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spiperone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tranquillizers, neuroleptics, 4'-fluoro-4-piperidinobutyrophenone derivatives	2470	749-02-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: spiperone spiroperidol spiroperidone spiropitan	A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA. Molecular weight: 395.48 Formula: C23H26FN3O2 CLOGP: 3 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 52.65 ALOGS: -3.38 ROTB: 6

Molecule

Description

Molfile Inchi Smiles

Synonyms:

spiperone
spiroperidol
spiroperidone
spiropitan

A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.

Molecular weight: 395.48
Formula: C23H26FN3O2
CLOGP: 3
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 52.65
ALOGS: -3.38
ROTB: 6

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1969	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
MeSH PA	D014150	Antipsychotic Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018492	Dopamine Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D014149	Tranquilizing Agents
CHEBI has role	CHEBI:35471	psychotropic drugs
CHEBI has role	CHEBI:35476	neuroleptics
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:48561	dopaminergic antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Schizophrenia	indication	58214004	DOID:5419

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.57	acidic
pKa2	8.15	Basic
pKa3	5.3	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	8.65	CHEMBL	KEGG DRUG
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	ANTAGONIST	Ki	10.22	CHEMBL	KEGG DRUG
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Kd	7.40	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	6.50	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.94	CHEMBL
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	5.80	CHEMBL
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	6.96	CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	8.10	CHEMBL
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	9.92	CHEMBL
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN	ANTAGONIST	Ki	5.30	IUPHAR
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	6.32	PDSP
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	ANTAGONIST	Ki	6	IUPHAR
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	9.70	CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	ANTAGONIST	Ki	8.10	IUPHAR
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	ANTAGONIST	Ki	9.20	IUPHAR
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	4.20	CHEMBL
5-hydroxytryptamine receptor 1F	GPCR	P30939	5HT1F_HUMAN		Ki	8.40	PDSP
5-hydroxytryptamine receptor 1E	GPCR	P28566	5HT1E_HUMAN		Ki	5.30	PDSP
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	6.22	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.49	CHEMBL
HLA class I histocompatibility antigen, A-3 alpha chain	Unclassified	P04439	1A03_HUMAN		Kd	5.60	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		IC50	6.02	CHEMBL
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	8.89	CHEMBL
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	5.32	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		Ki	8.14	CHEMBL
Alpha-1D adrenergic receptor	GPCR		ADA1D_RAT		Ki	7.66	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Ki	10.82	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	7.52	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	9	CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT		Ki	8	CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_MOUSE		Ki	7.20	CHEMBL
5-hydroxytryptamine receptor 2C	GPCR		5HT2C_RAT		Ki	6	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		Ki	7.87	CHEMBL
5-hydroxytryptamine receptor 6	GPCR		5HT6R_RAT	ANTAGONIST	Ki	5.80	IUPHAR
Vesicular acetylcholine transporter	Transporter		VACHT_RAT		Ki	5.99	CHEMBL
Muscarinic acetylcholine receptor	GPCR		ACM1_RAT ACM3_RAT ACM4_RAT ACM5_RAT ACM2_RAT		Ki	4.30	CHEMBL
Serotonin 1 (5-HT1) receptor	GPCR		5HT1A_RAT 5HT1B_RAT 5HT1D_RAT 5HT1F_RAT		Ki	6.80	CHEMBL
Dopamine receptor	GPCR		DRD1_RAT DRD3_RAT DRD5_RAT DRD4_RAT DRD2_RAT		Ki	8.70	CHEMBL
Serotonin 2 (5-HT2) receptor	GPCR		5HT2C_RAT 5HT2A_RAT 5HT2B_RAT		Ki	9.35	CHEMBL
Dopamine receptor	GPCR		DRD3_MOUSE DRD4_MOUSE DRD2_MOUSE DRD1_MOUSE DRD5_MOUSE		IC50	4.46	CHEMBL
Beta-casein	Unclassified		CASB_RAT		Ki	8.81	CHEMBL
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_MOUSE	ANTAGONIST	Ki	8.30	IUPHAR

External reference:

ID	Source
D01051	KEGG_DRUG
C0037956	UMLSCUI
CHEBI:9233	CHEBI
SIP	PDB_CHEM_ID
CHEMBL267930	ChEMBL_ID
D013134	MESH_DESCRIPTOR_UI
DB17056	DRUGBANK_ID
5265	PUBCHEM_CID
99	IUPHAR_LIGAND_ID
1553	INN_ID
4X6E73CJ0Q	UNII
77222007	SNOMEDCT_US

Pharmaceutical products:

None