding sites (1.8 nm) whereas its affinity was 100-fold lower at other 5-ht receptor types, at alpha 1, alpha 2- and beta-adrenoceptors and at dopamine d1 and d2 receptors. |
1993-03-09 |
2023-08-12 |
Not clear |
| R A Glennon, R Higgs, R Young, H Iss. Further studies on N-methyl-1(3,4-methylenedioxyphenyl)-2-aminopropane as a discriminative stimulus: antagonism by 5-hydroxytryptamine3 antagonists. Pharmacology, biochemistry, and behavior. vol 43. issue 4. 1993-02-01. PMID:1361990. |
low doses of the 5-hydroxytryptamine1a (5-ht1a) antagonist nan-190, the 5-ht2 antagonist pirenperone, and the dopamine antagonist haloperidol were able to somewhat attenuate the mdma stimulus; however, none of these agents decreased mdma-appropriate responding to less than 46%. |
1993-02-01 |
2023-08-11 |
rat |
| J L Wiley, J H Porte. Serotonergic drugs do not substitute for clozapine in clozapine-trained rats in a two-lever drug discrimination procedure. Pharmacology, biochemistry, and behavior. vol 43. issue 3. 1992-12-30. PMID:1448493. |
the present study examined the effects of haloperidol (d2 dopamine antagonist), ritanserin (5-ht2 antagonist), 1-alpha h,3-alpha,5-alpha h-tropan-3yl-3,5-dichlorobenzoate (mdl 72222) (5-ht3 antagonist), and buspirone (5-ht1a agonist) in stimulus substitution tests with rats trained to discriminate clozapine (5.0 mg/kg, ip) from vehicle in a two-lever drug discrimination procedure under a fixed ratio 30 schedule of food reinforcement. |
1992-12-30 |
2023-08-11 |
rat |