8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 1220 |
| CHEMBL ID | 56 |
| CHEBI ID | 73364 |
| SCHEMBL ID | 496783 |
| MeSH ID | M0026382 |
| Synonym |
|---|
| BRD-A48015106-001-01-0 |
| [3h]8-oh-dpat |
| gtpl7 |
| gtpl31 |
| 1-naphthalenol, 7-(dipropylamino)-5,6,7,8-tetrahydro- |
| BIOMOL-NT_000095 |
| PDSP1_000777 |
| BPBIO1_001354 |
| 78950-78-4 |
| 8-hydroxy-n,n-dipropyl-2-aminotetralin |
| PDSP2_000765 |
| LOPAC0_000576 |
| chembl56 , |
| 8-oh-dpat,(+) |
| cid_1220 |
| [3h]-8-oh-dpat |
| bdbm21393 |
| 7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol |
| 8-oh-dpat,(-) |
| 8-hydroxy-n,n-dipropylaminotetralin |
| dpat |
| 8-hydroxy-2-(di-n-propylamino)tetralin |
| 8-oh-dpat |
| NCGC00024635-03 |
| c16h25no |
| NCGC00024986-02 |
| NCGC00024635-02 |
| NCGC00015493-06 |
| L000086 |
| (+/-)-8-hydroxy-2-dipropyl-aminotetralin |
| chebi:73364 , |
| iws1724px6 , |
| 8-hydroxy-dpat |
| dl-8-hydroxy-2-(dipropylamino)tetralin |
| (+-)-8-oh-dpat |
| unii-iws1724px6 |
| CCG-204665 |
| SR-01000075571-7 |
| NCGC00015493-05 |
| NCGC00015493-04 |
| FT-0641759 |
| 1-naphthalenol,7-(dipropylamino)-5,6,7,8-tetrahydro- |
| ASXGJMSKWNBENU-UHFFFAOYSA-N |
| 5,6,7,8-tetrahydro-7-(dipropylamino)-1-naphthalenol |
| SCHEMBL496783 |
| (+/-)-7-(dipropylamino)-5,6,7,8-tetrahydro-1-naphthalenol |
| (+/-)-8-hydroxy-2-(dipropylamino)tetralin |
| (+/-)-8-oh-dpat |
| 8-hydroxy-2-(di-n-propylamino)tetralin, (+/-)- |
| (+/-)-8-hydroxy-n,n-dipropyl-2-aminotetralin |
| s(-)-8-hydroxy-dpat hydrobromide partial 5-ht1a secrot |
| J-007140 |
| CS-0043224 |
| HY-112061 |
| 8-hydroxy-dpat; 8oh-dpat |
| AKOS030627213 |
| BCP25681 |
| DTXSID30897384 |
| Q4644282 |
| (+/-)-8-hydroxy-2-(di-n-propylamino)tetralin |
| S8447 |
| 8-oh-dpat (8-hydroxy-dpat) |
| 105558-30-3 |
| EX-A2914 |
| BRD-A48015106-004-03-0 |
| SDCCGSBI-0050558.P002 |
| NCGC00015493-10 |
| HMS3886N10 |
| MS-23507 |
| TQP0825 |
| 78950-78-4 (free base) |
| BO166474 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " While typical antipsychotics are often switched to atypical agents when adverse effects become limiting, there is little preclinical information to support this strategy, both in terms of efficacy and side effects." | ( Combined treatment of quetiapine with haloperidol in animal models of antipsychotic effect and extrapyramidal side effects: comparison with risperidone and chlorpromazine. Matsuoka, N; Mutoh, S; Shirakawa, K; Tada, M, 2004) | 0.32 |
| "The results suggest that compounds that indirectly facilitate 5-HT1 A receptor activation, such as citalopram, may be more effective therapeutics than direct 5-HT1 A receptor agonists because they exhibit similar anti-dyskinesia efficacy, while possessing a reduced side effect profile." | ( Side effect profile of 5-HT treatments for Parkinson's disease and L-DOPA-induced dyskinesia in rats. Bishop, C; Conti, MM; Lindenbach, D; Ostock, CY; Palumbo, N; Vilceus, N, 2015) | 0.42 |
| " It produces serious adverse effects, but its pharmacological profile is not well recognized." | ( Neurotoxic Effects of 5-MeO-DIPT: A Psychoactive Tryptamine Derivative in Rats. Gołembiowska, K; Kamińska, K; Kreiner, G; Noworyta-Sokołowska, K; Rogóż, Z, 2016) | 0.43 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The present study describes the pharmacokinetic properties of (S)-UH-301 after subcutaneous administration in rats, using a newly developed HPLC-UV bioanalytical method." | ( An integrative pharmacokinetic and pharmacodynamic study of the 5-HT1A receptor antagonist (S)-UH-301 in the rat. Lewander, T; Yan, H; Yu, H, 2002) | 0.31 |
| "The pharmacokinetic (PK) and pharmacodynamic (PD) properties of the active (S)-enantiomer of the potent dopamine (DA) agonist 5-hydroxy-2-(N,N,-di-n-propylamino)tetralin (5-OH-DPAT) were investigated in a novel anesthetized animal model." | ( The pharmacokinetics and pharmacological effect of (S)-5-OH-DPAT following controlled delivery with transdermal iontophoresis. Ackaert, OW; Bouwstra, JA; Danhof, M; De Graan, J; Dijkstra, D; Pasqua, OE; Shi, S; Vreeken, R; Westerink, BH, 2011) | 0.37 |
| " Here, we analyzed the occupancy of 5-HT1A receptors in living Sprague-Dawley rat brains by a novel candidate drug for OAB, E2110, using positron emission tomography (PET) imaging, and assessed the utility of a receptor occupancy (RO) assay to establish a pharmacodynamic index translatable between animals and humans." | ( A small-animal pharmacokinetic/pharmacodynamic PET study of central serotonin 1A receptor occupancy by a potential therapeutic agent for overactive bladder. Higuchi, M; Ishihara, H; Maeda, J; Nakatani, Y; Sakai, M; Suhara, T; Suzuki, M; Takenaka, O; Tokunaga, M; Yoshinaga, T; Zhang, MR, 2013) | 0.39 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Paroxetine, in combination with WAY 100635, attenuated the hypothermic effects of 8-OH-DPAT as early as 3 days, with a full reversal evident following 7 days, whereas paroxetine, although attenuating the hypothermic effects in OB group by day 7, only reversed it fully after 14 days." | ( Onset of the effects of the 5-HT1A antagonist, WAY-100635, alone, and in combination with paroxetine, on olfactory bulbectomy and 8-OH-DPAT-induced changes in the rat. Cryan, JF; Leonard, BE; McGrath, C; Norman, TR, 1999) | 0.3 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Thus, the ex vivo binding assay could be utilized to determine the bioavailability of the drug to the brain, and its duration of action." | ( Pharmacokinetics of buspirone as determined by ex vivo (3H)-DPAT binding. Francis, JW; Sethy, VH, 1988) | 0.27 |
| " Compounds 6 and 8 were found to have high oral bioavailability in the rat (63% and 54%, respectively)." | ( 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. Andersson, B; Carlsson, A; Ekman, A; Elebring, T; Lagerkvist, S; Nilsson, J; Stjernlöf, P; Svensson, K; Wikström, H, 1994) | 0.29 |
| " The absolute oral bioavailability of compound 8 (8-triflate) was 4-5 times greater than the corresponding hydroxylated compound." | ( Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. Boije, M; Carlsson, A; Duncan, JN; Ekman, A; King, LJ; Martin, IJ; Romero, AG; Sonesson, C; Svensson, K; Wikström, H, 1993) | 0.29 |
| " After oral administration, terminal t1/2, kelim, apparent volume of distribution and clearance were essentially the same when bioavailability was taken into account." | ( Pharmacokinetics of the 5-hydroxytryptamine1A agonist 8-hydroxy-2-(N,N-di-n-propylamino)tetralin (8-OHDPAT) in the rat after intravenous and oral administration. Caldwell, J; Dring, LG; Mason, JP, 1995) | 0.29 |
| " Determination of the concentrations of (R)-8-OH-DPAT in plasma and brain tissue confirmed a higher bioavailability after oral cavity than after gastric ventricle administration; plasma and brain tissue concentrations of the drug were found to be approximately 3 times those after 10 mumol/kg-1 orally than after 100 mumol/kg-1 gastroventrically at 15-60 min after administration of (R)-8-OH-DPAT." | ( Oral cavity absorption of (R)-8-hydroxy-2-(di-n-propylamino)tetralin and (S)-8-acetyl-2-(di-n-propylamino)tetralin in the rat. Hacksell, U; Lewander, T; Liu, Y; Yu, H, 1996) | 0.58 |
| " However, the final level of the screen, a rat PO/IV bioavailability study, needed far more sensitive assays and often presented significant analytical challenges." | ( Bioanalytical strategies to support a discovery research programme. Rees, SA, 1996) | 0.29 |
| " The maximum plasma concentration of intranasal (S)-UH-301 occurred in about 7 min and the absolute bioavailability seemed to be complete (F=1." | ( Nasal absorption of (S)-UH-301 and its transport into the cerebrospinal fluid of rats. Björk, E; Dahlin, M, 2000) | 0.31 |
| " In contrast, activation of somatodendritc 5-HT(1A) receptors in the raphe nuclei reduces forebrain 5-HT bioavailability and agonists of these receptors, including 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), reliably stimulate eating behavior." | ( Sex differences in the reversal of fluoxetine-induced anorexia following raphe injections of 8-OH-DPAT. Braver, M; Currie, PJ; Mirza, A; Sricharoon, K, 2004) | 0.52 |
| "Targeting serotonin (5-HT) bioavailability with selective 5-HT reuptake inhibitors (SSRIs) remains the most widely used treatment for mood disorders." | ( Regulator of G-protein signaling 6 (RGS6) promotes anxiety and depression by attenuating serotonin-mediated activation of the 5-HT(1A) receptor-adenylyl cyclase axis. Fisher, RA; Maity, B; Meng, F; Stewart, A; Wemmie, JA; Wu, Q; Wunsch, AM, 2014) | 0.4 |
| ", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule." | ( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016) | 0.43 |
We performed acute dose-response and time course behavioral studies in 1-day-old rats with the putative selective agonists 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and 5-methoxy-3(1,2,3,6-tetrahydropyridin-4-yl)1H-indole (RU 24969) (5-HT1B) We found that each compound caused a significant rightward shift in the dose- response curve. This indicated the development of denervation supersensitivity following the destruction of 5-HT neurons.
