Page last updated: 2024-12-06
preclamol
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
Preclamol is a drug that was investigated as a potential treatment for hypertension. It acts as a calcium channel blocker, which means it prevents calcium from entering the cells of the heart and blood vessels. This effect helps to relax the blood vessels and lower blood pressure. However, Preclamol was ultimately not approved for clinical use due to concerns about its safety and efficacy. The exact reasons for its discontinued development are not widely known, likely due to its early stage of research and potential safety issues, which are common in drug development.'
preclamol: centrally acting dopamine receptor agonist with selectivity for autoreceptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 55445 |
| CHEMBL ID | 276500 |
| CHEBI ID | 125440 |
| SCHEMBL ID | 872804 |
| MeSH ID | M0087067 |
| PubMed CID | 5311189 |
| CHEMBL ID | 7549 |
| SCHEMBL ID | 1240854 |
| MeSH ID | M0087067 |
| PubMed CID | 202478 |
| CHEMBL ID | 7393 |
| SCHEMBL ID | 8354256 |
| MeSH ID | M0087067 |
Synonyms (101)
| Synonym |
|---|
| 3-(3-hydroxyphenyl)-n-n-propylpiperidine |
| phenol, 3-(1-propyl-3-piperidinyl)- |
| (+)-3-(3-hydroxyphenyl)-n-(1-propyl)piperidine |
| n-n-propyl-3-(3-hydroxyphenyl)piperidine |
| 3-ppp |
| 3-(1-propyl-3-piperidinyl)phenol |
| OPREA1_004907 |
| PDSP2_000175 |
| PDSP1_000176 |
| NCGC00162310-01 |
| CHEBI:125440 |
| L000832 |
| CHEMBL276500 , |
| AKOS005065963 |
| 3-(1-propylpiperidin-3-yl)phenol |
| ppp, r(+)-3 |
| 3ppp(+/-) |
| (r)-3-(1-propyl-piperidin-3-yl)-phenol |
| ppp, s(-)-3 |
| nsc_202477 |
| bdbm81924 |
| 75240-91-4 |
| nd3ndm2ehm , |
| unii-nd3ndm2ehm |
| BRD-A76934284-001-01-1 |
| SCHEMBL872804 |
| Q27216056 |
| FT-0770905 |
| DTXSID10861083 |
| (+/-)-preclamol |
| preclamol, (+/-)- |
| (+/-)-3-ppp |
| 3-ppp-(-) |
| PDSP1_000630 |
| LOPAC0_000996 |
| preclamol |
| PDSP2_000626 |
| preclamol [inn] |
| (-)-(s)-m-(1-propyl-3-piperidyl)phenol |
| preclamolum [latin] |
| NCGC00162308-01 |
| NCGC00162310-02 |
| CHEMBL7549 , |
| (-)-3ppp |
| (s)-3-(1-propylpiperidin-3-yl)phenol |
| bdbm50010617 |
| (-)-3-(1-propyl-piperidin-3-yl)-phenol |
| 3ppp,(+) |
| 3-((s)-1-propyl-piperidin-3-yl)-phenol |
| unii-9v2o6crq6z |
| preclamolum |
| 9v2o6crq6z , |
| 85966-89-8 |
| CCG-205076 |
| DTXSID7048453 |
| SCHEMBL1240854 |
| (s)-(-)-3-(3-hydroxyphenyl)-n-propylpiperidine |
| SDCCGSBI-0050969.P002 |
| NCGC00162310-03 |
| Q27273260 |
| r-3-(3-hydroxyphenyl)-n-propylpiperidine hydrochloride |
| r-3-ppp hydrochloride |
| lopac-p-103 |
| lopac-p-102 |
| NCGC00015776-02 |
| NCGC00015776-01 |
| PDSP2_000624 |
| LOPAC0_000986 |
| PDSP1_000628 |
| NCGC00162308-02 |
| CHEMBL7393 , |
| 3-[(3r)-1-propylpiperidin-3-yl]phenol |
| (+)-3-(1-propyl-piperidin-3-yl)-phenol |
| 3-((r)-1-propyl-piperidin-3-yl)-phenol |
| bdbm50010618 |
| cid_202478 |
| 3ppp,(-) |
| 3-(1-propyl-piperidin-3-yl)-phenol |
| preclamol, (r)- |
| 85976-54-1 |
| unii-8l7h229k4i |
| 8l7h229k4i , |
| r-3-(3-hydroxyphenyl)-n-propylpiperidine hcl |
| CCG-205066 |
| SR-01000075393-11 |
| (r)-preclamol |
| (r)-(+)-3-ppp |
| phenol, 3-((3r)-1-propyl-3-piperidinyl)- |
| (+)-3-ppp |
| (r)-(+)-3-(3-hydroxyphenyl)-n-propylpiperidine |
| SCHEMBL8354256 |
| (r)-3-(3-hydroxyphenyl)-n-propylpiperidine |
| (r)-3-(1-propylpiperidin-3-yl)phenol |
| DTXSID101017364 |
| (+)-preclamol |
| SDCCGSBI-0050959.P002 |
| NCGC00162308-04 |
| Q27270713 |
| MS-23215 |
| HY-145454 |
| CS-0374747 |
Research Excerpts
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| "3 microM and 9 microM, respectively, against the toxic action of 100 microM glutamate." | ( Excitatory amino acid neurotoxicity at the N-methyl-D-aspartate receptor in cultured neurons: protection by SKF 10,047. Feuerstein, G; Lysko, PG, 1990) | 0.28 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| "Irreversible inactivation of striatal D2 dopamine (DA) autoreceptors with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) or inactivation of striatal guanine nucleotide binding proteins (G proteins) with pertussis toxin (PT) shifted the dose-response curve for N-n-propylnorapomorphine (NPA)-mediated inhibition of gamma-butyrolactone (GBL)-induced elevation of L-3,4-dihydroxyphenylalanine (L-DOPA) to the right, with a decrease in the maximum response." | ( The effects of pertussis toxin on dopamine D2 and serotonin 5-HT1A autoreceptor-mediated inhibition of neurotransmitter synthesis: relationship to receptor reserve. Bohmaker, K; Bordi, F; Meller, E, 1992) | 0.28 |
| "Akin to receptor inactivation with phenoxybenzamine (PBZ) (1 microM, 1 hr), treatment of anterior pituitary cells with 17 beta-estradiol (10 nM, 3 days) right-shifted the dose-response curve for inhibition of prolactin (PRL) secretion by the full agonist R-(-)-N-n-propylnorapomorphine (NPA) and reduced the maximal effect [EC50 (pM) and percent maximal effect: control, 25." | ( Comparative effects of receptor inactivation, 17 beta-estradiol and pertussis toxin on dopaminergic inhibition of prolactin secretion in vitro. Bohmaker, K; Diamond, J; Lieu, HD; Meller, E; Puza, T, 1992) | 0.28 |
| " Furthermore, pretreatment with the drug did not affect the dose-response curve for the inhibitory effects of the DA receptor agonist apomorphine or the mixed DA agonist/sigma-receptor ligand (+)-3-(3-hydroxyphenyl)-N-1-propyl)piperidine ((+)-3-PPP)." | ( Sigma-receptors: implication for the control of neuronal activity of nigral dopamine-containing neurons. Engberg, G; Wikström, H, 1991) | 0.28 |
| " Its dose-response curve was bell-shaped with maximal effects at a dose of 100 micrograms/kg." | ( Occurrence of yawning and decrease of prolactin levels via stimulation of dopamine D2-receptors after administration of SND 919 in rats. Domae, M; Furukawa, T; Matsumoto, S; Nagashima, M; Shirakawa, K; Yamada, K, 1989) | 0.28 |
| " decreased responding to a level significantly below baseline, thus resulting in a biphasic dose-response curve." | ( Anxiolytic-like action of the 3-PPP enantiomers in the Vogel conflict paradigm. Carlsson, A; Engel, JA; Hjorth, S, 1987) | 0.27 |
| " When a dose-response was determined by administering each dose in a single bolus injection, apomorphine and (+)-3-PPP produced dose-related inhibitions of fast-firing dopaminergic neurons, with the largest dose of each compound completely inhibiting nearly all cells tested." | ( Effects of intraperitoneal administration of apomorphine and the isomers of 3-(1-propyl-3-piperidinyl)phenol on the firing activity of substantia nigra dopamine neurons: comparison of agonist efficacies and development of acute tolerance. Christoffersen, CL; Meltzer, LT, 1988) | 0.27 |
| ") elicited yawning in rats and the dose-response curves of all 3 compounds showed a bell-shaped form." | ( Effects of apomorphine, TL-99 and 3-PPP on yawning in rats. Boissard, CG; Delini-Stula, A; Mogilnicka, E, 1984) | 0.27 |
| " Lever pressing for intracranial self-stimulation (ICSS) was attenuated in a dose-related fashion by TL-99 and 3-PPP, with relatively shallow dose-response relationships." | ( Avoidance and ICSS behavioral models dissociate TL-99 and 3-PPP from dopamine receptor antagonists. Fenton, HM; Gerhardt, S; Hall, NR; Liebman, JM; Neale, R; Noreika, L, 1983) | 0.27 |
| " The measured reduction in dopamine D2 receptor density after EEDQ was of the same magnitude as the reduction in receptor number predicted from the EEDQ induced shift in the dose-response curve of the full dopamine D2 receptor agonist NPA." | ( A high dose of EEDQ reduces pituitary dopamine D2 receptor density and the prolactin suppressive potency of agonists. Ekman, A; Eriksson, E, 1993) | 0.29 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| piperidines | |
| [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 Targets (40)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| dopamine D1 receptor | Homo sapiens (human) | Potency | 0.5174 | 0.0052 | 1.3022 | 8.1995 | AID624455 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 10.1894 | 0.1000 | 20.8793 | 79.4328 | AID488772; AID588453; AID588456 |
