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Compound InformationSONAR Target prediction
Name:

PERPHENAZINE

Unique Identifier:SPE01503934
MolClass: Checkout models in ver1.5 and ver1.0
Molecular Formula:
Molecular Weight:377.763 g/mol
X log p:16.257  (online calculus)
Lipinksi Failures1
TPSA35.02
Hydrogen Bond Donor Count:0
Hydrogen Bond Acceptors Count:4
Rotatable Bond Count:6
Canonical Smiles:OCCN1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc23)CC1
Source:synthetic
Therapeutics:antipsychotic
Generic_name:Perphenazine
Chemical_iupac_name:2-[4-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
Drug_type:Approved Drug
Pharmgkb_id:PA450882
Kegg_compound_id:C07427
Drugbank_id:APRD00429
Melting_point:97 oC
H2o_solubility:28.3 mg/L
Logp:4.176
Isoelectric_point:7.94
Cas_registry_number:58-39-9
Mass_spectrum:http://webbook.nist.gov/cgi/cbook.cgi?Spec=C58399&Index=0&Type=Mass&Large=on
Drug_category:Antipsychotics; Phenothiazines; Dopamine Antagonists; ATC:N05AB03
Indication:For use in the management of the manifestations of psychotic disorders and for the
control of severe nausea and vomiting in adults.
Pharmacology:Perphenazine is a piperazinyl phenothiazine, acts on the central nervous system, and
has a greater behavioral potency than other phenothiazine derivatives whose side
chains do not contain a piperazine moiety. It is a member of a class of drugs called
phenothiazines, which are dopamine D1/D2 receptor antagonists. Perphenazine is 10 to
15 times as potent as chlorpromazine; that means perphenazine is a highly potent
antipsychotic. In equivalent doses it has approximately the same frequency and
severity of early and late extrapypramidal side-effects compared to Haloperidol.
Mechanism_of_action:Binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The
mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine
D2 neurotransmitter receptors in the chemoreceptor trigger zone and vomiting centre.
Perphenazine also binds the alpha andrenergic receptor. This receptor-s action is
mediated by association with G proteins that activate a phosphatidylinositol-calcium
second messenger system.
Organisms_affected:Humans and other mammals

Found: 203 nonactive | as graph: single | with analogs [1] << Back 31 32 33 34 35 36 37 38 39 40  Next >> [203]
Species: 4932
Condition: CIN2
Replicates: 2
Raw OD Value: r im 0.8305±0.00480833
Normalized OD Score: sc h 1.0177±0.0166115
Z-Score: 0.9902±0.919325
p-Value: 0.41734
Z-Factor: -3.93762
Fitness Defect: 0.8739
Bioactivity Statement: Nonactive
Experimental Conditions
Library:Spectrum
Plate Number and Position:17|F8
Drug Concentration:50.00 nM
OD Absorbance:600 nm
Robot Temperature:27.10 Celcius
Date:2006-02-14 YYYY-MM-DD
Plate CH Control (+):0.038974999999999996±0.00089
Plate DMSO Control (-):0.8017±0.01343
Plate Z-Factor:0.9285
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DBLink | Rows returned: 6
4748 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol
74835 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol dihydrochloride
168090 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethanol hydrochloride
213548 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-1,4-dimethyl-2,3,5,6-tetrahydropyrazin-1-yl]ethanol diiodide
213549 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-1,4-dimethyl-2,3,5,6-tetrahydropyrazin-1-yl]ethanol
4282573 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]-2,3,5,6-tetrahydropyrazin-1-yl]ethanol

internal high similarity DBLink | Rows returned: 1
LOPAC 01145 1.0000

active | Cluster 17541 | Additional Members: 13 | Rows returned: 3
SPE01500184 0
LAT005D03 0
LOPAC 00253 0

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