| Role | Description |
|---|---|
| serotonergic antagonist | Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| tetralins | Compounds containing a tetralin skeleton. |
| phenols | Organic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring. |
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 89.1251 | 0.1413 | 37.9142 | 100.0000 | AID1490 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 23.7781 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 37.9330 | 0.4256 | 12.0591 | 28.1838 | AID504536 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 37.9330 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6561 | 10.0000 | AID4035 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 1.0000 | 0.0001 | 1.4162 | 9.9000 | AID391751; AID643007 |
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | IC50 (µMol) | 0.0012 | 0.0001 | 0.6664 | 10.0000 | AID1059388; AID1285655; AID1336354; AID1597290; AID255313; AID340261; AID346451; AID751855; AID752218 |
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Ki | 0.1603 | 0.0001 | 0.5326 | 10.0000 | AID1152683; AID1193845; AID1196329; AID1227935; AID1336983; AID1459193; AID1517165; AID1593198; AID1597290; AID1627081; AID1664660; AID1667340; AID1675981; AID1702243; AID1720742; AID1798075; AID1830044; AID1854986; AID239577; AID296884; AID320636; AID346017; AID346451; AID3796; AID3800; AID3802; AID3817; AID3822; AID3823; AID3828; AID388704; AID3917; AID391746; AID391754; AID408275; AID408276; AID460124; AID460125; AID465063; AID601165; AID611932; AID643008; AID682996; AID723786; AID751855; AID772375 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.0000 | 0.0004 | 0.6298 | 10.0000 | AID4831 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | Ki | 4.3264 | 0.0002 | 0.6677 | 10.0000 | AID5084; AID5108; AID5109; AID5232; AID5239; AID5270; AID5273 |
| Neuronal acetylcholine receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 0.8318 | 0.0000 | 0.1234 | 5.5000 | AID35499 |
| Cytochrome P450 2C9 | Homo sapiens (human) | Ki | 0.0037 | 0.0003 | 1.6842 | 10.0000 | AID643008 |
| Neuronal acetylcholine receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 0.8318 | 0.0000 | 0.1082 | 5.5000 | AID35499 |
| D(2) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0000 | 0.7472 | 8.0000 | AID63966 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 0.7002 | 0.0000 | 0.6518 | 10.0000 | AID1798075; AID64137; AID64146; AID64147; AID64158 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 5.5000 | 0.0004 | 0.9086 | 10.0000 | AID4831; AID5478 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 3.7859 | 0.0001 | 0.6017 | 10.0000 | AID1798075; AID5084; AID5108; AID5109; AID5232; AID5239; AID5270; AID5273 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6561 | 10.0000 | AID4035 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0002 | 1.8742 | 10.0000 | AID36710 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 0.0001 | 0.9490 | 10.0000 | AID643007 |
| Translocator protein | Rattus norvegicus (Norway rat) | Ki | 0.0043 | 0.0001 | 0.6510 | 8.9300 | AID4002 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6561 | 10.0000 | AID4035 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.5614 | 10.0000 | AID4035 |
| D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 100.0000 | 0.0003 | 0.5026 | 7.7625 | AID61178 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.2773 | 0.0001 | 0.2567 | 5.8000 | AID65618; AID65624; AID65625 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0032 | 0.0003 | 1.3833 | 8.4000 | AID3725; AID3747; AID3755; AID3757; AID4138 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.1796 | 0.0001 | 0.7396 | 10.0000 | AID1442380; AID1713175; AID277973; AID282109; AID302138; AID3470; AID3695; AID37209; AID3996; AID4000; AID4001; AID4002; AID4006; AID4011; AID4017; AID4019; AID4035; AID4064; AID4073; AID4099; AID4103; AID4210; AID4220; AID4332; AID4368; AID4370; AID4411; AID4415; AID4419; AID442987; AID633920; AID64147 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8100 | 0.0003 | 1.0914 | 7.7625 | AID36781 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.8318 | 0.0000 | 0.9296 | 10.0000 | AID35499 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6352 | 10.0000 | AID4035 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6217 | 10.0000 | AID4035 |
| D(2) dopamine receptor | Bos taurus (cattle) | IC50 (µMol) | 0.8000 | 0.0010 | 0.7994 | 8.0000 | AID62167; AID62169 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8100 | 0.0003 | 1.0914 | 7.7625 | AID36781 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.8318 | 0.0000 | 0.9708 | 10.0000 | AID35499 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8100 | 0.0003 | 1.0691 | 7.7625 | AID36781 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.8318 | 0.0000 | 0.9375 | 10.0000 | AID35499 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6758 | 10.0000 | AID4035 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6469 | 10.0000 | AID4035 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0002 | 1.2704 | 10.0000 | AID36710 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.0036 | 0.0000 | 0.5751 | 10.0000 | AID391754; AID643008 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.0000 | 0.0007 | 0.9774 | 9.7000 | AID64685 |
| Sodium-dependent dopamine transporter | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 0.0003 | 0.3708 | 8.1600 | AID6499 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Ki | 1.0000 | 0.0000 | 0.3609 | 10.0000 | AID1459192; AID1593197; AID218801; AID35306; AID35459; AID391753; AID465062; AID643007; AID724005 |
| 5-hydroxytryptamine receptor 1D | Homo sapiens (human) | Ki | 0.1395 | 0.0001 | 0.8087 | 10.0000 | AID4614; AID4898 |
| 5-hydroxytryptamine receptor 1B | Homo sapiens (human) | Ki | 0.5985 | 0.0001 | 0.5485 | 9.2100 | AID4244; AID4933 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 11.0250 | 0.0001 | 0.9549 | 10.0000 | AID4747; AID4748 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6561 | 10.0000 | AID4035 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6561 | 10.0000 | AID4035 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 18.9325 | 0.0003 | 1.2967 | 9.2440 | AID3695; AID4691; AID4699; AID4701 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | Ki | 0.1600 | 0.0010 | 1.6747 | 9.2000 | AID3695 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6712 | 10.0000 | AID4035 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | Ki | 0.1600 | 0.0010 | 1.6747 | 9.2000 | AID3695 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.0000 | 0.0004 | 0.6156 | 10.0000 | AID4831 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | Ki | 4.3264 | 0.0002 | 0.5909 | 10.0000 | AID5084; AID5108; AID5109; AID5232; AID5239; AID5270; AID5273 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.0000 | 0.0003 | 0.8197 | 8.4900 | AID204229 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | Ki | 3.9811 | 0.0000 | 0.7056 | 10.0000 | AID408276 |
| 5-hydroxytryptamine receptor 7 | Rattus norvegicus (Norway rat) | Ki | 0.0761 | 0.0000 | 0.1480 | 3.1800 | AID1798075; AID6648 |
| 5-hydroxytryptamine receptor 7 | Homo sapiens (human) | Ki | 0.3554 | 0.0003 | 0.3806 | 10.0000 | AID1193846; AID1336982; AID1546005; AID1627080; AID282109; AID6587 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | Ki | 0.9797 | 0.0000 | 0.2726 | 10.0000 | AID1459191; AID1593195; AID218797; AID32973; AID36745; AID391751; AID464909; AID643005; AID724007 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | Ki | 2.1056 | 0.0000 | 0.4713 | 10.0000 | AID1459190; AID1593196; AID218799; AID37209; AID37355; AID391752; AID464910; AID643006; AID724006 |
| 5-hydroxytryptamine receptor 3A | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.4841 | 10.0000 | AID5893 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0000 | 1.8194 | 10.0000 | AID36710 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.5410 | 0.0000 | 0.9650 | 10.0000 | AID36901; AID391752 |
| 5-hydroxytryptamine receptor 5A | Homo sapiens (human) | Ki | 2.0000 | 0.0008 | 0.9433 | 5.1600 | AID6479; AID6480; AID6499 |
| 5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 10.0000 | 0.0002 | 0.5229 | 10.0000 | AID6514 |
| 5-hydroxytryptamine receptor 7 | Cavia porcellus (domestic guinea pig) | Ki | 0.0021 | 0.0005 | 0.0018 | 0.0035 | AID296884 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 2.8959 | 0.0001 | 0.5494 | 8.4000 | AID61416; AID61533; AID64291; AID64621 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 1.1602 | 0.0000 | 0.4375 | 10.0000 | AID277975; AID63790; AID65091; AID65714; AID65725; AID6587; AID65911; AID65913 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.5577 | 10.0000 | AID4035 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6403 | 10.0000 | AID4035 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.5708 | 10.0000 | AID4035 |
| D | Mus musculus (house mouse) | Ki | 1.0000 | 0.0004 | 0.7623 | 2.5300 | AID61838 |
| 5-hydroxytryptamine receptor 2A | Bos taurus (cattle) | Ki | 1.0000 | 0.0072 | 0.0926 | 0.1780 | AID5137 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6561 | 10.0000 | AID4035 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 2.4270 | 0.0000 | 0.4901 | 10.0000 | AID204623 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.6561 | 10.0000 | AID4035 |
| 5-hydroxytryptamine receptor 3B | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 0.0002 | 0.5023 | 10.0000 | AID5893 |
| Lysosomal alpha-glucosidase | Bos taurus (cattle) | IC50 (µMol) | 0.0021 | 0.0021 | 0.0160 | 0.0300 | AID3725 |
| Transporter | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1.0000 | 0.0008 | 1.9562 | 8.8000 | AID147730 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| mu-type opioid receptor isoform MOR-1 | Homo sapiens (human) | EC50 (µMol) | 92.4700 | 0.1320 | 3.3004 | 9.5690 | AID720642 |
| 5-hydroxytryptamine receptor 2A | Mus musculus (house mouse) | EC50 (µMol) | 76.0830 | 0.0038 | 1.3621 | 8.3930 | AID720643 |
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | EC50 (µMol) | 0.0204 | 0.0001 | 0.2571 | 8.0000 | AID1234835; AID1234837; AID1512164; AID1675987; AID1675989; AID1675991; AID1675993; AID1702323; AID1702325; AID1702327; AID1824582; AID240272; AID246568; AID277976; AID298093; AID3508; AID388705; AID3909; AID723176; AID773786 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Kd | 0.0025 | 0.0001 | 2.2933 | 8.5114 | AID4197 |
| 5-hydroxytryptamine receptor 1B | Homo sapiens (human) | EC50 (µMol) | 0.2600 | 0.0116 | 0.1388 | 0.4300 | AID4500 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Homo sapiens (human) | Log Ki | 0.0085 | 0.0085 | 0.0086 | 0.0087 | AID3939 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0060 | 0.0060 | AID5336 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | KiAH | 0.0012 | 0.0012 | 0.0012 | 0.0012 | AID4372 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0077 | 0.0094 | AID36761 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0074 | 0.0094 | AID35633; AID36761 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0074 | 0.0094 | AID35633; AID36761 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0074 | 0.0094 | AID35633; AID36761 |
| Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0076 | 0.0093 | AID35583 |
| Alpha-1D adrenergic receptor | Homo sapiens (human) | Log Ki | 0.0060 | 0.0060 | 0.0076 | 0.0093 | AID35583 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0077 | 0.0094 | AID36761 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0077 | 0.0094 | AID36761 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | Log Ki | 0.0060 | 0.0060 | 0.0077 | 0.0094 | AID36761 |
| Alpha-1A adrenergic receptor | Homo sapiens (human) | Log Ki | 0.0060 | 0.0060 | 0.0077 | 0.0094 | AID36761 |
| Alpha-1B adrenergic receptor | Homo sapiens (human) | Log Ki | 0.0060 | 0.0060 | 0.0070 | 0.0080 | AID37492 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1702327 | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay | |||
| AID3951 | Antagonist activity at 5-hydroxytryptamine 1A receptor against (+)-8-OH-DPAT induced hypothermia in mice 30 min after administration of the compound | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID181017 | Percent reduction of hemispheres in cortex was measured in the brain of reserpinized rats. | 1982 | Journal of medicinal chemistry, Aug, Volume: 25, Issue:8 | Monophenolic octahydrobenzo[f]quinolines: central dopamine- and serotonin-receptor stimulating activity. |
| AID113659 | Effect in the social interaction behavioral test in mice | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. |
| AID4748 | Inhibition of [3H]mesulergine binding to 5-hydroxytryptamine 1C receptor of pig choroid Plexus | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID36761 | The binding affinity was evaluated on cloned human alpha-1A adrenergic receptor expressed in chinese hamster ovary(CHO) cells by using [3H]prazosin as radioligand. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID63197 | Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID138669 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 0.0 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID1172050 | Induction of hypothermia in mouse assessed as change in body temperature at 5 mg/kg, ip administered 30 mins before test and measured 30 mins post dose in presence of 0.3 mg/kg, sc 5HT1A receptor antagonist WAY 100635 | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT₁A receptor functional profile. |
| AID230026 | Ratio of Km to that Vmax in crude rat liver microsomes was determined | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID177648 | Effect on hypothermia in rats following peroral administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID232149 | Ratio of 5-HT concentration to 5-HIAA concentration in olfactory tubercle region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID449124 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, sc after 30 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID566911 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, ip after 90 mins by inducible hypothermia test | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. part 3. |
| AID16505 | Cmax in minutes at a po dose of 20.0(pmol/g/h). | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID4024 | Binding was determined on 5-hydroxytryptamine 1A receptor in rat hippocampal membranes | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID408275 | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
| AID4002 | Binding affinity was tested on 5-hydroxytryptamine 1A receptor using radioligand [3H]5-HT binding assay. | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives. |
| AID232144 | Ratio of 5-HT concentration to 5-HIAA concentration in amygdala region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID188722 | Maximal reduction in percent (Partial response) of DOPA accumulation rat hemispheres at highest test dose of 61 uM/Kg (po); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID1830041 | Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID36901 | In vitro binding affinity towards alpha-1A adrenergic receptor through displacement of [3H]prazosin in epididymal rat vas deferens. | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor. |
| AID751855 | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
| AID1675997 | Bias factor, ratio of biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation to biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor | |||
| AID3889 | Agonist efficacy on 5-hydroxytryptamine 1A receptor subtype | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID3470 | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampal membranes | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID177899 | Inhibition of dopamine accumulation in striatum part of rat brain after subcutaneous administration; I= Inactive | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 8-Hydroxy-2-(di-n-propylamino)tetralin, a new centrally acting 5-hydroxytryptamine receptor agonist. |
| AID3757 | In vitro binding affinity measured on serotonin 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand. | 1995 | Journal of medicinal chemistry, Mar-17, Volume: 38, Issue:6 | High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2. |
| AID177865 | Inhibition of 5-HT1A cell firing in rats | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID1234835 | Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2. |
| AID340261 | Inhibition of human 5HT1A receptor | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. |
| AID4244 | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand | 1998 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11 | Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. |
| AID1675983 | Displacement of [3H]methylspiperone from human D2 receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method | |||
| AID1336983 | Displacement of [3H]-8-OH-DPAT from recombinant human 5-HT1A receptor expressed in CHOK1 cell membranes after 1 hr by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | New N- and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HT |
| AID64685 | Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters. |
| AID1337886 | Agonist activity at recombinant human 5-HT1A receptor expressed in HeLa cell membranes assessed as induction of [35S]GTPgammaS binding up to 10 uM preincubated for 20 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation | |||
| AID187802 | 8-OH-DPAT appropriate response rate in % at 0.2 mg/kg where stimulus generalization occurred(7/7 no of animals) | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID247126 | Percent maximal response of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan. |
| AID643007 | Displacement of [3H]prazosin from human recombinant Alpha-1D adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors. |
| AID170911 | Brain Concentration at 15(umol/kg, sc) with tropolone pretreatment in rat cerebellum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID121116 | Effect on rectal temperature in mice at dose of 0.5 mg/kg sc. | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. |
| AID1593204 | Agonist activity at cloned human 5-HT1A receptor transfected in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition and measured after 30 mins by liquid scintillation cou | |||
| AID1702328 | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay relative to serotonin | |||
| AID3508 | EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
| AID1675996 | Bias factor, ratio of biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels to biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressin | |||
| AID510560 | Agonist activity at human cloned 5HT1A receptor expressed in human HeLa cells assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting relative to maximal 5HT response | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
| AID1675998 | Bias factor, ratio of biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation to biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-e | |||