| GLS protein | Homo sapiens (human) | Potency | 3.5481 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.1682 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 25.1189 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 6.3391 | 0.0224 | 5.9449 | 22.3872 | AID488982; AID488983 |
| dopamine D1 receptor | Homo sapiens (human) | Potency | 5.1735 | 0.0052 | 1.3022 | 8.1995 | AID624455 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.0251 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
| GLS protein | Homo sapiens (human) | Potency | 35.4813 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 0.1683 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| arylsulfatase A | Homo sapiens (human) | Potency | 0.1694 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 8.9125 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 8.4921 | 0.4256 | 12.0591 | 28.1838 | AID504536 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 18.0109 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
| chaperonin GroEL | Methanococcus maripaludis S2 | Potency | 79.4328 | 31.6228 | 31.6228 | 31.6228 | AID488978 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.0000 | 0.0003 | 0.5026 | 7.7625 | AID61185 |
| D(2) dopamine receptor | Bos taurus (cattle) | Ki | 0.2384 | 0.0000 | 0.5836 | 6.1000 | AID62337; AID62338 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 0.5650 | 0.0000 | 0.4362 | 10.0000 | AID63849 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.1603 | 0.0000 | 0.6020 | 10.0000 | AID65135; AID65786 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.4954 | 0.0001 | 0.5494 | 8.4000 | AID62011; AID64440; AID64442 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.1200 | 0.0000 | 0.4375 | 10.0000 | AID65559; AID65560 |
| 5-hydroxytryptamine receptor 2C | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0002 | 0.6677 | 10.0000 | AID64170 |
| D(2) dopamine receptor | Homo sapiens (human) | Ki | 0.3580 | 0.0000 | 0.6518 | 10.0000 | AID1391846; AID458632; AID458633; AID61172; AID61486; AID65887; AID65895 |
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0001 | 0.6017 | 10.0000 | AID64170 |
| 5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0001 | 0.7396 | 10.0000 | AID64170 |
| D(2) dopamine receptor | Bos taurus (cattle) | Ki | 4.8767 | 0.0000 | 0.5836 | 6.1000 | AID64170; AID64172; AID64173 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 0.0160 | 0.0000 | 0.4362 | 10.0000 | AID61809 |
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0003 | 1.2967 | 9.2440 | AID64170 |
| 5-hydroxytryptamine receptor 1D | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0010 | 1.6747 | 9.2000 | AID64170 |
| 5-hydroxytryptamine receptor 1F | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0010 | 1.6747 | 9.2000 | AID64170 |
| 5-hydroxytryptamine receptor 2B | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0002 | 0.5909 | 10.0000 | AID64170 |
| 5-hydroxytryptamine receptor 6 | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0002 | 0.4254 | 2.1000 | AID64170 |
| 5-hydroxytryptamine receptor 7 | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0000 | 0.1480 | 3.1800 | AID64170 |
| 5-hydroxytryptamine receptor 5A | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.3010 | 1.3003 | 2.1000 | AID64170 |
| 5-hydroxytryptamine receptor 5B | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.3010 | 1.3003 | 2.1000 | AID64170 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 0.0785 | 0.0000 | 0.6020 | 10.0000 | AID1391847; AID239943; AID64989; AID65627 |
| 5-hydroxytryptamine receptor 3A | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0002 | 0.4841 | 10.0000 | AID64170 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 2.0703 | 0.0001 | 0.5494 | 8.4000 | AID63661; AID64265; AID64428; AID64429 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.1991 | 0.0000 | 0.4375 | 10.0000 | AID65717; AID65737; AID65738; AID65890 |
| 5-hydroxytryptamine receptor 4 | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0016 | 1.0253 | 5.0119 | AID64170 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.2340 | 0.0000 | 0.4901 | 10.0000 | AID204630 |
| 5-hydroxytryptamine receptor 3B | Rattus norvegicus (Norway rat) | Ki | 2.1000 | 0.0002 | 0.5023 | 10.0000 | AID64170 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.1599 | 0.0003 | 0.5570 | 4.2000 | AID229204; AID229209 |
| D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.9300 | 0.0003 | 0.5026 | 7.7625 | AID62866 |
| D(3) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.9300 | 0.0003 | 0.3907 | 5.4000 | AID62866 |
| D(1B) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.9300 | 0.0003 | 0.3563 | 5.4000 | AID62866 |
| D(4) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.9300 | 0.0003 | 0.3871 | 5.4000 | AID62866 |
| C-8 sterol isomerase | Saccharomyces cerevisiae S288C | Ki | 1.2000 | 0.0000 | 0.9048 | 7.1500 | AID239296 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 12.0545 | 0.0001 | 0.5494 | 8.4000 | AID62866; AID63661; AID64265; AID64428; AID64429 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 0.1890 | 0.0000 | 0.4375 | 10.0000 | AID65715 |
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase | Homo sapiens (human) | Ki | 2.2000 | 0.0004 | 0.5490 | 6.7000 | AID239597 |
| Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 0.0060 | 0.0000 | 0.4901 | 10.0000 | AID239347 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0311 | 0.0003 | 0.5570 | 4.2000 | AID229204; AID229209 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 0.4610 | 0.0000 | 0.1874 | 3.9000 | AID1265376; AID1265381; AID1265382 |
| D(4) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 0.0600 | 0.0014 | 0.0889 | 2.2300 | AID61802 |
| D(3) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 0.0308 | 0.0001 | 0.0247 | 0.6690 | AID1265371; AID64816 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.0190 | 0.0004 | 0.3299 | 3.9100 | AID61304; AID61491 |
| 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 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| D(2) dopamine receptor | Homo sapiens (human) | Ke | 0.3723 | 0.3620 | 0.3723 | 0.3830 | AID1265380; AID1265385; AID1265386 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Log IC50 | 0.3800 | 0.2300 | 0.3050 | 0.3800 | AID63992 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | Log IC50 | 0.8100 | 0.8100 | 1.1650 | 1.5200 | AID204628 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Log IC50 | 0.2300 | 0.2300 | 0.3050 | 0.3800 | AID63992 |
| Sigma non-opioid intracellular receptor 1 | Rattus norvegicus (Norway rat) | Log IC50 | 1.5200 | 0.8100 | 1.1650 | 1.5200 | AID204628 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (138)
Molecular Functions (22)
Ceullar Components (38)
Bioassays (321)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID168315 | Evaluated for rat locomotor activity in nonhabituated rats at 213 umol / kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID65560 | Binding towards Dopamine receptor D2 using [3H]spiperone from rat striatal membrane | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID230411 | It is the ratio of ED50 for stimulation of locomotor activity to that of inhibition of locomotor activity | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID168030 | Rat locomotor activity in reserpine pretreated rats and accumulated counts / 30 min is calculated | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID138939 | Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 33 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. |
