LASSBio-579: structure in first source [MeSH]
| ID Source | ID |
|---|---|
| PubMed CID | 11624518 |
| CHEMBL ID | 597601 |
| SCHEMBL ID | 6014220 |
| MeSH ID | M0508093 |
| Synonym |
|---|
| L022513 |
| lassbio-579 |
| CHEMBL597601 , |
| bdbm50308002 |
| 1-[(1-(4-chlorophenyl)-1h-pyrazol-4-yl)methyl]-4-phenylpiperazine |
| 591774-47-9 |
| SCHEMBL6014220 |
| 1-[[1-(4-chlorophenyl)pyrazol-4-yl]methyl]-4-phenylpiperazine |
| DTXSID10469649 |
| PD089339 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2A | Rattus norvegicus (Norway rat) | Ki | 4.5700 | AID457689; AID734513 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.6000 | AID763652 |
| D(4) dopamine receptor | Homo sapiens (human) | Ki | 0.1750 | AID734514; AID763658 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.4900 | AID734510 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 8.5350 | AID734511; AID763655 |
| D(2) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 2.4900 | AID734510 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID763656 | Displacement of [3H]-ketanserin from 5HT2A receptor in rat brain cortical membranes after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID734514 | Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID734509 | Displacement of [3H]-prazosin from alpha1B adrenergic receptor in Wistar rat liver membrane after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID457691 | Selectivity index, ratio of Ki for Wistar rat striatum D2-like receptor to Ki for Wistar rat cortex 5HT2A receptor | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID763635 | Antipsychotic activity in CF1 mouse assessed as prevention of apomorphine-induced climbing behaviour at 0.1 to 10 mg/kg, ip administered 30 mins prior apomorphine challenge measured 5 to 30 mins post challenge | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID734512 | Displacement of [3H]-OH-8-DPAT from 5HT1A receptor in Wistar rat hippocampal membrane after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID763657 | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat brain hippocampal membranes after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID734510 | Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID457697 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 30 mins (Rvb = 1.8 +/- 1.1 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID734511 | Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID457689 | Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID457700 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 30 mg/kg, po after 30 mins (Rvb = 1.8 +/- 1.1 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID457687 | Displacement of [3H]nemonapride from D2-like receptor in Wistar rat striatum homogenate | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID457699 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 90 mins (Rvb = 2.4 +/- 2.6 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID457692 | Selectivity index, ratio of Ki for Wistar rat hippocampus 5HT1A receptor to Ki for Wistar rat cortex 5HT2A receptor | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID734520 | Drug metabolism in Wistar rat assessed as CYP1A2-mediated p-hydroxylated metabolite formation at 50 mg/kg, ip after 48 hrs by HPLC analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID457696 | Antipsychotic activity in CF1 mouse assessed as reduction in apomorphine-induced climbing at 15 mg/kg, po | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID457706 | Toxicity in CF1 mouse assessed as induction of motor impairment by measuring permanence time at 15 mg/kg, po by rotarod test (Rvb = 241.4 +/- 18.0 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID763654 | Displacement of [3H]-RX821002 from alpha2 adrenoreceptor in rat brain cortical membranes after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID734513 | Displacement of [3H]-ketanserin from 5HT2A receptor in Wistar rat cortical membrane after 15 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID457688 | Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID734517 | Drug metabolism in Wistar rat assessed as CYP1A2-mediated decrease in parent compound level at 50 mg/kg, ip after 30 mins by HPLC analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID734515 | Displacement of [3H]-YM-09151-2 from D2 dopamine receptor in Wistar rat brain striatal membrane after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID734518 | Drug metabolism in Wistar rat assessed as CYP1A2-mediated p-hydroxylated metabolite formation at 50 mg/kg, ip after 30 mins by HPLC analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID763652 | Displacement of [3H]-prozosin from alpha1B adrenoreceptor in rat liver membranes after 45 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID763651 | Displacement of [3H]-QNB from muscarinic receptor in rat brain cortical membranes at 30 uM after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID763659 | Displacement of [3H]-YM-09151-2 from D2 receptor in rat brain striatal membranes after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID734516 | Drug metabolism in Wistar rat plasma assessed as p-hydroxylated metabolite level at 50 mg/kg, ip after 24 hrs | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID457698 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 60 mins (Rvb = 2.7 +/- 2.9 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID763629 | Selectivity ratio of Ki for dopamine D2 receptor in rat brain striatal membranes to Ki for 5HT2A receptor in rat brain cortical membranes | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID457701 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 30 mg/kg, po after 60 mins (Rvb = 2.7 +/- 2.9 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID734519 | Drug metabolism in Wistar rat assessed as CYP1A2-mediated decrease in parent compound level at 50 mg/kg, ip after 48 hrs by HPLC analysis | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID763655 | Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID457690 | Selectivity index, ratio of Ki for Wistar rat striatum D2-like receptor to Ki for Wistar rat hippocampus 5HT1A receptor | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| AID734508 | Displacement of [3H]-QNB from muscarinic receptor in Wistar rat brain membrane after 60 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Apr, Volume: 62ISSN: 1768-3254 | Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound. |
| AID763658 | Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting | 2013 | European journal of medicinal chemistry, Aug, Volume: 66ISSN: 1768-3254 | Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579. |
| AID457702 | Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 30 mg/kg, po after 90 mins (Rvb = 2.4 +/- 2.6 sec) | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 ISSN: 1464-3391 | Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors. |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (30.00) | 29.6817 |
| 2010's | 7 (70.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (10.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 9 (90.00%) | 84.16% |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Anochlesia | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
| Dementia Praecox | 0 | 2010 | 2016 | 11.0 | high | 0 | 0 | 0 | 1 | 3 | 0 | |
| Disease Models, Animal | 0 | 2013 | 2016 | 9.5 | medium | 0 | 0 | 0 | 0 | 2 | 0 | |
| Hypothermia | 0 | 2008 | 2013 | 13.5 | medium | 0 | 0 | 0 | 1 | 1 | 0 | |
| Hypothermia, Accidental | 0 | 2008 | 2013 | 13.5 | medium | 0 | 0 | 0 | 1 | 1 | 0 | |
| Schizophrenia | 0 | 2010 | 2016 | 11.0 | high | 0 | 0 | 0 | 1 | 3 | 0 | |
| Sensitivity and Specificity | 0 | 2007 | 2007 | 17.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Article | Year |
|---|---|
| Pharmacokinetic evaluation of LASSBio-579: an N-phenylpiperazine antipsychotic prototype. The Journal of pharmacy and pharmacology, , Volume: 60, Issue:6 | 2008 |
| Article | Year |
|---|---|
| Pharmacokinetic evaluation of LASSBio-579: an N-phenylpiperazine antipsychotic prototype. The Journal of pharmacy and pharmacology, , Volume: 60, Issue:6 | 2008 |