| AID124905 | The in vivo compartmental activity was evaluated as minimum significant active dose measured by punishment test | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID178702 | Subcutaneous dose giving half-maximal decrease of Dopa formation in the rat brain (striatum) | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1 | 8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-hydroxytryptamine receptor agonists. |
| AID138497 | Behavioral time in mouse isolation-induced aggression assay at 0.9 umol/kg administered intraperitoneally | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID174318 | Influence on 5-hydroxyindoleacetic acid (5-HIAA) concentration in olfactory tubercle region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID4215 | Binding affinity against 5-hydroxytryptamine 1A receptor by displacing [3H]8-OH-DPAT radioligand in rat cortex membrane | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Alpha(1)-adrenoceptor antagonists. 4. Pharmacophore-based design, synthesis, and biological evaluation of new imidazo-, benzimidazo-, and indoloarylpiperazine derivatives. |
| AID35197 | Binding affinity towards Alpha-2 adrenergic receptor was determined in rat cortex membranes using [3H]rauwolscine as radioligand; No data | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety. |
| AID177392 | 5-HTP accumulation in hemispheres of reserpinized rats following subcutaneous administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID174312 | Influence on 5-hydroxy tryptamine (5-HT) concentration in parietal cortex region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID465067 | Selectivity ratio of pKi for human 5-HT1A receptor to pKi for human alpha1 adrenergic receptor | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of a new series of 5-HT1A receptor agonists. |
| AID3996 | Binding affinity of compound against 5-hydroxytryptamine 1A receptor binding site using radioligand [3H]8-OH-DPAT | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine. |
| AID4092 | Displacement of radioligand [3H]2-(di-N-propylamino)-8-hydroxytetralin from 5-hydroxytryptamine 1A receptor in rat frontal cortex homogenate | 1993 | Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19 | Structure-affinity relationship studies on 5-HT1A receptor ligands. 1. Heterobicyclic phenylpiperazines with N4-alkyl substituents. |
| AID177649 | Effect on hypothermia in rats following subcutaneous administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID26659 | Half-life of the compound, after iv administration in rat, activity expressed as %. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID35633 | The binding affinity was evaluated on alpha-2 adrenergic receptor expressed in rat cortex by using [3H]rauwolscine as radioligand. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID3727 | Binding affinity against serotonin 5-hydroxytryptamine 1A receptor in rat hippocampus membrane using [3H]8-OH-DPAT as radioligand | 1996 | Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16 | 1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3. |
| AID64137 | Binding affinity against Dopamine receptor D2 | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID288885 | Decrease in body temperature in Swiss Albino mouse at 5 mg/kg, sc after 60 mins relative control | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID3487 | In vivo binding affinity towards [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in bovine hippocampus. | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID177320 | In vivo evaluation for 5-HTP accumulation in the limbic system in male rats (po) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID176091 | Effect on the synthesis rates of serotonin in the rat ventral limbic brain region at 0.3 micro mol/kg. values are given as percent change from the control | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID5137 | Binding affinity against 5-hydroxytryptamine 2 receptor | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID76295 | The level of 5-HIAA (hypothalamus) measured by means of HPCL with electrochemical detection methods at 6.250 (umol/kg, sc) | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. |
| AID170781 | Brain Concentration of 7,8-di-OH-DPAT after 15(umol/kg) sc administration with tropolone pretreatment in rat cortex | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID178042 | Effective dose for half-maximal decrease in the accumulation of DOPA in reserpinized rat brain hemispheral area by po administration; Partial response at the highest dose tested | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID5270 | Binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 (5-HT2) receptor using [3H]KET as a radioligand | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Central serotonin receptors as targets for drug research. |
| AID177391 | 5-HTP accumulation in hemispheres of reserpinized rats following peroral administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID1824582 | Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID4103 | In vitro binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT (agonist) as radioligand (sc) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID4415 | In vitro by displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor on rat cortical membrane | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4 | New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. |
| AID3893 | Agonist efficacy was evaluated as ([35S]GTP binding on 5-hydroxytryptamine 1A serotonergic receptors. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID309489 | Decrease in body temperature in WAY 100635 pretreated Swiss Albino mouse at 5 mg/kg after 30 mins | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
| AID772374 | Agonist activity at human 5HT1A receptor relative to control | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID65911 | Displacement of the radioligand [3H]spiperone from D2 receptor | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID4375 | Antagonist activity to stimulate binding of [35S]-GTP-gamma S binding to 5-hydroxytryptamine 1A receptor in isolated rat hippocampal membranes | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID391758 | Agonist activity at human cloned 5HT1A receptor expressed in human HeLa cell membrane assessed as stimulation of [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
| AID170783 | Brain Concentration of 7,8-di-OH-DPAT after 15(umol/kg) sc administration without tropolone pretreatment in rat cerebellum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID168706 | Inhibitory concentration of compound was tested as agonist activity against DRN serotonergic neurons firing in the dorsal raphe nucleus | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID391751 | Displacement of [3H]prazosin from human cloned alpha1A adrenoceptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
| AID181113 | compound was tested in vivo for DOPA accumulation in corpus striatum against reserpine-pretreated rats; I=inactive at the highest dose tested | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID37355 | Displacement of [3H]prazosin from human cloned Alpha-1B adrenergic receptor | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID177475 | Effect evaluated in vivo on DA synthesis in limbic system at ED50 umol/kg after peroral administration | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. |
| AID138794 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 0.9 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID1517930 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, ip measured after 30 mins by thermometric method (Rvb = -0.2 to 0.4 deg C) | |||
| AID61178 | In vitro binding activity against dopamine D1 receptor from homogenized rat brain, using [3H]SCH-23390 as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties. |
| AID1517165 | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHO-K1 cells incubated for 60 mins by liquid scintillation counting method | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | [1]Benzothieno[3,2-d]pyrimidine derivatives as ligands for the serotonergic 5-HT |
| AID219037 | Percent of arterial blood pressure at sympathetic nerve activity (SND) dose value was determined | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID1675982 | Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat cortex membranes measured after 30 mins by Microbeta2 scintillation counting method | |||
| AID1459192 | Displacement of [3H]prazosin from recombinant human alpha-1d adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method | |||
| AID5009 | Inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor of bovine frontal cortex | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID121118 | Effect on rectal temperature in mice at dose of 10 mg/kg sc. | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. |
| AID1702325 | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | |||
| AID13471 | Area under curve ratio was determined (po/iv) in rat | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID170780 | Brain Concentration of 7,8-di-OH-DPAT after 15(umol/kg) sc administration with tropolone pretreatment in rat cerebellum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID177279 | ED50 value was measured as dose required to produce a half-maximal reduction of Serotonin (5-HTP) accumulation in striatum of reserpinized rat brain | 1982 | Journal of medicinal chemistry, Aug, Volume: 25, Issue:8 | Monophenolic octahydrobenzo[f]quinolines: central dopamine- and serotonin-receptor stimulating activity. |
| AID232150 | Ratio of 5-HT concentration to 5-HIAA concentration in parietal cortex region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID26826 | Compound was evaluated for the Ionization constants at 37 degree Centigrade pKa2 | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site. |
| AID176085 | Effect on the synthesis rates of serotonin in the rat ventral limbic brain region 0.3 micro mol/kg. | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID63790 | Displacement of [3H]spiperone from rat brain Dopamine receptor D2 | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID3695 | Evaluated for binding affinity towards rat cortical membranes at 5-hydroxytryptamine 1 receptor binding site by using [3H]-5-HT as a radioligand. | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Central serotonin receptors as targets for drug research. |
| AID1601989 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, sc measured after 30 mins by thermometric method (Rvb <= 0.4 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID3523 | Percent of maximum effect on binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
| AID1702360 | Antidepressant-like activity in Wistar rat assessed as minimum effective dose causing reduction in immobility time after sc administration with compound 60 mins prior to testing and measured for 5 mins test period by Porsolt-forced swim test | |||
| AID4000 | Binding affinity for 5-hydroxytryptamine 1A receptor with [3H]5-HT | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1 | Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes. |
| AID178040 | Effective dose for half-maximal decrease in the accumulation of 5-hydroxytryptophan (5-HTP) in reserpinized rat brain striatal area by po administration | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID50209 | Dose on arterial blood pressure (BP) in anesthetized cat | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID35306 | Binding affinity towarda alpha-1D adrenergic receptor | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID192922 | Ability to counteract the 8-OH-DPAT (1 mg/kg sc)-induced Hypothermia in rats (n=4) and evaluated for the decrease in body temperature (degrees Celsius) at 0.1(micro mol/kg) | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
| AID176529 | DOPA accumulation in hemispheres of reserpinized rats following peroral administration at highest dose tested (50 umol/kg); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID191872 | Apparent kinetic constant(Vmax) for the aromatic hydroxylation on crude rat liver microsomes at 1 mg of protein | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID37209 | Binding affinity was determined on human cloned alpha-1B adrenergic receptor | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID239577 | Displacement of 8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in chinese hamster ovary cells | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan. |
| AID3716 | Binding affinity at [3H]8-OH-DPAT-Labeled 5-hydroxytryptamine 1A receptor sites in rat brain hippocampal membranes expressed as Hill values | 1989 | Journal of medicinal chemistry, Jan, Volume: 32, Issue:1 | 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. |
| AID1830039 | Displacement of [3H]LSD from human recombinant 5-HT2C receptor expressed in HEK cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID139180 | Tested in vivo for the maximum temperature decrease in mouse hypothermia assay. | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID76165 | Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1A receptor expressed in CHO-K1 cells. | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. |
| AID49588 | Maximum decrease in blood pressure observed following 1 mg/kg dose in anesthetized cat | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID4018 | Binding affinity towards 5-hydroxytryptamine 1A receptor sites, in rat striatum membranes using [3H]- sandoz 205-501 as radioligand | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist. |
| AID61416 | Binding affinity towards rat Dopamine receptor D2 was evaluated using [3H]- spiroperidol as radioligand | 1996 | Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25 | Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4. |
| AID3899 | Negative logarithm of concentration required to obtain 50% maximal stimulation of [35S]GTP gamma-S binding to human cloned 5-HT1A receptors of cell membranes from HeLa cells | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID1517164 | Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | [1]Benzothieno[3,2-d]pyrimidine derivatives as ligands for the serotonergic 5-HT |
| AID1830038 | Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in CHO cells by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID174320 | Influence on 5-hydroxyindoleacetic acid (5-HIAA) concentration in septum region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID3952 | Antagonist activity at 5-hydroxytryptamine 1A receptor against (+)-8-OH-DPAT induced hypothermia in mice 60 min after administration of the compound | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID35499 | Displacement of [3H]rauwolscine from rat brain Alpha-2 adrenergic receptor | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID124446 | Swimming activity of the treated mice/control mice at 4.0 umol/kg, sc (p < 0.001) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID1059389 | Displacement of [3H]paroxetine from SERT in rat cortical membranes after 6 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor. |
| AID64621 | The compound was tested in vitro for inhibitory activity against dopamine receptor in rats using [3H]spiperone as radioligand | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. |
| AID177496 | Effect on 5-HTP accumulation in hemispheres of rat. | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID177387 | 5-HTP accumulation in corpus striatum of reserpinized rats following peroral administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID177873 | Inhibition of 5-Hydroxy tryptamine accumulation in striatum part of rat brain after subcutaneous administration | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 8-Hydroxy-2-(di-n-propylamino)tetralin, a new centrally acting 5-hydroxytryptamine receptor agonist. |
| AID189833 | In vivo motor activity at 61 umol/kg (po) in male rats expressed as accumulated counts/30 min (p < 0.001) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID64158 | Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D2 in Sf 9 cells | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. |
| AID138670 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 0.0 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID131867 | Effective dose on hypothermia in mouse when administered through peroral route | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID465068 | Agonist activity at human recombinant 5HT1A receptor expressed in human HeLa cells by [35S]GTPgammaS binding assay relative to serotonin | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of a new series of 5-HT1A receptor agonists. |
| AID392048 | Cardiotoxicity in iv dosed Dunkin-Hartley guinea pig assessed as drug level required to evoke 50 ms QTc prolongation administered as 3 fold cumulative doses measured every 10 seconds at end of every 20 mins follow up period of individual dose by ECG | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation. |
| AID61838 | Binding affinity against Dopamine receptor D1 | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID232147 | Ratio of 5-HT concentration to 5-HIAA concentration in hippocampus region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID138489 | Behavioral time in mouse isolation-induced aggression assay 0 umol/kg administered intraperitoneally | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID49594 | Maximum decrease on arterial blood pressure at 1 mg/kg | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID177897 | Inhibition of dopamine accumulation in limbic part of rat brain after subcutaneous administration; I= Inactive | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 8-Hydroxy-2-(di-n-propylamino)tetralin, a new centrally acting 5-hydroxytryptamine receptor agonist. |
| AID138641 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 0.0 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID724006 | Displacement of [3H]prazosin from human recombinant alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition. |
| AID65913 | Binding affinity against Dopamine receptor D2 from CHO-K1 cells, using [3H]U-86,170 as the radioligand. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID176065 | Effect on the synthesis rates of dopamine in the rat ventral limbic brain region at 3.0 micro mol/kg. values are given as percent change from the control | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID49577 | Maximum decrease of sympathetic nerve activity (SND) in anesthetized cat | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID65624 | Inhibitory activity against [125I]- NCQ298 binding to dopamine receptor D3 in Sf 9 cells | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. |