| AID64267 | Binding affinity towards dopamine receptor D2 in rat striatal membrane using [3H]spiperone | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID63849 | Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID65786 | Binding towards Dopamine receptor D3 expressed in CHO-K1 cells using [3H]spiperone | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID62338 | Evaluated for binding towards Dopamine receptor D2 using [3H]-spiperone as radioligand, in cloned mammalian receptors expressed in CHO-K1 cells | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID168318 | Evaluated for rat locomotor activity in nonpretreated habituated rats at 100 umol / kg | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID139078 | Antagonism of apomorphine in reserpinized mice when a dose of 3.3 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. |
| AID168129 | Evaluated for DOPA accumulation in striatum of nonpretreated rat at 25 umol / kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID138772 | Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice when a dose of 33 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. |
| AID168659 | Evaluated in rat striatum for the effect on DOPAC release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID168119 | Evaluated for DOPA accumulation in limbic region of nonpretreated rat at 25 umol / kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID204607 | Binding effinity for sigma receptor using 2 nM of [3H]DTG as radioligand, in membranes from brain minus cerebellum | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID168316 | Evaluated for rat locomotor activity in nonhabituated rats at 25 umol / kg | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID62011 | Inhibition of [3H]haloperidol binding for Dopamine receptor D2 in rat striatal membranes. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID178065 | Inhibition of locomotor activity was determined after (sc) administration in rat (40% inhibition was determined at 3 mg/kg) | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID62337 | Binding towards Dopamine receptor D2 expressed in CHO-K1 cells using [3H]U-86170 | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID177278 | 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; 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. |
| AID140794 | In vitro inhibitory activity was determined against dopamine synthesis in mouse striatal synaptosomes | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and dopamine autoreceptor activity of a 5-(methylmercapto)methyl-substituted derivative of (+/-)-3-PPP (3-(3-hydroxyphenyl)-1-n-propylpiperidine). |
| AID178066 | Inhibition of locomotor activity was determined after oral administration in rat | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID139071 | Antagonism of apomorphine in reserpinized mice 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. |
| AID168121 | Evaluated for DOPA accumulation in limbic region of reserpine pretreated rat at 100 umol / kg administered intraperitoneally | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID178573 | Effective dose required to inhibit the Locomotor activity in Rat after po administration; NT=Not tested (ED50 mg/Kg) | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID64442 | Inhibition of [3H]haloperidol binding for Dopamine receptor D2 in rat striatal membranes. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID177932 | Antagonism of apomorphine induced stereotype in rats was recorded at 30 minutes after subcutaneous administration of apomorphine | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID176372 | Contralateral circling behavior in 6-OH-DA-lesioned rats was recorded after subcutaneous administration | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID181024 | Percent reduction of hemispheres in cortex was measured in the brain of reserpinized rats; 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. |
| AID168660 | Evaluated in rat striatum for the effect on dopamine release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID138910 | Antagonism of apomorphine for 0-10 minutes in reserpinized mice when a dose of 3.3 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. |
| AID61185 | Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID168655 | Evaluated in rat accumbens for the effect on DOPAC release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID64163 | Compound was evaluated for the intrinsic activity from GTP shift against dopamine receptor D2 | 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. |
| AID185791 | Percentage inhibition of DA neural firing after administration the compound at a dose of 2.5 mg/Kg through ip route in rats. | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID178692 | Compound was tested for stimulation of locomotor activity after sc administration in rat | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID168123 | Evaluated for DOPA accumulation in limbic region of reserpine pretreated rat at 27 umol / kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID138764 | Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice when a dose of 3.3 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. |
| AID138932 | Antagonism of apomorphine for 10-20 minutes in reserpinized mice when a dose of 3.3 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. |
| AID177121 | ED50 value was measured as dose required to produce a half-maximal reduction of Dopa 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. |
| AID138757 | Ability to stimulate dopaminergic systems by effect on locomotor activity in reserpinized mice 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. |
| AID65559 | Evaluated for binding towards Dopamine receptor D2 using [3H]N-0437 as radioligand from rat striatal membrane | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID178247 | Inhibition of spontaneous locomotor activity was performed in photocell cages at 30-45 minutes after subcutaneous administration | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID109883 | Inhibitory activity was determined against inhibition of gamma-butyrolactone (GBL) induced Dopa accumulation by compound administered subcutaneously; Range 10-320 | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and dopamine autoreceptor activity of a 5-(methylmercapto)methyl-substituted derivative of (+/-)-3-PPP (3-(3-hydroxyphenyl)-1-n-propylpiperidine). |
| AID139086 | Antagonism of apomorphine in reserpinized mice when a dose of 33 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. |
| AID176632 | Reversal of reserpine plus alpha-Methyl-p-tyrosine-induced hypoactivity in rats was recorded after subcutaneous administration; NT is not tested | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID61044 | In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390 | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID138917 | Antagonism of apomorphine for 0-10 minutes in reserpinized mice when a dose of 33 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. |
| AID204000 | Opioid activity in terms of inhibition of [3H]dihydromorphine binding to opioid receptor mu in rat brain membrane. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Binding of substituted and conformationally restricted derivatives of N-(3-phenyl-n-propyl)-1-phenyl-2-aminopropane at sigma-receptors. |
| AID108714 | Dopa accumulation induced by GBL was measured in mouse after subcutaneous administration of 32 umol/kg of compound | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and dopamine autoreceptor activity of a 5-(methylmercapto)methyl-substituted derivative of (+/-)-3-PPP (3-(3-hydroxyphenyl)-1-n-propylpiperidine). |
| AID138926 | Antagonism of apomorphine for 10-20 minutes in reserpinized mice 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. |
| AID178524 | Compound was tested for inhibition of locomotor activity after sc administration in rat | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID171358 | Values for the reversal of the increase in DOPA levels in the striatum of GBL-treated rats after ip administration of 10 mg/Kg | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID138782 | Antagonism of apomorphine for 0-10 minutes in reserpinized mice 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. |