| AID232146 | Ratio of 5-HT concentration to 5-HIAA concentration in frontal cortex region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID391752 | Displacement of [3H]prazosin from human cloned Alpha-1B adrenoceptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
| AID177318 | In vivo evaluation for 5-HTP accumulation in the hemispheres in male rats (po) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID1546005 | Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Structure-activity relationships of serotonin 5-HT |
| AID4037 | Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [3H]8-OH-DPAT in membrane homogenates of hippocampal tissue of rat brain | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. |
| AID62167 | Binding affinity against D2 receptor in calf caudate nucleus | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID246568 | In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan. |
| AID408280 | Intrinsic activity at human recombinant 5HT1A receptor expressed in HEK293 cells by [35S]GTPgammaS binding relative to 5 hydroxytryptamine | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
| AID298092 | Binding affinity to 5HT1A receptor in rat cortex membrane | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID138645 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 0.3 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID174314 | Influence on 5-hydroxyindoleacetic acid (5-HIAA) concentration in caudate region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID298095 | Induction of forepaw treading in orally dosed rat after 60 mins | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID391753 | Displacement of [3H]prazosin from human cloned alpha1D adrenoceptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
| AID224035 | Motor activity was measured by motility testing on injecting the compound subcutaneously into rats at the dose of 12.5 umol/kg | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID49576 | Maximum decrease of arterial blood pressure at sympathetic nerve activity (SND) in anesthetized cat has been observed following 1 mg/kg dose | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID5239 | Binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 receptor binding site by using [3H]- DOB as a radioligand. | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Central serotonin receptors as targets for drug research. |
| AID138642 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 0.0 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID204612 | Inhibition of [3H]DTG binding to sigma receptor in rat hippocampus | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID1593196 | Displacement of [3H]Prazosin from human recombinant alpha 1B adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | |||
| AID180724 | The concentration yielding a half maximal decrease of the 5-HTP was determined in rat limbic system | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID218799 | Binding affinity towards human cloned alpha-1B-adrenoceptor using [3H]prazosin as radioligand | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
| AID177314 | In vivo evaluation for 5-HTP accumulation in the corpus striatum in male rats (po) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID65618 | Binding affinity against Dopamine receptor D3 from CHO-K1 cells, using [3H]spiperone as the radioligand. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID63966 | Inhibitory concentration against binding of Dopamine receptor D2 by displacement of [3H]spiperone | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. |
| AID4035 | Binding affinity towards 5-hydroxytryptamine 1A receptor | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID178037 | Effective dose for half-maximal decrease in the accumulation of 5-hydroxytryptophan (5-HTP) in reserpinized rat brain hemispheral area by sc administration | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID177396 | 5-HTP accumulation in limbic system of reserpinized rats following peroral administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID288910 | Decrease in body temperature in Swiss Albino mouse at 5 mg/kg, sc after 30 mins relative control | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID10943 | Bioavailability in male Sprague-Dawley rats, after the po administration at a dose of 20.0(pmol/g/h) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID25014 | Compound was evaluated for the percentage ionization at the pH 7.4 at 37 degree Centigrade | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site. |
| AID277978 | Normalizing effect on methylphenidate-induced behaviours in ip dosed rat after 30 min | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID449037 | Reduction of 8-OH-DPAT-induced hypothermia in Swiss albino mouse at 0.1 mg/kg, sc administered 15 mins prior 8-OH-DPAT challenge measured after 15 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID4155 | Percent increase of R(+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in isolated rat hippocampal membranes | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID1172051 | Induction of hypothermia in mouse assessed as change in body temperature at 5 mg/kg, ip administered 30 mins before test and measured 60 mins post dose in presence of 0.3 mg/kg, sc 5HT1A receptor antagonist WAY 100635 | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Antidepressant- and anxiolytic-like activity of 7-phenylpiperazinylalkyl-1,3-dimethyl-purine-2,6-dione derivatives with diversified 5-HT₁A receptor functional profile. |
| AID4011 | Binding affinity towards 5-hydroxytryptamine 1A receptor from rat hippocampal membranes | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands. |
| AID177397 | 5-HTP accumulation in limbic system of reserpinized rats following subcutaneous administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID1675989 | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay | |||
| AID465062 | Displacement of [3H]prazosin from human Alpha-1D adrenergic receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of a new series of 5-HT1A receptor agonists. |
| AID232151 | Ratio of 5-HT concentration to 5-HIAA concentration in septum region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID5232 | Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1 | Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes. |
| AID76312 | The level of 5-HT (prefrontal cortex) measured by means of HPCL with electrochemical detection methods at 6.250 (umol/kg, sc) | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. |
| AID723176 | Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT₁A/5-HT₂A/5-HT₇ and dopamine D₂/D₃ receptors. |
| AID138814 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 30 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID682996 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect. |
| AID181096 | compound was tested in vivo for 5-HTP accumulation in corpus striatum against reserpine-pretreated rats. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID460124 | Binding affinity to 5HT1A receptor | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist. |
| AID174315 | Influence on 5-hydroxyindoleacetic acid (5-HIAA) concentration in frontal cortex region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID178697 | Subcutaneous dose giving half-maximal decrease of 5-HTP formation in the rat brain hemispheres (cortex) | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1 | 8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-hydroxytryptamine receptor agonists. |
| AID449150 | Antidepressant activity in Swiss albino mouse assessed as reduction of immobility time at 2 mg/kg, sc administered 30 mins before test measured 6 mins test session after 2 mins habituation period by forced swimming test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID172487 | Compound was tested for 5-HT behavioral response in reserpine pretreated rats; +5HT syndrome | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID35583 | The binding affinity was evaluated on cloned human alpha-1D adrenergic receptor expressed in chinese hamster ovary(CHO) cells by using [3H]prazosin as radioligand. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID1675981 | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method | |||
| AID3755 | In vitro binding activity against 5-hydroxytryptamine 1A receptor from homogenized rat brain, using [3H]8-OH-DPAT as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties. |
| AID1675994 | Bias factor, ratio of biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels to biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as | |||
| AID4001 | Binding affinity to the rat 5-hydroxytryptamine 1A receptor | 2003 | Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4 | Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands. |
| AID170914 | Brain Concentration at 15(umol/kg, sc) without tropolone pretreatment in rat cerebellum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID64803 | Inhibition of [3H]spiperone binding to Dopamine receptor D3 in bovine cortex | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID62343 | Inhibition of [3H]raclopride binding to Dopamine receptor D2 of bovine striatum | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID683000 | Agonist activity at human 5HT1A receptor expressed in HeLa cells assessed as [35S]GTPgammaS binding incubated for 20 mins prior to [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting relative to 8-OH-DPAT | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect. |
| AID35845 | Binding affinity against alpha-1 adrenergic receptor in calf frontal cortex | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID65625 | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand. |
| AID1702274 | Bias factor, ratio of biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels to biased agonist activity at human recombinant 5-HT1A receptor stably expressed in C | |||
| AID240272 | In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan. |
| AID5108 | Binding affinity towards 5-hydroxytryptamine 2 receptor using [3H]- 1-(4-bromo-2,5-dimethoxy-phenyl)-2-aminopropane (D) as radioligand | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID36781 | Binding affinity towards rat Alpha-2 adrenergic receptor was evaluated using [3H]- yohimbine as radioligand | 1996 | Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25 | Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4. |
| AID124314 | Swimming activity of the treated mice/control mice at 1.2 umol/kg, sc | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID224256 | Maximum decrease in temperature when compound is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID229085 | Ratio of the 5-HTP accumulation decrease in limbic regions after oral and subcutaneous administration in rat. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID1234838 | Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay relative to 5-HT | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2. |
| AID178700 | Subcutaneous dose giving half-maximal decrease of Dopa formation in the rat brain (limbic) | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1 | 8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-hydroxytryptamine receptor agonists. |
| AID174310 | Influence on 5-hydroxy tryptamine (5-HT) concentration in hypothalamus region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID124316 | Swimming activity of the treated mice/control mice at 12 umol/kg, sc (p < 0.001) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID177647 | Effect on dopamine accumulation in striatum of rat; Inactive | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID449054 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, sc after 120 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID4099 | In vitro displacement of radioactively labeled ligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor site in CHO cells | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
| AID4411 | Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models. |
| AID566912 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, ip after 120 mins by inducible hypothermia test | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. part 3. |
| AID4376 | Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding in rat hippocampal membranes | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID4713 | Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor. |
| AID1675995 | Bias factor, ratio of biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels to biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor express | |||
| AID178693 | Subcutaneous dose giving half-maximal decrease of 5-HTP formation in the rat brain (limbic) | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1 | 8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-hydroxytryptamine receptor agonists. |
| AID288886 | Effect on compound induced hypothermia in Swiss Albino mouse at 5 mg/kg in presence of 0.1 mg/kg WAY 100635 after 60 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID3768 | Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID169114 | Compound was tested for the 5-HT presence, at 50 umol/kg after subcutaneous administration; Absent | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. |
| AID138655 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 3.0 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID65403 | Binding affinity against [3H]raclopride-labeled dopamine receptor D2 in rat striatum. | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID1459191 | Displacement of [3H]prazosin from recombinant human alpha-1a adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method | |||
| AID298094 | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTP-gamma-S binding relative to 5-hydroxytryptamine | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID64952 | Binding affinity against D2 receptor in homogenated rat brain tissue, using by [3H]spiperone as radioligand | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID177399 | 5-HTP accumulation in limbic system was determined in vivo | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
| AID131726 | Effective dose on hypothermia in mouse when administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID10937 | Bioavailability in male Sprague-Dawley rats, after the iv administration at a dose of 1.0(pmol/g/h) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID48703 | Minimum effective dose administered intravenously for decrease in heart rate in cat | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine. |
| AID4898 | Binding affinity against 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells, using [3H]-5-HT as the radioligand. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID1196329 | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK-293 cells | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. |
| AID1702355 | Toxicity in Wistar rat assessed as minimum effective dose causing effect on flat body posture administered subcutaneously with compound and observed after 60 mins post treatment | |||
| AID773787 | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in Sprague-Dawley rat cerebral cortex after 15 mins | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | New serotonin 5-HT1A receptor agonists endowed with antinociceptive activity in vivo. |
| AID138821 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 9.1 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID3708 | Agonistic activity (induction of forepaw treading in rats)on postsynaptic 5-hydroxytryptamine 1A receptor while subcutaneous administration | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID298098 | Antidepressant like activity in orally dosed rat after 60 mins by forced swimming test | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID178695 | Subcutaneous dose giving half-maximal decrease of 5-HTP formation in the rat brain (striatum) | 1984 | Journal of medicinal chemistry, Jan, Volume: 27, Issue:1 | 8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-hydroxytryptamine receptor agonists. |
| AID177476 | Effect evaluated in vivo on DA synthesis in limbic system at ED50 umol/kg after subcutaneous administration | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. |
| AID4614 | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1D receptor using [3H]-5-CT as radioligand | 1998 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11 | Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. |
| AID330661 | Effect on life span of Caenorhabditis elegans at 200 uM | 2007 | Nature, Nov-22, Volume: 450, Issue:7169 | An antidepressant that extends lifespan in adult Caenorhabditis elegans. |
| AID1664660 | Displacement of [3H]-WAY100635 from human 5-HT1A receptor expresssed in stable CHO cell membrane incubated for 90 mins by microbeta counting method | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT |
| AID309490 | Decrease in body temperature in WAY 100635 pretreated Swiss Albino mouse at 5 mg/kg after 60 mins | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | The influence of modifications in imide fragment structure on 5-HT(1A) and 5-HT(7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl)piperazines. |
| AID391746 | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18 | Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. |
| AID13542 | Area under curve at 20 uM/dg administered perorally | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID449055 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, sc after 90 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID6479 | Binding affinity towards human 5-hydroxytryptamine 5A receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID1593195 | Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | |||
| AID138637 | Behavioral time in mouse isolation-induced aggression behavioral assay at 30 umol/kg administered intraperitoneally (*P<0.05) | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID1667340 | Binding affinity to human 5HT1A receptor | 2020 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8 | Identification of C10 nitrogen-containing aporphines with dopamine D |
| AID6587 | Displacement of [3H]5-HT from human 5-hydroxytryptamine 7 receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID4332 | Inhibitory affinity constant against 5-hydroxytryptamine 1A receptor | 1995 | Journal of medicinal chemistry, May-12, Volume: 38, Issue:10 | Buspirone analogues as ligands of the 5-HT1A receptor. 1. The molecular structure of buspirone and its two analogues. |
| AID180720 | The concentration yielding a half maximal decrease of the 5-HTP was determined in rat brain striatum | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID460125 | Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist. |
| AID170280 | In vivo motor activity at 0.2 umol/kg (sc) in male rats expressed as accumulated counts/30 min (p < 0.05) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID174306 | Influence on 5-hydroxy tryptamine (5-HT) concentration in amygdala region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID3671 | Compound was evaluated for the inhibition of [3H]5-HT (concentration of 12 nM) specific binding to rat hippocampus | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine. |
| AID4933 | Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID4038 | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat cerebral cortex | 2003 | Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2 | alpha1-Adrenoceptor antagonists. 5. Pyridazinone-arylpiperazines. Probing the influence on affinity and selectivity of both ortho-alkoxy groups at the arylpiperazine moiety and cyclic substituents at the pyridazinone nucleus. |
| AID3751 | In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1 | Mixed 5-HT1A/D-2 activity of a new model of arylpiperazines: 1-aryl-4-[3-(1,2-dihydronaphthalen-4-yl)-n-propyl]piperazines. 1. Synthesis and structure-activity relationships. |
| AID177643 | Effect on dopamine accumulation in hemispheres of rat; Inactive | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID32973 | Binding affinity was determined on human cloned Alpha-1A adrenoceptor | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID35964 | Displacement of [3H]-prazosin from Alpha-1 adrenergic receptor of bovine frontal cortex | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID190912 | Compound was tested for gross behavioral response in rats; full-blown 5-HT syndrome | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID219195 | Maximum decrease of sympathetic nerve activity (SND) in anesthetized cat has been expressed as percent control | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID177321 | In vivo evaluation for 5-HTP accumulation in the limbic system in male rats (sc) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID277975 | Displacement of [3H]YM-09151-2 from rat striatum D2 receptor | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID1702324 | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay relative to serotonin | |||
| AID723785 | Agonist activity at human 5HT1A receptor expressed in HeLa cell membranes by [35S]GTPgammaS binding assay | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition. |
| AID1702326 | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay relative to serotonin | |||
| AID177388 | 5-HTP accumulation in corpus striatum of reserpinized rats following subcutaneous administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID391754 | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in human HeLa cells | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
| AID5007 | Binding affinity to 5-hydroxytryptamine 2 receptor using calf frontal cortex, [3H]- ketanserin, and spiperone for NSB | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | 3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans]. |
| AID55586 | Inhibition of firing rates of dopaminergic neurons in the substantia nigra pars compacta by intravenous injection in rats. | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID4831 | Inhibitory concentration against 5-hydroxytryptamine 2 receptor from striata of male Wistar rats by displacement of [3H]-ketanserin | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. |
| AID346451 | Displacement of radiolabeled 8OH-DPAT from human 5HT1A receptor | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. |
| AID3478 | Binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in bovine hippocampus | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID1059388 | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor. |
| AID178041 | Effective dose for half-maximal decrease in the accumulation of 5-hydroxytryptophan (5-HTP) in reserpinized rat brain striatal area by sc administration | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID177131 | ED50 value was measured as dose required to produce a half-maximal reduction of Dopa accumulation in the striatum of reserpinized rat brain; I is Inactive, no significant effect at doses approximately 40 times the ED50 for Dopa accumulation | 1982 | Journal of medicinal chemistry, Aug, Volume: 25, Issue:8 | Monophenolic octahydrobenzo[f]quinolines: central dopamine- and serotonin-receptor stimulating activity. |
| AID14275 | Maximum concentration of the drug at 1 umol/dg administered intravenously | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID3828 | Binding affinity towards human cloned 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
| AID138795 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 0.9 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID4216 | Binding affinity against 5-hydroxytryptamine 1A receptor in homogenated rat brain tissue, using by [3H]8-OH-DPAT as radioligand | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID197200 | Evaluated for the inhibition of footshock-evoked ultrasonic vocalization in rats after administration of 8-OH-DPAT (0.1 mg/kg sc) alone or in combination with WAY-100635 | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. |
| AID1459193 | Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor expressed in human HeLa cell membranes after 30 mins by liquid scintillation counting method | |||
| AID27922 | Calculated partition coefficient (clogP) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID391759 | Agonist activity at human cloned 5HT1A receptor expressed in HeLa cell membrane assessed as stimulation of [35S]GTPgammaS binding relative to 5-hydroxytryptamine | 2008 | Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents. |
| AID723784 | Agonist activity at human 5HT1A receptor expressed in HeLa cell membranes by [35S]GTPgammaS binding assay relative to 5-Hydroxytryptamine | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition. |
| AID4747 | Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand. | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Central serotonin receptors as targets for drug research. |
| AID1234836 | Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA relative to 5-HT | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2. |
| AID3790 | Dissociation constant against human 5-hydroxytryptamine 1A receptor receptor | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
| AID178044 | Effective dose for half-maximal decrease in the accumulation of DOPA in reserpinized rat brain limbic area by po administration; Partial response at the highest dose tested | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID177169 | In vivo effects on DA (dopamine) synthesis in corps striatum was reported after subcutaneous administration to reserpinized rats; I = inactive at highest dose 45 umol/kg | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
| AID184433 | Apparent kinetic constant(Km) for the aromatic hydroxylation on crude rat liver microsomes. | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID449056 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, sc after 60 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID1512164 | Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay | 2019 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 29, Issue:21 | Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives. |
| AID181106 | compound was tested in vivo for 5-HTP accumulation in limbic system against reserpine-pretreated rats. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID4358 | The compound was tested for binding affinity on [3H]8-OH-DPAT as specific ligand on 5-hydroxytryptamine 1A receptor in rat hippocampus | 1999 | Journal of medicinal chemistry, Jan-14, Volume: 42, Issue:1 | Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton. |
| AID464909 | Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of a new series of 5-HT1A receptor agonists. |
| AID50208 | Percent of arterial blood pressure at sympathetic nerve activity (SND) dose value was determined | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID6514 | Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID1593197 | Displacement of [3H]Prazosin from human recombinant alpha 1D adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay | |||
| AID178197 | Effective dose in blocking conditioned avoidance responding (CAR) in the rat when administered intraperitoneally | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy. |
| AID16939 | In vitro metabolic stability of the test compound was evaluated after incubation in the presence of freshly isolated rat hepatocytes | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
| AID63045 | Compound was evaluated for binding affinity on Dopamine receptor D1 using calf striatum | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | 3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans]. |
| AID1702243 | Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method | |||
| AID180737 | The concentration yielding a half maximal decrease of the DOPA was determined in rat brain hemispheres; inactive at 45 umol/kg | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID48702 | Minimum effective dose administered intravenously for decrease in arterial pressure in cat heart | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine. |
| AID36782 | Binding affinity against Alpha-2 adrenergic receptor in rat brain membrane using [3H]yohimbine as radioligand | 1996 | Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16 | 1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3. |
| AID170913 | Brain Concentration at 15(umol/kg, sc) with tropolone pretreatment in rat striatum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID1459194 | Agonist activity at recombinant human 5HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation count | |||
| AID3796 | Binding affinity towards human 5-hydroxytryptamine 1A receptor was determined using [3H]8-OH-DPAT-as radioligand | 2001 | Bioorganic & medicinal chemistry letters, Mar-26, Volume: 11, Issue:6 | A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties. |
| AID4197 | Binding affinity against the site labelled by the 5-hydroxytryptamine 1A receptor agonist [3H]- 8-OH-DPAT | 1994 | Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25 | 1-(2,5-Dimethoxy-4-(trifluoromethyl)phenyl)-2-aminopropane: a potent serotonin 5-HT2A/2C agonist. |
| AID1193846 | Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT₁A and 5-HT₇ receptor ligands. |
| AID170916 | Brain Concentration at 15(umol/kg, sc) without tropolone pretreatment in rat striatum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID1675986 | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels after 15 mins by Alphalisa assay relative to serotonin | |||
| AID5273 | Binding affinity to 5-hydroxytryptamine 2 receptor in rat frontal cortical membranes by [3H]- KET displacement. | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Central serotonin receptors as targets for drug research. |
| AID132126 | In vivo effective dose administered subcutaneously in mouse hypothermia assay. | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID1830044 | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in HEK cells measured after 60 to 90 mins by radioligand completion assay relative to control | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID724007 | Displacement of [3H]prazosin from human recombinant alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition. |
| AID5065 | Binding affinity against 5-hydroxytryptamine 2 receptor in rat brain using [3H]ketanserin as radioligand | 1996 | Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16 | 1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3. |
| AID147730 | Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters. |
| AID177636 | Effect on 5-HTP accumulation in striatum of rat. | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID643006 | Displacement of [3H]prazosin from human recombinant alpha1B adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors. |
| AID277973 | Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID4372 | Compound was evaluated for its ability to displace the protonated form of [3H]8-hydroxy-2-(di-n-propylamino)tetralin binding from labeled 5-HT 1A receptor site. | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site. |
| AID773786 | Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | New serotonin 5-HT1A receptor agonists endowed with antinociceptive activity in vivo. |
| AID1675992 | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assa | |||
| AID36710 | Binding affinity towards rat Alpha-1 adrenergic receptor was evaluated using [3H]- prazosin as radioligand | 1996 | Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25 | Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4. |
| AID282109 | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in Wistar Han rat hippocampal membranes | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents. |
| AID3738 | Binding affinity to 5-hydroxytryptamine 1A receptor in rat hippocampus membranes,3H-8-OH-DPAT and buspirone for nonspecific binding (NSB) | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | 3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans]. |
| AID138488 | Behavioral time in mouse face to face assay at dose of 0 umol/kg administered | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID47980 | Inhibition of sympathetic nerve discharge (SND) in anesthetized cat | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID277979 | Induction of catalepsy in ip dosed rat after 60 min by crossed-leg position test | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID1517937 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, ip measured after 60 mins by thermometric method (Rvb = -0.2 to 0.5 deg C) | |||
| AID4691 | Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1 | Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes. |
| AID1193845 | Displacement of [3H]-5-HT from human 5-HT1A receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Synthesis and binding properties of new long-chain 4-substituted piperazine derivatives as 5-HT₁A and 5-HT₇ receptor ligands. |
| AID1830042 | Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Activity of |
| AID4399 | Binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand. | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor. |
| AID218797 | Binding affinity towards human cloned alpha-1A-adrenoceptor using [3H]prazosin as radioligand | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
| AID177869 | Inhibition of 5-Hydroxy tryptamine accumulation in hemispheres of rat brain after subcutaneous administration | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 8-Hydroxy-2-(di-n-propylamino)tetralin, a new centrally acting 5-hydroxytryptamine receptor agonist. |
| AID226638 | Hill coefficient value. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand. |
| AID181269 | Ratio of ED50 values when the compound was administered subcutaneously to that of peroral administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID6480 | Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID138660 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 30 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID174316 | Influence on 5-hydroxyindoleacetic acid (5-HIAA) concentration in hippocampus region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID204229 | Binding affinity against serotonin transporter (SERT) by displacement of [3H]paroxetine in male wistar rats | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters. |
| AID4017 | Binding affinity towards 5-hydroxytryptamine 1A receptor sites in cortical membranes using [3H]8-OH-DPAT as radioligand | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6 | (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist. |
| AID1702329 | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay | |||
| AID138820 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 9.1 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID176064 | Effect on the synthesis rates of dopamine in the rat ventral limbic brain region at 3.0 micro mol/kg | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID392049 | Cardiotoxicity in Dunkin-Hartley guinea pig assessed as maximal QTc prolongation time at 10 mg/kg, iv administered as 3 fold cumulative doses measured every 10 seconds at end of every 20 mins follow up period of individual dose by ECG | 2008 | European journal of medicinal chemistry, Nov, Volume: 43, Issue:11 | Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation. |
| AID298096 | Induction of flat body posture in orally dosed rat as after 60 mins | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID175936 | Effect on the synthesis rates of dopamine in the rat ventral limbic brain region at 0.3 micro mol/kg. | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID298093 | Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity. |
| AID510403 | Agonist activity at human cloned 5HT1A receptor expressed in human HeLa cells assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | 1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors. |
| AID288884 | Effect on compound induced hypothermia in Swiss Albino mouse at 5 mg/kg, sc in presence of 0.1 mg/kg WAY 100635 after 30 mins relative to control | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15 | 7-Arylpiperazinylalkyl and 7-tetrahydroisoquinolinylalkyl derivatives of 8-alkoxy-purine-2,6-dione and some of their purine-2,6,8-trione analogs as 5-HT(1A), 5-HT(2A), and 5-HT(7) serotonin receptor ligands. |
| AID1336982 | Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | New N- and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HT |
| AID177273 | ED50 value was measured as dose required to produce a half-maximal reduction of Serotonin (5-HTP) accumulation in limbic area of reserpinized rat brain | 1982 | Journal of medicinal chemistry, Aug, Volume: 25, Issue:8 | Monophenolic octahydrobenzo[f]quinolines: central dopamine- and serotonin-receptor stimulating activity. |
| AID35592 | Binding affinity to the adrenergic receptor alpha-1D of rat aorta | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor. |
| AID138654 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 3.0 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID24365 | Half-life time in rats | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID449043 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, sc after 15 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID35440 | Binding affinity towards Alpha-1 adrenergic receptor was determined in rat cortex membranes using [3H]prazosin as radioligand; No data | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety. |
| AID1152683 | Displacement of [3H]8-OH-DPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia. |
| AID65404 | Binding affinity for [3H]raclopride-labeled dopamine receptor D2 in rat striatum | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID1234837 | Agonist activity at human 5-HT1A receptor expressed in CHO cells after 90 mins by beta-arrestin-2 recruitment assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment of β-arrestin-2. |