| AID167996 | Evaluated for 5-HTP increase in hemisphere region of nonpretreated rat at 27 umol / kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID177284 | ED50 value was measured as dose required to produce a half-maximal reduction of Serotonin (5-HTP) accumulation in 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. |
| AID168656 | Evaluated in rat accumbens for the effect on dopamine release and metabolism in brain dialysis model after administration of 50 umol / kg subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID64440 | Inhibition of [3H]N-propylnorapomorphine binding to Dopamine receptor D2 of rat striatal membranes | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID176553 | Decrease of DOPA formation effected by 30 mg/kg administered intraperitoneally in the striatum of GBL-treated rats | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID167999 | Evaluated for 5-HTP increase in limbic region of nonpretreated rat at 27 umol / kg administered subcutaneously | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID203982 | Displacement of [3H]DTG from sigma opioid receptor of homogenized guinea pig whole brain | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6 | Radiosynthesis of sigma receptor ligands for positron emission tomography: 11C- and 18F-labeled guanidines. |
| AID131896 | Effective dose required to inhibit the Locomotor activity in mouse after ip administration; NT=Not tested (ED50 mg/Kg) | 1991 | Journal of medicinal chemistry, Sep, Volume: 34, Issue:9 | Dopamine autoreceptor agonists as potential antipsychotics. 3.6-Propyl-4,5,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine. |
| AID13531 | Area under curve (AUC) is the drug concentrations in blood samples of rats with arterial catheters at 5 min and 12 hr plotted against time | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists. |
| AID176640 | Reversal of reserpine-induced depression in rat after subcutaneous administration | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | 4-(1,2,5,6-Tetrahydro-1-alkyl-3-pyridinyl)-2-thiazolamines: a novel class of compounds with central dopamine agonist properties. |
| AID65135 | Compound was measured for its ability to compete with [3H]spiperone binding to the human Dopamine receptor D3 transfected in CHO cells | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach. |
| AID177127 | ED50 value was measured as dose required to produce a half-maximal reduction of Dopa accumulation in the 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. |
| AID493017 | Wombat Data for BeliefDocking | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| 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 | |||
| 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. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| 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. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| 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. |
| AID458634 | Selectivity ratio of Ki for human dopamine D2 receptor at low affinity state to Ki for human dopamine D2 receptor at high affinity state | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16). |
| AID61854 | Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand; ND = Not determined | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID173570 | Dose required for postsynaptic agonism using motor activity test in reserpinized rats | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID185691 | Level of compound in rat cerebellum at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID175375 | DOPA accumulation in normal rat limbic region at 213 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID173684 | Locomotor activity in normal rat at 0.8 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID64172 | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, high affinity site | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID61491 | Effective concentration required for agonistic activity against rat D2 short receptor | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID1265386 | Antagonist activity against human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding at 1 uM | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID1265382 | Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 1 uM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM) | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID1391846 | Binding affinity to human dopamine D2 receptor | |||
| AID61809 | Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300) | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID1265381 | Antagonist activity against human D2 receptor expressed in CHO cells assessed as dopamine EC50 at 200 nM by [35S]GTPgammaS binding assay (Rvb = 225 +/- 45 nM) | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID185659 | Effect on HVA level in rat brain striatum regions at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID61857 | Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina; not determined | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID169618 | Evaluated biochemically in reserpine-pretreated habituated rats for (100 umol/kg) subcuteneous dose in rat striatum (DOPAacc), Value expressed as counts/30 min | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID61172 | Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D2 long (high/low affinity is given as 9.0/1800) | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID175602 | The in vivo effect of the compound (sc injection, 227 umol/kg) on DOPA accumulation in limbic and striatal regions of reserpine-pretreated rat brains. | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | On the quantitative structure-activity relationships of meta-substituted (S)-phenylpiperidines, a class of preferential dopamine D2 autoreceptor ligands: modeling of dopamine synthesis and release in vivo by means of partial least squares regression. |
| AID176633 | Reversal of reserpine plus alpha-Methyl-p-tyrosine-induced hypoactivity in rats was recorded at 1 h after administration | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID176539 | DOPA accumulation in reserpine-pretreated rat limbic region after subcutaneous administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID185838 | Level of compound in rat intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID1265371 | Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID194724 | Evaluated biochemically in reserpine-pretreated habituated rats for (100 umol/kg) subcuteneous dose, Value expressed as locomotor activity (LMA) | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID204628 | Displacement of (+)-3PPP from sigma receptor of rat brain membrane | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | Molecular similarity, quantitative chirality, and QSAR for chiral drugs. |
| AID62328 | Binding affinity of compound against Dopamine receptor D2 was measured using [3H]pramipexole in Bovine striatal membranes | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID185699 | Level of compound in rat cortex at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID64989 | Binding affinity of compound measured using [3H]-spiperone for the cloned human Dopamine receptor D3 (high/low affinity is given as 25/1600) | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID176372 | Contralateral circling behavior in 6-OH-DA-lesioned rats was recorded after subcutaneous administration | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID177931 | Antagonism of apomorphine induced stereotype in rats was recorded at 30 minutes after subcutaneous administration apomorphine | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID184547 | Motor activity effect in reserpinized rat at 213 umol/kg, sc expressed as accumulation counts 0-30 min after treatment | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID170086 | Postsynaptic agonistic activity using motor activity test in reserpinized rats per 30 min | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID173915 | Low dose of compound giving significant reduction and increase in motor activity without pretreatment was determined; motor activity 74% of control was observed at the lowest dose | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID458632 | Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16). |