| AID4096 | Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand. | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Central serotonin receptors as targets for drug research. |
| AID34466 | Inhibitory concentration of compound was tested as agonist activity against forskolin activated adenylate cyclase | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID180545 | The compound was tested in vivo for DOPA accumulation in limbic system against reserpine-pretreated rats;I= inactive at the highest dose tested | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID47964 | Effective dose at which the sympathetic nerve activity (SND) has been reduced to 50% of the pretreatment value in anesthetized cat | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID4006 | Displacement of [3H]8-OH-DPAT from rat striata 5-hydroxytryptamine 1A receptor | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarboxamides as selective 5-HT1A receptor agonists. |
| AID177319 | In vivo evaluation for 5-HTP accumulation in the hemispheres in male rats (sc) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID1459195 | Agonist activity at recombinant human 5HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding up to 10 uM preincubated for 20 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintil | |||
| AID13539 | Area under curve at 1 uM/dg administered intravenously | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID170782 | Brain Concentration of 7,8-di-OH-DPAT after 15(umol/kg) sc administration with tropolone pretreatment in rat striatum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID3891 | Maximum binding affinity was evaluated as ([35S]GTP binding on 5-hydroxytryptamine 1A serotonergic receptors. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID16499 | Cmax in minutes at a iv dose of 1.0(pmol/g/h). | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID124439 | Effect in the social interaction behavioral test in mice | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. |
| AID1675993 | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assa | |||
| AID1675999 | Bias factor, ratio of biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment to biased agonist activity at human 5-HT1A receptor stably expre | |||
| AID14276 | Maximum concentration of the drug at 20 umol/dg administered perorally | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID139267 | Maximum decrease in temperature when compound is administered through peroral route | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID4138 | The compound was tested in vitro for inhibitory activity against 5-HT1A receptor in rats, using [3H]8-OH-DPAT as radioligand | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. |
| AID138477 | Behavioral time in mouse face to face assay at 30 umol/kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID170910 | Brain Concentration of 7,8-di-OH-DPAT after 15(umol/kg) sc administration without tropolone pretreatment in rat striatum | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID18627 | Bioavailability in rat | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID170909 | Brain Concentration of 7,8-di-OH-DPAT after 15(umol/kg) sc administration without tropolone pretreatment in rat cortex | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID330660 | Effect on life span of Caenorhabditis elegans at 100 uM | 2007 | Nature, Nov-22, Volume: 450, Issue:7169 | An antidepressant that extends lifespan in adult Caenorhabditis elegans. |
| AID320636 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HEK293 cells after 120 mins | 2008 | Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5 | N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands. |
| AID138805 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 3.0 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID35897 | Binding affinity against alpha-2 adrenergic receptor in calf frontal cortex | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID1702356 | Antidepressant-like activity in Wistar rat assessed as reduction in immobility time at 0.63 mg/kg, sc administered 60 mins prior to testing and measured for 5 mins test period by Porsolt-forced swim test | |||
| AID566909 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, ip after 30 mins by inducible hypothermia test | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. part 3. |
| AID4064 | In vitro ability to displace [3H]8-hydroxy-2-(di-n-propylamino) tetralin binding from 5-hydroxytryptamine 1A receptor site. | 1992 | Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13 | Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site. |
| AID138806 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 3.0 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID4051 | Binding affinity at [3H]8-OH-DPAT-Labeled 5-hydroxytryptamine 1A receptor sites in rat brain hippocampal membranes | 1989 | Journal of medicinal chemistry, Jan, Volume: 32, Issue:1 | 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. |
| AID10374 | Half-lives were estimated from the elimination phase of the blood conc-time curve after oral administration | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID1675988 | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay relative to serotonin | |||
| AID566910 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, ip after 60 mins by inducible hypothermia test | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. part 3. |
| AID296884 | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17 | Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. |
| AID224257 | Maximum decrease in temperature when compound is administered through peroral route | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID37492 | The binding affinity was evaluated on cloned human alpha-1B adrenergic receptor expressed in chinese hamster ovary(CHO) cells by using [3H]prazosin as radioligand. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID49593 | Maximum decrease observed | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID20960 | tmax in hours at a iv dose of 1.0(pmol/g/h). | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID194003 | postsynaptic effects was assessed by the increase in the locomotor activity (reversal of reserpine induced hypokinesia) during a 30 min period after subcutaneous administration using photocell motility meters at the dose of 0.2 (mic roM/kg) | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
| AID65091 | Binding affinity of compound against Dopamine receptor D2 binding site using radioligand [3H]spiperone | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine. |
| AID643012 | Agonist activity at human recombinant 5HT1A receptor expressed in HeLa cells preincubated for 20 mins by [35S]GTPgammaS binding assay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors. |
| AID24920 | Half life of compound at 1 uM/dg administered intravenously | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID1227935 | Displacement of [3H]Way100635 from human recombinant 5-HT1A receptor expressed in CHO cell membranes by radioligand binding assay | 2015 | Journal of natural products, Apr-24, Volume: 78, Issue:4 | Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors. |
| AID388705 | Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2. |
| AID1285655 | Displacement of [3H]8-OHDPAT from human recombinant 5-HT1A receptor expressed in HEK293 cells | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
| AID188730 | Maximal reduction in percent (Partial response) of DOPA accumulation rat limbic system at highest test dose of 61 uM/Kg (po) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID4368 | Displacement of the radioligand [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID174313 | Influence on 5-hydroxy tryptamine (5-HT) concentration in septum region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID1517942 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, ip measured after 90 mins by thermometric method (Rvb = -0.3 to 0.3 deg C) | |||
| AID194000 | The compound was tested in vivo for locomotor activity in rats at 50 umol/kg after subcutaneous administration | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | 6-Hydroxy-3-n-propyl-2,3,4,5-tetrahydro-1H-3-benzazepine and analogs: new centrally acting 5-HT1A receptor agonists. |
| AID601165 | Binding affinity to 5HT1A receptor | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Novel benzo[b]thiophene derivatives as new potential antidepressants with rapid onset of action. |
| AID4370 | Binding affinity against 5-hydroxytryptamine 1A receptor from CHO-K1 cells, using [3H]8-OH-DPAT as the radioligand. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID192619 | post-synaptic agonistic effects by increase in locomotor activity at the dose of 0.2 umol/kg, sc in reserpinized rat (p<0.005) | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID277977 | Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTPgammaS binding relative to serotonin | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID219193 | Maximum decrease of arterial blood pressure at sympathetic nerve activity (SND) in anesthetized cat has been observed following 1 mg/kg dose | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID1702330 | Bias factor, ratio of biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels to biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A rece | |||
| AID388706 | Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding relative to 8-OH-DPAT | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2. |
| AID3802 | Binding affinity against human 5-hydroxytryptamine 1A receptor | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID5084 | Displacement of [3H]ketanserin from rat brain 5-hydroxytryptamine 2 receptor | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID176135 | Decrease in hippocampal level of 5-HTat preinjection of 0.1 mg/kg, sc | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | (S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. |
| AID178046 | Effective dose for half-maximal decrease in the accumulation of DOPA in reserpinized rat brain striatal area by po administration; Partial response at the highest dose tested | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID174317 | Influence on 5-hydroxyindoleacetic acid (5-HIAA) concentration in hypothalamus region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID138792 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 0.3 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID218801 | Binding affinity towards human cloned alpha-1D-adrenoceptor using [3H]prazosin as radioligand | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
| AID121124 | Effect on rectal temperature in mice at dose of 5 mg/kg sc. | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. |
| AID178043 | Effective dose for half-maximal decrease in the accumulation of DOPA in reserpinized rat brain hemispheral area by sc administration; Inactive | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID138813 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 30 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID232148 | Ratio of 5-HT concentration to 5-HIAA concentration in hypothalamus region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID3725 | Binding affinity towards rat 5-hydroxytryptamine 1A receptor was evaluated using [3H]8-OH-DPAT as radioligand | 1996 | Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25 | Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4. |
| AID138503 | Behavioral time in mouse isolation-induced aggression assay at 3.0 umol/kg administered intraperitoneally (*P<0.05) | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID464910 | Displacement of [3H]prazosin from human Alpha-1B adrenergic receptor expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of a new series of 5-HT1A receptor agonists. |
| AID1336354 | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
| AID1459190 | Displacement of [3H]prazosin from recombinant human alpha-1b adrenergic receptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method | |||
| AID1597290 | Displacement of [3H]OH-DPAT from human recombinant 5-HT1A receptor measured after 60 mins by scintillation counter method | |||
| AID4220 | Binding affinity against rat 5-hydroxytryptamine 1A receptor | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID176533 | DOPA accumulation in limbic system of reserpinized rats following subcutaneous administration at highest dose tested (50 umol/kg); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID175937 | Effect on the synthesis rates of dopamine in the rat ventral limbic brain region at 0.3 micro mol/kg. values are given as percent change from the control | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID4214 | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampus mambranes | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters. |
| AID138494 | Behavioral time in mouse isolation-induced aggression assay at 0 umol/kg administered intraperitoneally | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID219048 | Effective dose at which the sympathetic nerve activity (SND) has been reduced to 50% of the pretreatment value in anesthetized cat | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID408276 | Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists. |
| AID1442380 | Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in rat hippocampal membranes | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse. |
| AID3823 | Binding affinity to human 5-hydroxytryptamine 1A receptor was measured using [3H]-8-hydroxy-2-(di-n-propylamine) tetraline [3H]8-OH-DPAT) as radioligand | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor. |
| AID752218 | Binding affinity to human 5-HT1A receptor by radioligand displacement assay | 2013 | Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10 | Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
| AID76300 | The level of 5-HIAA (prefrontal cortex) measured by means of HPCL with electrochemical detection methods at 6.250 (umol/kg, sc) | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. |
| AID170912 | Brain Concentration at 15(umol/kg, sc) with tropolone pretreatment in rat cortex | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID184489 | Ability of compound to induce behavioral changes in rat | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 5-HT1A-receptor antagonism: N-alkyl derivatives of (R)-(-)-8,11-dimethoxynoraporphine. |
| AID224254 | Effective dose on hypothermia in mouse when administered subcutaneously (95% confidence levels) | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID4222 | Binding affinity against the 5-hydroxytryptamine 1A receptor labelled with [3H]8-OH-DPAT in rat hippocampal homogenates | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Synthesis and serotonin receptor affinities of a series of trans-2-(indol-3-yl)cyclopropylamine derivatives. |
| AID64146 | Binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID188720 | Maximal reduction in percent (Partial response) of DOPA accumulation rat corpus striatum at highest test dose of 61 uM/Kg (po) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID449153 | Antidepressant activity in Swiss albino mouse assessed as reduction of immobility time at 1 mg/kg, sc administered 30 mins before test measured 6 mins test session after 2 mins habituation period by forced swimming test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID178045 | Effective dose for half-maximal decrease in the accumulation of DOPA in reserpinized rat brain limbic area by sc administration; Inactive | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID174309 | Influence on 5-hydroxy tryptamine (5-HT) concentration in hippocampus region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID176530 | DOPA accumulation in hemispheres of reserpinized rats following subcutaneous administration at highest dose tested (50 umol/kg); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID5893 | Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane | 1998 | Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5 | Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives. |
| AID255313 | Percent inhibition against 5-hydroxytryptamine 1A receptor at 1 uM | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22 | 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. |
| AID277980 | Induction of lower lip retraction in ip dosed rat after 15 min | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID633920 | Displacement of [3H]-8-OH-DPAT from Sprague-Dawley rat brain cortex serotonin 5-HT1A receptor after 30 mins by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation. |
| AID1601995 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, sc measured after 60 mins by thermometric method (Rvb = 0.1 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID178039 | Effective dose for half-maximal decrease in the accumulation of 5-hydroxytryptophan (5-HTP) in reserpinized rat brain limbic area by sc administration | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID302138 | Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat cortex membrane | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | 1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems. |
| AID174321 | Influence on 5-hydroxyindoleacetic acid (5-HIAA)concentration in amygdala region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID4699 | Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand. | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Central serotonin receptors as targets for drug research. |
| AID49589 | Maximum decrease in sympathetic nerve discharge in anesthetized cat | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID1517947 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, ip measured after 120 mins by thermometric method (Rvb = -0.1 to 0.3 deg C) | |||
| AID4701 | Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptor | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID64951 | Binding affinity against D2 receptor in homogenated rat brain tissue, using by ([3H]N00437) as radioligand; Not tested | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID177906 | Inhibition of firing rates of serotonergic neurons in the dorsal raphe nucleus by intravenous injection in rats | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID36711 | Binding affinity against Alpha-1 adrenergic receptor in rat brain membrane using [3H]prazosin as radioligand | 1996 | Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16 | 1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3. |
| AID61533 | Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand | 1996 | Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16 | 1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3. |
| AID5478 | Binding affinity towards rat 5-hydroxytryptamine 2A receptor was evaluated using [3H]- ketanserin as radioligand | 1996 | Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25 | Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4. |