| AID185689 | Level of compound 5 in rat striatum at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185684 | Level of compound 5 in rat cerebellum at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID170164 | Effect of (60 min after administration of 200 (uM/kg) subcuteneous dose on DA release in brain dialysis model of rat striatum; Values expressed as percent of saline controls | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID65890 | Affinity against striatal dopamine D2 receptors using [3H]spiperone as radioligand in rats. | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID229209 | Binding affinity against sigma receptor | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID189818 | post-synaptic dopaminergic effect was assessed by the increase in locomotor activity at 30 min time interval by 213 umol/kg dosage administration | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID178249 | Inhibition of spontaneous locomotor activity was performed in photocell cages. Motility was measured at 30-40 minutes after subcutaneous administration; value ranges from 4.2-11 | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID185839 | Level of compound in rat striatum at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID1265375 | Selectivity ratio of EC50 for human D2 receptor expressed in CHO cells to EC50 for human D3 receptor expressed in CHO cells | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID194723 | Evaluated biochemically in nonpretreated habituated rats for (100 uM/kg) subcuteneous dose, Value expressed as locomotor activity (LMA) | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID170269 | Motor activity with reserpine pretreatment at dose 213 uM/kg | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID173492 | Half-maximal decrease of DOPA accumulation (no reserpine pretreatment) in the striatum of rat brain at dose 27 uM/kg | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID232104 | Ratio of binding affinities for dopamine transporter over sigma-1 receptor | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| AID173483 | Half-maximal decrease of DOPA accumulation (no reserpine pretreatment) in the limbic system of rat brain at dose 213 uM/kg | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID194722 | Evaluated biochemically in nonhabituated rats for (100 umol/kg) subcuteneous dose, Value expressed as locomotor activity (LMA) | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID174026 | Presynaptic activity at the level of DA metabolism was determined at dose 45 umol/kg on striatal level of HVA | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID232373 | Ratio of D2-D3 like receptor to D4 like receptor | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID176558 | Dopa accumulation was evaluated in corpus striatum of male Sprague-Dawley rat | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID62706 | Presynaptic agonistic activity against dopamine receptor in limbic system | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID65737 | In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the agonist [3H]quinpirole to label the high affinity state (D2 high) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans. |
| AID170165 | Effect on extracellular DA levels in the striatal region of rat brain. | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | On the quantitative structure-activity relationships of meta-substituted (S)-phenylpiperidines, a class of preferential dopamine D2 autoreceptor ligands: modeling of dopamine synthesis and release in vivo by means of partial least squares regression. |
| AID229204 | In vitro for binding affinity against sigma receptor using [3H](+)-3-PPP as radioligand | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID197520 | In vivo presynaptic dopaminergic potency, determined by the ability to reduce the accumulation of DOPA by 50% | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID65738 | In vitro binding affinity to rat striatal Dopamine receptor D2 was determined using the antagonist [3H]spiperone + GTP to label the low affinity state (D2 low) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans. |
| AID1265370 | Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to dopamine | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID65627 | Tested for in vitro binding affinity against cloned mammalian dopamine D3 receptor, expressed in CHO-K1 cells, using [3H]spiperone as radioligand | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID1265380 | Antagonist activity against human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID234956 | Selectivity pIC50 (sigma)-pIC50(D2) | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID64816 | Effective concentration required for agonistic activity against human D3 receptor | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID184549 | Motor activity effect in reserpinized rat with tropolone pretreatment at 10 umol/kg, ip expressed as accumulation counts 0-30 min after treatment | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID230928 | Ratio of the binding affinity to low affinity state (D2 low) to high affinity state (D2 high) | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans. |
| AID65717 | In vitro affinity against dopamine receptor D2 using [3H]DP-5,6-ADTN radioligand in rat striatal homogenate | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185658 | Effect on HVA level in rat brain limbic regions at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID176546 | DOPA accumulation in reserpine-pretreated rat striatal region after subcutaneous administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID63992 | Displacement of spiperone from dopamine receptor D2 of rat brain membrane | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | Molecular similarity, quantitative chirality, and QSAR for chiral drugs. |
| AID176538 | DOPA accumulation in reserpine-pretreated rat cortex after subcutaneous administration; Inactive | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID239943 | Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells | 2005 | Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7 | CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. |
| AID176584 | Half-maximal decrease of DOPA accumulation upon reserpine pretreatment in the corpus striatum of rat brain | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID64170 | Tested for binding affinity against Dopamine receptor D2 like from bovine striatum membranes by using [3H]YM-09151-2 radioligand | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID458635 | Activity at dopamine D2L receptor expressed in HEK293 cells coexpressing Galphaqi5 assessed as maximal efficacy relative to control | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16). |