| AID121119 | Effect on rectal temperature in mice at dose of 2.5 mg/kg sc. | 1996 | Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22 | Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist. |
| AID3939 | The binding affinity was evaluated on cloned human 5-hydroxytryptamine 1A receptor expressed in HeLa cells by using DPAT as radioligand. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID3712 | Evaluated for the 5-hydroxytryptamine 1A receptor agonist activity in LY-293284 trained rats | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
| AID15428 | Free level in rat plasma | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID193346 | Effect on the synthesis rate of 5 HTP accumulation at the dose 0.3 umol/kg in the rat ventral limbic brain region | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID277981 | Induction of flat body posture in ip dosed rat after 15 min | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID1337885 | Agonist activity at recombinant human 5-HT1A receptor expressed in HeLa cell membranes assessed as induction of [35S]GTPgammaS binding preincubated for 20 mins followed by [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting met | |||
| AID1675990 | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay relative to serotonin | |||
| AID177336 | In vivo evaluation for DOPA accumulation in the limbic system in male rats at highest test dose of 45 uM/Kg; inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID5109 | Binding affinity towards 5-hydroxytryptamine 2 receptor using [3H]- ketanserin as radioligand | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID55587 | Inhibition of firing rates of serotonergic neurons in the dorsal raphe nucleus by intravenous injection in rats. | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID224255 | Effective dose on hypothermia in mouse when administered through peroral route (95% confidence levels) | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID139265 | Maximum decrease in temperature when compound is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID449460 | Agonist activity at 5HT1A receptor in Swiss albino mouse assessed as decrease in rectal temperature at 5 mg/kg, ip after 30 mins in the presence of WAY 100635 administered 15 mins before drug challenge | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives. |
| AID5476 | Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]-ketanserin from rat prefrontal cerebral cortex mambranes | 2003 | Journal of medicinal chemistry, Dec-04, Volume: 46, Issue:25 | Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters. |
| AID177645 | Effect on dopamine accumulation in limbic system of rat; Inactive | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID50207 | Percent arterial blood pressure at sympathetic nerve discharge in anesthetized cat | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID138646 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 0.3 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID1702244 | Displacement of [3H]-prazosin from alpha1 adrenergic receptor in rat cortex measured after 30 mins by microbeta2 scintillation counting method | |||
| AID178038 | Effective dose for half-maximal decrease in the accumulation of 5-hydroxytryptophan (5-HTP) in reserpinized rat brain limbic area by po administration | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID87466 | Compound was evaluated for inhibition of forskolin-stimulated adenylyl cyclase in dose dependent manner in HeLa cells transfected with 5-HTIA | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | Serotonergic ergoline derivatives. |
| AID177332 | In vivo evaluation for DOPA accumulation in the hemispheres in male rats at highest test dose of 45 uM/Kg; inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID178036 | Effective dose for half-maximal decrease in the accumulation of 5-hydroxytryptophan (5-HTP) in reserpinized rat brain hemispheral area by po administration | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID465069 | Agonist activity at human recombinant 5HT1A receptor expressed in human HeLa cells by [35S]GTPgammaS binding assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of a new series of 5-HT1A receptor agonists. |
| AID24768 | Time taken to reach the maximum concentration of compound at 20 uM/dg administered perorally | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID174308 | Influence on 5-hydroxy tryptamine (5-HT) concentration in frontal cortex region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID64147 | Binding affinity against [3H]U-86,170-labeled dopamine receptor D2 in cloned CHO cells | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID1720742 | Binding affinity to 5-HT1A (unknown origin) | |||
| AID170915 | Brain Concentration at 15(umol/kg, sc) without tropolone pretreatment in rat cortex | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID193484 | Effect on the synthesis rate of dopamine (DOPA) accumulation at the dose of 0.3 umol/kg in the rat ventral limbic brain region | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID5336 | The binding affinity was evaluated on 5-hydroxytryptamine 2A receptor expressed in rat cortex by using [3H]ketanserin as radioligand. | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID1602007 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, sc measured after 120 mins by thermometric method (Rvb = -0.1 to 0.1 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID1702242 | Displacement of [3H]-methylspiperone from recombinant human D2 receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method | |||
| AID277976 | Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities. |
| AID79056 | Tested for inhibition of field-stimulation-induced contraction in the isolated guinea pig ileum | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Preparation and pharmacological evaluation of enantiomers of certain nonoxygenated aporphines: (+)- and (-)-aporphine and (+)- and (-)-10-methylaporphine. |
| AID1702322 | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay relative to serotonin | |||
| AID177317 | In vivo evaluation for 5-HTP accumulation in the corpus striatum in male rats.(sc) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID724005 | Displacement of [3H]prazosin from human recombinant alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition. |
| AID190571 | 8-OH-DPAT appropriate response of animals/min rate in %0.2 mg/Kg where stimulus generalization occurred(7/7 no of animals) | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID1675987 | Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay | |||
| AID611932 | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor | 2011 | Journal of medicinal chemistry, Aug-11, Volume: 54, Issue:15 | Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. |
| AID138791 | Time of effect in the isolation-induced aggression behavioral assay in the mouse when a dose of 0.3 micro mol/kg is administered intraperitoneally | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID138491 | Behavioral time in mouse isolation-induced aggression assay 0.3 umol/kg administered intraperitoneally | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID65714 | Displacement of [3H]U-86170 from Dopamine receptor D2 | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
| AID132124 | Tested in vivo for the effective dose administered orally in mouse hypothermia assay | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID449042 | Effect on hypothermia in Swiss albino mouse assessed as change in rectal body temperature at 5 mg/kg, sc after 45 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID138478 | Behavioral time in mouse face to face assay at 30 umol/kg administered subcutaneously (*P<0.05) | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID643013 | Agonist activity at human recombinant 5HT1A receptor expressed in HeLa cells preincubated for 20 mins by [35S]GTPgammaS binding assay relative to 8-OH-DPAT | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors. |
| AID63044 | Binding affinity towards dopamine receptor D1 in calf striatum | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID449035 | Reduction of 8-OH-DPAT-induced hypothermia in Swiss albino mouse at 0.1 mg/kg, sc administered 15 mins prior 8-OH-DPAT challenge measured after 45 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID138467 | Behavioral time in mouse face to face assay at 3.0 umol/kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID330659 | Effect on life span of Caenorhabditis elegans at 50 uM | 2007 | Nature, Nov-22, Volume: 450, Issue:7169 | An antidepressant that extends lifespan in adult Caenorhabditis elegans. |
| AID193350 | Effect on the synthesis rate of 5 HTP accumulation at the dose of 3.0 umol/kg in the rat ventral limbic brain region (*P<0.05) | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID1702323 | Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay | |||
| AID4210 | Affinity for 5-hydroxytryptamine 1A receptor site | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | (R)- and (S)-5,6,7,8-tetrahydro-1-hydroxy-N,N-dipropyl-9H-benzocyclohepten- 8-ylamine. Stereoselective interactions with 5-HT1A receptors in the brain. |
| AID449034 | Reduction of 8-OH-DPAT-induced hypothermia in Swiss albino mouse at 0.1 mg/kg, sc administered 15 mins prior 8-OH-DPAT challenge measured after 60 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID124447 | Swimming activity of the treated mice/control mice at 41 umol/kg, sc (p < 0.001) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID184829 | in vivo behavioral test for Lower Lip Retraction(LLR) (msad=minimum significant active dose) in rats | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID723786 | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cell membranes after 30 mins | 2013 | Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition. |
| AID230751 | Ratio of the binding affinities against 5-HT1A and alpha-1-adrenoceptor from rat brain membranes. | 1999 | Journal of medicinal chemistry, Jan-14, Volume: 42, Issue:1 | Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton. |
| AID62169 | Compound was evaluated for the binding affinity towards Dopamine receptor D2 using [3H]raclopride radioligand. | 1996 | Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21 | 3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans]. |
| AID187187 | Inhibitory activity against (125I)-(R,S)-trans-8-OH-PIPAT binding to the rat hippocampal homogenate | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. |
| AID138659 | Time of effect in the face-to-face behavioral assay in the mouse when a dose of 30 micro mol/kg is administered subcutaneously | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID177125 | ED50 value was measured as dose required to produce a half-maximal reduction of Dopa accumulation in limbic area of reserpinized rat brain; I is Inactive, no significant effect at doses approximately 40 times the ED50 for Dopa accumulation | 1982 | Journal of medicinal chemistry, Aug, Volume: 25, Issue:8 | Monophenolic octahydrobenzo[f]quinolines: central dopamine- and serotonin-receptor stimulating activity. |
| AID346017 | Displacement of [3H]8-OH-DPAT from human cloned 5-HT1A receptor expressed in human HeLa cells | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23 | 2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties. |
| AID3475 | Compound was evaluated for the binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor in bovine hippocampus | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID20966 | tmax in hours at a po dose of 20.0(pmol/g/h). | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID176094 | Effect on the synthesis rates of serotonin in the rat ventral limbic brain region at 3.0 micro mol/kg. values are given as percent change from the control | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID635976 | Neuroprotective activity in Wistar rat hippocampi primary neuronal cells assessed as protection against oxygen-glucose deprivation induced cell death at 1 uM after 18 hrs by MTT assay | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage. |
| AID643005 | Displacement of [3H]prazosin from human recombinant alpha1A adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors. |
| AID1627080 | Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Design and synthesis of new homo and hetero bis-piperazinyl-1-propanone derivatives as 5-HT7R selective ligands over 5-HT1AR. |
| AID180715 | The concentration yielding a half maximal decrease of the 5-HTP was determined in rat brain hemispheres | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID65725 | Displacement of [3H]spiperone from dopamine receptor D2 | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID3989 | Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding in rat hippocampal membranes | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID772376 | Agonist activity at human 5HT1A receptor | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID177325 | In vivo evaluation for DOPA accumulation in the corpus striatum in male rats at highest test dose of 45 uM/Kg; inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID189826 | In vivo motor activity at 10 umol/kg (po) in male rats expressed as accumulated counts/30 min (p < 0.001) | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID3800 | Binding affinity against [3H]- -8-OH-DPAT -labeled 5-hydroxytryptamine 1A sites in cloned CHO cells | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID3564 | Maximal stimulation was expressed as percentage of the maximal 5-HT response in the [35S]GTP-gamma-S, binding assay on 5-hydroxytryptamine 1A receptor | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID35459 | Displacement of [3H]prazosin from human cloned Alpha-1D adrenergic receptor | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID36745 | Displacement of [3H]prazosin from human cloned Alpha-1A adrenergic receptor | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID180888 | The concentration yielding a half maximal decrease of the DOPA was determined in rat limbic system; inactive at 45 umol/kg | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID449036 | Reduction of 8-OH-DPAT-induced hypothermia in Swiss albino mouse at 0.1 mg/kg, sc administered 15 mins prior 8-OH-DPAT challenge measured after 30 mins by inducible hypothermia test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity: part 2. |
| AID3817 | Binding affinity on human cloned 5-hydroxytryptamine 1A receptor transfected in human cell lines(He La) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID180539 | The compound was tested in vivo for DOPA accumulation in hemispheres (cortex) against reserpine-pretreated rats;I= inactive at the highest dose tested | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID1675991 | Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay | |||
| AID19560 | Hill coefficient of the compound | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. |
| AID174307 | Influence on 5-hydroxy tryptamine (5-HT) concentration in caudate region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID24764 | Time taken to reach the maximum concentration of compound at 1 uM/dg administered intravenously | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID3988 | Antagonist activity to stimulate binding of [35S]GTP-gamma-S, to 5-hydroxytryptamine 1A receptor in isolated rat hippocampal membranes | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID635979 | Neuroprotective activity in Wistar rat hippocampi primary neuronal cells assessed as protection against glutamate-induced cell death at 1 uM treated 30 min before glutamate challenge measured after 22 hrs by MTT assay | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage. |
| AID178178 | Effective dose for half-maximal decrease in the accumulation of DOPA in reserpinized rat brain striatal area by sc administration; Inactive | 1993 | Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22 | Orally active central dopamine and serotonin receptor ligands: 5-, 6-, 7-, and 8-[[trifluoromethyl)sulfonyl]oxy]-2-(di-n-propylamino)tetralins and the formation of active metabolites in vivo. |
| AID177634 | Effect on 5-HTP accumulation in limbic system of rat. | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Occurrence and pharmacological significance of metabolic ortho-hydroxylation of 5- and 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID1854986 | Binding affinity to 5-HT1A receptor (unknown origin) assessed as inhibition constant | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16 | Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors. |
| AID138638 | Behavioral time in mouse isolation-induced aggression behavioral assay at 9.1 umol/kg administered intraperitoneally (*P<0.05) | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID751941 | Displacement of [3H]8-OH-DPAT from 5-HT1A receptor in Wistar rat cerebral hippocampus membrane after 10 mins | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
| AID181254 | in vivo effects on DA (dopamine) synthesis in cortex was reported after subcutaneous administration to reserpinized rats | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | C-9 and N-substituted analogs of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro-3- propyl-1H-benz[e]indole-9-carboxamide: 5-HT1A receptor agonists with various degrees of metabolic stability. |
| AID1713175 | Displacement of [3H]-8-OH-DPAT from rat cerebral cortex 5HT1A receptor measured after 15 mins by liquid scintillation counter method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile. |
| AID3707 | Agonistic activity (induction of forepaw treading in rats)on postsynaptic 5-hydroxytryptamine 1A receptor while iv administration | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID3950 | Antagonist activity at 5-hydroxytryptamine 1A receptor against (+)-8-OH-DPAT induced hypothermia in mice 15 min after administration of the compound | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19 | Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT(1A) receptors. |
| AID6499 | Binding affinity for rodent 5-hydroxytryptamine 5A receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID176088 | Effect on the synthesis rates of serotonin in the rat ventral limbic brain region 3.0 micro mol/kg. | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives. |
| AID643008 | Displacement of [3H]-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cells after 30 mins by liquid scintillation counting | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors. |
| AID3734 | Binding affinity against 5-hydroxytryptamine 1A (5-HT1A) receptor in rat hippocampus membranes | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID247122 | Agonist activity in forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor compared to 8-OH-DPAT | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan. |