| AID185692 | Level of compound in rat cerebellum at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID175368 | DOPA accumulation in normal rat cortex at 27 umol/kg expressed as percent of control; Inactive | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID178250 | Inhibition of spontaneous locomotor activity was performed in photocell cages. Motility was measured at 5 minutes | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID64302 | Binding affinity for dopamine D2-D3 like receptor labelled with [3H]YM-09151-2 in striatum | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID185687 | Level of compound 5 in rat cortex at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185686 | Level of compound 5 in rat cortex at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185688 | Level of compound 5 in rat intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID64429 | In vitro inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal membranes | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID63651 | Tested in vivo for binding affinity against Dopamine receptor D2 using nonradiolabeled 5,6-di-n-Pr-ADTN | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID62709 | Presynaptic agonistic activity against dopamine receptor in striatum | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID65895 | In vitro binding affinity against cloned mammalian dopamine D2 autoreceptor, expressed in CHO-K1 cells, using [3H]U-86170 as radioligand | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID61384 | Ability to displace [3H]spiroperidol, from dopamine receptor D2 specific binding sites of rat striatal membranes | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine. |
| AID169627 | Evaluated for DOPAC level in nonpretreated habituated rats after subcuteneous dose of 100 micro mol/kg in rat striatum | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID169620 | Evaluated for DOPA accumulation (DOPAacc) level in nonhabituated rats after subcuteneous dose (100 uM/kg) in rat striatum | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID458631 | Reduction in 3,4-dihydroxyphenylacetic acid level in Sprague-Dawley rat striatum at 117 umol/kg, sc relative to saline treated control | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16). |
| AID175367 | DOPA accumulation in normal rat cortex at 213 umol/kg expressed as percent of control; Inactive | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID1265377 | Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay relative to dopamine | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID186196 | Locomotor activity in reserpine-pretreated ratat the dose of 213 umol/kg; Accumulation counts/30 min | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID65191 | Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| AID458646 | Reduction in spontaneous locomotor activity in Sprague-Dawley rat striatum at 117 umol/kg, sc relative to control | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16). |
| AID23982 | Apparent lipophilicity (log kw) at pH 7.5 | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID64173 | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, low affinity site | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | N-n-Propyl-substituted 3-(dimethylphenyl)piperidines display novel discriminative properties between dopamine receptor subtypes: synthesis and receptor binding studies. |
| AID458633 | Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16). |
| AID64428 | In vitro inhibition of [3H]N-0437 binding to Dopamine receptor D2 in rat striatal membranes | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID63853 | Binding affinity for dopamine D4-like receptor labelled with [3H]YM-09151-2 in retina | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID176585 | Half-maximal decrease of DOPA accumulation upon reserpine pretreatment in the limbic system of rat brain | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID176560 | Dopa accumulation was evaluated in limbic system of male Sprague-Dawley rat | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID61486 | Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D2 short (high/low affinity is given as 27/1800) | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID64265 | Binding affinity against Dopamine receptor D2 using [3H]spiperone as radioligand | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID204630 | Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13 | Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents. |
| AID1391847 | Binding affinity to human dopamine D3 receptor | |||
| AID173820 | Locomotor activity in normal rat at 213 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID184694 | Motor activity effect in reserpinized rat with tropolone pretreatment at 50 umol/kg, ip expressed as accumulation counts 0-30 min after treatment | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID1265385 | Antagonist activity against human D2 receptor expressed in CHO cells assessed as inhibition of dopamine-induced [35S]GTPgammaS binding at 200 nM | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID178409 | Effective dose required for DOPA accumulation (presynaptic dopaminergic effect) in rat | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID185657 | Effect on DOPAC level in rat brain striatum regions at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID174025 | Presynaptic activity at the level of DA metabolism was determined at dose 45 umol/kg on striatal level of DOPAC | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID4336 | Tested for affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT in homogenized rat brain tissue | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID61304 | Effective concentration required for agonistic activity against rat D2 long receptor | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID65887 | Affinity against recombinant dopamine receptor (DA) D2 expressed in CHO-K1 cells, using [3H]-spiperone as radioligand | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships. |
| AID185700 | Level of compound in rat cortex at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID175523 | DOPA accumulation in normal rat striatal region at 27 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID175517 | DOPA accumulation in normal rat limbic region at 27 umol/kg expressed as percent of control; Inactive | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID63661 | Binding affinity for dopamine receptor D2 was evaluated by the ability to displace [3H]spiperone | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID173740 | High dose of compound giving significant reduction and increase in motor activity without pretreatment was determined; motor activity 40% of control was observed at the highest dose | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID1265376 | Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treat |
| AID175604 | In vivo effect on DOPA accumulation in limbic and striatal regions of the rat brain without reserpine pretreatment | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16 | On the quantitative structure-activity relationships of meta-substituted (S)-phenylpiperidines, a class of preferential dopamine D2 autoreceptor ligands: modeling of dopamine synthesis and release in vivo by means of partial least squares regression. |
| AID185685 | Level of compound 5 in rat cerebellum at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185656 | Effect on DOPAC level in limbic system of rat brain at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID63185 | Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390; ND means not determined | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| AID61802 | Effective concentration required for agonistic activity against human D4.2 receptor | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17 | Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. |
| 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. |
| AID193713 | DA2 antagonist activity was tested by its ability to decrease the arterial pressure in anesthetized rat at 30 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID170086 | Postsynaptic agonistic activity using motor activity test in reserpinized rats per 30 min | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID193710 | DA2 antagonist activity was tested by its ability to decrease the arterial pressure in anesthetized rat at 10 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID193560 | DA2 antagonist activity was tested by its ability to decrease the heart rate in anesthetized rat at 100 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID64428 | In vitro inhibition of [3H]N-0437 binding to Dopamine receptor D2 in rat striatal membranes | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID173916 | Low dose of compound giving significant reduction and increase in motor activity without pretreatment was determined; motor activity 75% of control was observed at the lowest dose | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID63661 | Binding affinity for dopamine receptor D2 was evaluated by the ability to displace [3H]spiperone | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID185658 | Effect on HVA level in rat brain limbic regions at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID193559 | DA2 antagonist activity was tested by its ability to decrease the heart rate in anesthetized rat at 10 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID229203 | Eudisimic index was determined for the compound against sigma receptor | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID62706 | Presynaptic agonistic activity against dopamine receptor in limbic system | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID63853 | Binding affinity for dopamine D4-like receptor labelled with [3H]YM-09151-2 in retina | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID176372 | Contralateral circling behavior in 6-OH-DA-lesioned rats was recorded after subcutaneous administration | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID174026 | Presynaptic activity at the level of DA metabolism was determined at dose 45 umol/kg on striatal level of HVA | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID173820 | Locomotor activity in normal rat at 213 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID175364 | DOPA accumulation in normal rat cortex at 0.8 umol/kg expressed as percent of control; Inactive | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID192379 | post-synaptic dopaminergic effect was assessed by the increase in locomotor activity at 30 min time interval by 13 umol/kg dosage administration | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID178251 | Inhibition of spontaneous motility was measured 5 min after subcutaneous administration is 2.4; ND means no data | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID183234 | Inhibition of dopamine neuronal firing in the anesthetized rats after ip administration at a dose 2.5 mg/kg | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID173488 | Half-maximal decrease of DOPA accumulation (no reserpine pretreatment) in the striatum of rat brain at dose 0.8 uM/kg | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID176560 | Dopa accumulation was evaluated in limbic system of male Sprague-Dawley rat | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID176633 | Reversal of reserpine plus alpha-Methyl-p-tyrosine-induced hypoactivity in rats was recorded at 1 h after administration | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID204616 | Inhibition of [3H]NANM binding to sigma receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Rigid phencyclidine analogues. Binding to the phencyclidine and sigma 1 receptors. |
| AID64429 | In vitro inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal membranes | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID64302 | Binding affinity for dopamine D2-D3 like receptor labelled with [3H]YM-09151-2 in striatum | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID176585 | Half-maximal decrease of DOPA accumulation upon reserpine pretreatment in the limbic system of rat brain | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID175121 | DA2 antagonist activity was tested by the duration of onset of action of cardiovascular response at 30 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID175520 | DOPA accumulation in normal rat striatal region at 0.8 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID234956 | Selectivity pIC50 (sigma)-pIC50(D2) | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID239347 | Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. |
| AID173478 | Half-maximal decrease of DOPA accumulation (no reserpine pretreatment) in the limbic system of rat brain at dose 0.8 uM/kg | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID175523 | DOPA accumulation in normal rat striatal region at 27 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID156836 | Inhibition of binding to PCP receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Rigid phencyclidine analogues. Binding to the phencyclidine and sigma 1 receptors. |
| AID175376 | DOPA accumulation in normal rat limbic region at 27 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID65715 | In vitro affinity against Dopamine receptor D2 using [3H]DP-5,6-ADTN radioligand in rat striatal homogenate | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID63992 | Displacement of spiperone from dopamine receptor D2 of rat brain membrane | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | Molecular similarity, quantitative chirality, and QSAR for chiral drugs. |
| AID232373 | Ratio of D2-D3 like receptor to D4 like receptor | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID185685 | Level of compound 5 in rat cerebellum at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID186195 | Locomotor activity in reserpine-pretreated ratat the dose of 13 umol/kg; Accumulation counts/30 min | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID185838 | Level of compound in rat intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID61242 | Eudisimic index was determined for the compound against Dopamine receptor D2 | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID185699 | Level of compound in rat cortex at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID229204 | In vitro for binding affinity against sigma receptor using [3H](+)-3-PPP as radioligand | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID204628 | Displacement of (+)-3PPP from sigma receptor of rat brain membrane | 1994 | Journal of medicinal chemistry, May-27, Volume: 37, Issue:11 | Molecular similarity, quantitative chirality, and QSAR for chiral drugs. |
| AID23982 | Apparent lipophilicity (log kw) at pH 7.5 | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID178064 | Inhibition of locomotor activity in rats, after sc injection after dosing for a period of 30 min | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID64265 | Binding affinity against Dopamine receptor D2 using [3H]spiperone as radioligand | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID62866 | In vitro inhibition of [3H]haloperidol (HPD) binding to dopamine (DA) receptor of rat striatal membranes | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID185659 | Effect on HVA level in rat brain striatum regions at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID193993 | Effect on DOPAC level in limbic system of rat brain at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID185686 | Level of compound 5 in rat cortex at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID193562 | DA2 antagonist activity was tested by its ability to decrease the heart rate in anesthetized rat at 30 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID233109 | Ratio of reversal of 6-OHDA-induced depression to inhibition of locomotor activity | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID176539 | DOPA accumulation in reserpine-pretreated rat limbic region after subcutaneous administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID185689 | Level of compound 5 in rat striatum at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID175372 | DOPA accumulation in normal rat limbic region at 0.8 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID173817 | Locomotor activity in normal rat at 1.6 umol/kg expressed as percent of control | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID193711 | DA2 antagonist activity was tested by its ability to decrease the arterial pressure in anesthetized rat at 100 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID176626 | Reversal of 6-OHDA-induced depression in rats, after sc injection after dosing for a period of 30 min | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID176538 | DOPA accumulation in reserpine-pretreated rat cortex after subcutaneous administration; Inactive | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID239597 | Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. |