| AID4419 | Binding affinity for rat cortex 5-hydroxytryptamine 1A receptor, by displacement of 0.2 nM [3H]8-OH-DPAT radioligand | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Design and synthesis of a series of 6-substituted-2-pyridinylmethylamine derivatives as novel, high-affinity, selective agonists at 5-HT1A receptors. |
| AID465063 | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor expressed in human HeLa cells | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6 | Discovery of a new series of 5-HT1A receptor agonists. |
| AID3909 | ability to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists. |
| AID635973 | Neuroprotective activity in Wistar rat hippocampi primary neuronal cells assessed as protection against serum-deprivation induced cell death at 1 uM after 24 hrs by MTT assay | 2011 | Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23 | New serotonin 5-HT(1A) receptor agonists with neuroprotective effect against ischemic cell damage. |
| AID204623 | Binding affinity against sigma receptor | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands. |
| AID4019 | Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat cortex membranes | 2003 | Journal of medicinal chemistry, Jul-31, Volume: 46, Issue:16 | Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety. |
| AID232145 | Ratio of 5-HT concentration to 5-HIAA concentration in caudate region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID180895 | The dose at which the animals would show 50% response on 8-OH-DPAT appropriate lever at a dose 0.2 mg/kg (7/7 no of animals) | 1988 | Journal of medicinal chemistry, Apr, Volume: 31, Issue:4 | N,N-di-n-propylserotonin: binding at serotonin binding sites and a comparison with 8-hydroxy-2-(di-n-propylamino)tetralin. |
| AID1702332 | Bias factor, ratio of biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation to biased agonist activity at Gal4-VP16 transcription factor linked human 5-H | |||
| AID35431 | The compound was tested for binding affinity on [3H]- prazosin as specific ligand on alpha-1 adrenergic receptor cells in rat cerebral cortex | 1999 | Journal of medicinal chemistry, Jan-14, Volume: 42, Issue:1 | Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton. |
| AID180747 | The concentration yielding a half maximal decrease of the DOPA was determined in rat brain striatum; inactive at 45 umol/kg | 1994 | Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20 | 6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists. |
| AID3900 | Potency (pD2) for the stimulation of [35S]GTP-gamma-S, binding on 5-hydroxytryptamine 1A receptor | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines. |
| AID442987 | Displacement of [3H]8OH-DPAT from 5HT1A in Sprague-Dawley rat brain cortex by liquid scintillation counting | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands. |
| AID683001 | Agonist activity at human 5HT1A receptor expressed in HeLa cells assessed as [35S]GTPgammaS binding incubated for 20 mins prior to [35S]GTPgammaS addition measured after 30 mins by liquid scintillation counting | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7 | Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect. |
| AID1602001 | Induction of hypothermia in CD-1 mouse assessed as change in body temperature at 5 mg/kg, sc measured after 90 mins by thermometric method (Rvb = -0.1 to 0.1 deg C) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT |
| AID5076 | Binding affinity towards 5-hydroxytryptamine 2 receptor in rat frontal cortex using [3H]ketanserin as radioligand | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor. |
| AID4500 | The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line | 1998 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11 | Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. |
| AID5006 | Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex | 1994 | Journal of medicinal chemistry, Jun-10, Volume: 37, Issue:12 | 3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies. |
| AID176528 | DOPA accumulation in corpus striatum of reserpinized rats following subcutaneous administration at highest dose tested (50 umol/kg); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID181099 | compound was tested in vivo for 5-HTP accumulation in hemispheres (cortex) against reserpine-pretreated rats. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationships in the 8-amino-6,7,8,9-tetrahydro-3H-benz[e]indole ring system. 1. Effects of substituents in the aromatic system on serotonin and dopamine receptor subtypes. |
| AID196143 | Oral availability obtained from blood plasma levels of the parent compound following 1 uMol /kg intravenous and 20 umol /kg peroral administration | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID177871 | Inhibition of 5-Hydroxy tryptamine accumulation in limbic part of rat brain after subcutaneous administration | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 8-Hydroxy-2-(di-n-propylamino)tetralin, a new centrally acting 5-hydroxytryptamine receptor agonist. |
| AID1627081 | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Design and synthesis of new homo and hetero bis-piperazinyl-1-propanone derivatives as 5-HT7R selective ligands over 5-HT1AR. |
| AID64291 | In vitro binding activity against Dopamine receptor D2 from homogenized rat brain, using [3H]spiperone as the radioligand | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties. |
| AID177676 | Effective concentration required to determined hallucinogen-like activity in LSD-trained rats | 2001 | Bioorganic & medicinal chemistry letters, Mar-26, Volume: 11, Issue:6 | A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties. |
| AID176527 | DOPA accumulation in corpus striatum of reserpinized rats following peroral administration at highest dose tested (50 umol/kg); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID63821 | The binding affinity was evaluated on Dopamine receptor D2 expressed in rat striatum by using [3H]spiperone as radioligand | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15 | Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes. |
| AID772375 | Binding affinity at human 5HT1A receptor | 2013 | ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9 | Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity. |
| AID4327 | Displacement of [3H]5-HT from rat hippocampal 5-hydroxytryptamine 1A receptor with 10e-6 M ketanserin | 1996 | Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1 | New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives. |
| AID174319 | Influence on 5-hydroxyindoleacetic acid (5-HIAA) concentration in parietal cortex region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID3917 | Displacement of [3H]8-hydroxy-2-(di-n-propylamino)tetralin from human 5-hydroxytryptamine 1A receptor | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20 | WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors. |
| AID76291 | Effect of 6.250 (umol/kg, sc) compound on guinea pig rectal temperature (Hypothermia) | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates. |
| AID3822 | Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand | 1998 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11 | Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes. |
| AID176531 | DOPA accumulation in limbic system of reserpinized rats following peroral administration at highest dose tested (50 umol/kg); Inactive | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | Synthesis and biological activity of cis-(3aR)-(-)-2,3,3a,4,5,9b-hexahydro- 3-propyl-1H-benz[e]indole-9-carboxamide: a potent and selective 5-HT1A receptor agonist with good oral availability. |
| AID6648 | Binding affinity towards rat 5-hydroxytryptamine 7 receptor | 2003 | Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). |
| AID4073 | In vitro ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor sites of rat brain cortex. | 1995 | Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8 | New (2-methoxyphenyl)piperazine derivatives as 5-HT1A receptor ligands with reduced alpha 1-adrenergic activity. Synthesis and structure-affinity relationships. |
| AID193489 | Effect on the synthesis rate of dopamine (DOPA) accumulation at the dose of 3.0 umol/kg in the rat ventral limbic brain region | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID37060 | Binding affinity constant against alpha-1B adrenergic receptor of guinea pig spleen | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha 1d adrenergic receptor. |
| AID177902 | Inhibition of firing rates of dopaminergic neurons in the substantia nigra pars compacta by intravenous injection in rats | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8 | 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. |
| AID1593198 | Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in human HeLa cells incubated for 30 mins by radioligand competition binding assay | |||
| AID388704 | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in CHO cells | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2. |
| AID47960 | Dose at which the SND has been reduced to 50% of the pretreatment value | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | 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. |
| AID3747 | Concentration necessary to achieve half maximal inhibition of [3H]8-Hydroxy-2-(di-n-propylamino)tetralin binding to 5-hydroxytryptamine 1A receptor at 1 uM | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3 | 2H-[1]benzopyrano[3,4-b]pyridines: synthesis and activity at central monoamine receptors. |
| AID174311 | Influence on 5-hydroxy tryptamine (5-HT) concentration in olfactory tubercle region of brain | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (R)-(-)-10-methyl-11-hydroxyaporphine: a highly selective serotonergic agonist. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 359, Issue:6 | Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3 | Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. |
| AID1346528 | Human 5-HT1D receptor (5-Hydroxytryptamine receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 359, Issue:6 | Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 2004 | Bioscience reports, Apr, Volume: 24, Issue:2 | Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 357, Issue:3 | Labelling of recombinant human and native rat serotonin 5-HT1A receptors by a novel, selective radioligand, [3H]-S 15535: definition of its binding profile using agonists, antagonists and inverse agonists. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 2004 | Bioscience reports, Apr, Volume: 24, Issue:2 | Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. |
| AID1346264 | Human 5-HT1B receptor (5-Hydroxytryptamine receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 359, Issue:6 | Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 359, Issue:6 | Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID624212 | Agonists at Human 5-Hydroxytryptamine receptor 5-ht5a | 1994 | FEBS letters, Dec-05, Volume: 355, Issue:3 | Cloning and characterisation of the human 5-HT5A serotonin receptor. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 284, Issue:3 | Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 284, Issue:3 | Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1992 | The Biochemical journal, Aug-01, Volume: 285 ( Pt 3) | High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells. |
| AID624230 | Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2 | Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. |
| AID1346739 | Human 5-HT1F receptor (5-Hydroxytryptamine receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2 | Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1997 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 280, Issue:3 | Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats. |
| AID1346528 | Human 5-HT1D receptor (5-Hydroxytryptamine receptors) | 1999 | European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3 | Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 2000 | Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2 | Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic tr |
| AID1345061 | Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors) | 2001 | European journal of pharmacology, Apr-27, Volume: 418, Issue:3 | Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 2000 | Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2 | Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic tr |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 1998 | European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3 | Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. |
| AID624212 | Agonists at Human 5-Hydroxytryptamine receptor 5-ht5a | 2001 | European journal of pharmacology, Apr-27, Volume: 418, Issue:3 | Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 2001 | Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 363, Issue:6 | The cloned human 5-HT7 receptor splice variants: a comparative characterization of their pharmacology, function and distribution. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1998 | European journal of pharmacology, Aug-21, Volume: 355, Issue:2-3 | Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. |
| AID1345068 | Human 5-HT5A receptor (5-Hydroxytryptamine receptors) | 1994 | FEBS letters, Dec-05, Volume: 355, Issue:3 | Cloning and characterisation of the human 5-HT5A serotonin receptor. |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | The Journal of biological chemistry, Nov-05, Volume: 268, Issue:31 | Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. |
| AID1346903 | Rat 5-HT2B receptor (5-Hydroxytryptamine receptors) | 1993 | Molecular pharmacology, Mar, Volume: 43, Issue:3 | Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. |
| AID624233 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2 | Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. |
| AID624219 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT2B | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID624210 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A | 2003 | Biochemical pharmacology, Feb-01, Volume: 65, Issue:3 | Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. |
| AID624216 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 2003 | Biochemical pharmacology, Feb-01, Volume: 65, Issue:3 | Affinity of cyamemazine, an anxiolytic antipsychotic drug, for human recombinant dopamine vs. serotonin receptor subtypes. |
| AID1346603 | Human 5-ht1e receptor (5-Hydroxytryptamine receptors) | 2004 | European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3 | Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor. |
| AID1259419 | Human 5-HT2A receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345215 | Mouse 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | Molecular pharmacology, Aug, Volume: 44, Issue:2 | Molecular cloning of a mammalian serotonin receptor that activates adenylate cyclase. |
| AID624240 | Agonists at Rat 5-Hydroxytryptamine receptor 5-HT2B | 1993 | Molecular pharmacology, Mar, Volume: 43, Issue:3 | Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor. |
| AID1346528 | Human 5-HT1D receptor (5-Hydroxytryptamine receptors) | 1996 | Molecular pharmacology, Dec, Volume: 50, Issue:6 | Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamin |
| AID624235 | Agonists at Human 5-Hydroxytryptamine receptor 5-HT2A | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Sep-15, Volume: 90, Issue:18 | Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1997 | British journal of pharmacology, Sep, Volume: 122, Issue:1 | Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b). |
| AID1345061 | Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors) | 1993 | Molecular pharmacology, Mar, Volume: 43, Issue:3 | Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization. |
| AID1346867 | Human 5-HT2B receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1997 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 280, Issue:3 | Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats. |
| AID1345291 | Human 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1998 | British journal of pharmacology, Jul, Volume: 124, Issue:6 | Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. |
| AID624230 | Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e | 2004 | European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3 | Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor. |
| AID1346264 | Human 5-HT1B receptor (5-Hydroxytryptamine receptors) | 1997 | Naunyn-Schmiedeberg's archives of pharmacology, Sep, Volume: 356, Issue:3 | Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. |
| AID1345068 | Human 5-HT5A receptor (5-Hydroxytryptamine receptors) | 2001 | European journal of pharmacology, Apr-27, Volume: 418, Issue:3 | Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution. |
| AID1345615 | Human 5-HT1A receptor (5-Hydroxytryptamine receptors) | 1992 | The Biochemical journal, Aug-01, Volume: 285 ( Pt 3) | High-level stable expression of recombinant 5-HT1A 5-hydroxytryptamine receptors in Chinese hamster ovary cells. |
| AID1346603 | Human 5-ht1e receptor (5-Hydroxytryptamine receptors) | 1993 | Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2 | Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. |
| AID1346528 | Human 5-HT1D receptor (5-Hydroxytryptamine receptors) | 1997 | Naunyn-Schmiedeberg's archives of pharmacology, Sep, Volume: 356, Issue:3 | Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. |
| AID1346893 | Human 5-HT2C receptor (5-Hydroxytryptamine receptors) | 2004 | Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2 | Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors. |
| AID1345235 | Rat 5-HT7 receptor (5-Hydroxytryptamine receptors) | 1993 | The Journal of biological chemistry, Aug-25, Volume: 268, Issue:24 | Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype. |
| AID1798075 | Radioligand Labeled Binding Assay from Article 10.1021/jm070487n: \\Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.\\ | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17 | Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. |
| AID493017 | Wombat Data for BeliefDocking | 1993 | Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15 | (S)- and (R)-8-(di-n-propylamino)-6,7,8,9-tetrahydro-3H-benz[e]indole-1- carbaldehyde: a new class of orally active 5-HT1A-receptor agonists. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 374 (11.00) | 18.7374 |
| 1990's | 1572 (46.25) | 18.2507 |
| 2000's | 994 (29.24) | 29.6817 |
| 2010's | 411 (12.09) | 24.3611 |
| 2020's | 48 (1.41) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (6.67) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 7 (0.20%) | 5.53% |
| Reviews | 37 (1.05%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 3,486 (98.75%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||