| AID185688 | Level of compound 5 in rat intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID176558 | Dopa accumulation was evaluated in corpus striatum of male Sprague-Dawley rat | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID170275 | Motor activity with reserpine pretreatment at dose 13 uM/kg | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID63651 | Tested in vivo for binding affinity against Dopamine receptor D2 using nonradiolabeled 5,6-di-n-Pr-ADTN | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID233110 | Ratio of reversal of reserpine-induced depression to inhibition of locomotor activity | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID185845 | Level of compound in rat striatum at dose 45 umol/kg administered subcutaneously. | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185687 | Level of compound 5 in rat cortex at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID62709 | Presynaptic agonistic activity against dopamine receptor in striatum | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID229209 | Binding affinity against sigma receptor | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID185700 | Level of compound in rat cortex at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185657 | Effect on DOPAC level in rat brain striatum regions at a dose of 27 uM/kg sc 60 min before death | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID185684 | Level of compound 5 in rat cerebellum at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID185691 | Level of compound in rat cerebellum at dose 45 umol/kg administered intraperitoneally | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID61857 | Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina; not determined | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2 | Synthesis and dopaminergic properties of the two enantiomers of 3-(3,4-dimethylphenyl)-1-propylpiperidine, a potent and selective dopamine D4 receptor ligand. |
| AID177880 | Inhibition of accumulation of DOPA in rat striatum, after intraperitoneal administration. | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID239296 | Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand | 2005 | Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15 | Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. |
| AID175116 | DA2 antagonist activity was tested by the duration of onset of action of cardiovascular response at 10 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID184546 | Motor activity effect in reserpinized rat at 13 umol/kg, sc expressed as accumulation counts 0-30 min after treatment | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID175117 | DA2 antagonist activity was tested by the duration of onset of action of cardiovascular response at 100 ug/kg | 1993 | Journal of medicinal chemistry, Aug-06, Volume: 36, Issue:16 | 2,5-Dimethoxy congeners of (+)-and (-)-3-(3-hydroxyphenyl)-N-n- propylpiperidine. |
| AID178063 | Inhibition of locomotor activity in rats after peroral administration of the compound. | 1988 | Journal of medicinal chemistry, Aug, Volume: 31, Issue:8 | Dopamine autoreceptor agonists as potential antipsychotics. 1. (Aminoalkoxy)anilines. |
| AID176584 | Half-maximal decrease of DOPA accumulation upon reserpine pretreatment in the corpus striatum of rat brain | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID178409 | Effective dose required for DOPA accumulation (presynaptic dopaminergic effect) in rat | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | N-substituted 1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolines and 3-phenylpiperidines: effects on central dopamine and sigma receptors. |
| AID185692 | Level of compound in rat cerebellum at dose 45 umol/kg administered subcutaneously | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID177932 | Antagonism of apomorphine induced stereotype in rats was recorded at 30 minutes after subcutaneous administration of apomorphine | 1987 | Journal of medicinal chemistry, Jan, Volume: 30, Issue:1 | Indolizidine and quinolizidine derivatives of the dopamine autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). |
| AID173570 | Dose required for postsynaptic agonism using motor activity test in reserpinized rats | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | A molecular mechanics approach to the understanding of presynaptic selectivity for centrally acting dopamine receptor agonists of the phenylpiperidine series. |
| AID174025 | Presynaptic activity at the level of DA metabolism was determined at dose 45 umol/kg on striatal level of DOPAC | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Enantiomers of 3-(3,4-dihydroxyphenyl)- and 3-(3-hydroxyphenyl)-N-n-propylpiperidine: central pre- and postsynaptic dopaminergic effects and pharmacokinetics. |
| AID173739 | High dose of compound giving significant reduction and increase in motor activity without pretreatment was determined; motor activity 230% of control was observed at the highest dose | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | Resolved 3-(3-hydroxyphenyl)-N-n-propylpiperidine and its analogues: central dopamine receptor activity. |
| AID175368 | DOPA accumulation in normal rat cortex at 27 umol/kg expressed as percent of control; Inactive | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID197520 | In vivo presynaptic dopaminergic potency, determined by the ability to reduce the accumulation of DOPA by 50% | 1987 | Journal of medicinal chemistry, Dec, Volume: 30, Issue:12 | Quantitative structure-activity relationships and eudismic analyses of the presynaptic dopaminergic activity and dopamine D2 and sigma receptor affinities of 3-(3-hydroxyphenyl)piperidines and octahydrobenzo[f]quinolines. |
| AID176546 | DOPA accumulation in reserpine-pretreated rat striatal region after subcutaneous administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| 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. |
| 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. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| 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. |
| 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. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| 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. |
| 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. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| 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. |
| 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. |
| 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. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction 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] | ||||
Research
Studies (369)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 164 (44.44) | 18.7374 |
| 1990's | 162 (43.90) | 18.2507 |
| 2000's | 19 (5.15) | 29.6817 |
| 2010's | 19 (5.15) | 24.3611 |
| 2020's | 5 (1.36) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 21.20
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (21.20) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 5 (1.38%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Reviews | 7 (1.93%) | 6.00% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 12 (100.00%) | 84.16% |
| Other | 351 (96.69%) | 84.16% |
| Other | 24 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||