All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Stem definition	Drug id	CAS RN
	1796	24219-97-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: mianserin hydrochloride mianserin mianserine (+/-)-Mianserin mianserine hydrochloride mianserin HCl mianserine HCl	A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. Molecular weight: 264.37 Formula: C18H20N2 CLOGP: 4.01 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 6.48 ALOGS: -3.06 ROTB: 0

Drug dosage:

Dose	Unit	Route
60	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	3.40 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	6.48 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	22 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	13.75 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	21.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	9.60 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1976	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Camptocormia	171.27	31.49	29	4876	272	50599947
Coma	170.40	31.49	91	4814	56788	50543431
Pleurothotonus	150.95	31.49	33	4872	1268	50598951
Hyponatraemia	126.38	31.49	91	4814	96048	50504171
Toxicity to various agents	114.89	31.49	121	4784	212378	50387841
Hepatocellular injury	102.23	31.49	50	4855	25897	50574322
Somnolence	88.54	31.49	91	4814	154894	50445325
Fall	86.64	31.49	132	4773	334800	50265419
Poisoning deliberate	84.54	31.49	31	4874	7881	50592338
Agranulocytosis	80.56	31.49	40	4865	21381	50578838
Bradypnoea	77.32	31.49	23	4882	3051	50597168
Drug interaction	74.51	31.49	94	4811	199527	50400692
Cholestasis	74.12	31.49	40	4865	25361	50574858
Bradycardia	68.97	31.49	54	4851	64372	50535847
Miosis	61.09	31.49	23	4882	6287	50593932
Thymus disorder	57.35	31.49	11	4894	217	50600002
Altered state of consciousness	57.02	31.49	32	4873	21878	50578341
Brain death	53.74	31.49	17	4888	2766	50597453
Blood lactic acid	52.26	31.49	9	4896	94	50600125
Housebound	51.27	31.49	10	4895	216	50600003
Vertigo	48.14	31.49	40	4865	51792	50548427
Acute kidney injury	47.97	31.49	82	4823	227976	50372243
Extrapyramidal disorder	47.28	31.49	23	4882	11747	50588472
Sedation complication	47.25	31.49	21	4884	8745	50591474
Drug abuse	43.16	31.49	40	4865	59806	50540413
Cutaneous lymphoma	42.04	31.49	8	4897	151	50600068
Oesophageal food impaction	40.96	31.49	8	4897	174	50600045
Limbic encephalitis	38.99	31.49	8	4897	225	50599994
Morbid thoughts	37.35	31.49	9	4896	533	50599686
Behaviour disorder	35.66	31.49	12	4893	2368	50597851
Oesophageal achalasia	34.43	31.49	8	4897	405	50599814
Drug-device interaction	33.21	31.49	6	4899	84	50600135
Herbal interaction	33.08	31.49	6	4899	86	50600133
Rash	31.62	31.49	3	4902	437468	50162751

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Cerebral artery thrombosis	101.44	25.69	22	3208	720	29570577
Brain scan abnormal	87.61	25.69	20	3210	830	29570467
Coma	84.69	25.69	53	3177	39397	29531900
Areflexia	64.30	25.69	20	3210	2734	29568563
Somnolence	49.62	25.69	56	3174	93899	29477398
Hemiplegia	47.26	25.69	20	3210	6574	29564723
Respiratory distress	46.89	25.69	34	3196	32072	29539225
Poikiloderma	46.63	25.69	9	3221	162	29571135
Ischaemic stroke	46.07	25.69	26	3204	15951	29555346
Cholestasis	44.04	25.69	29	3201	23433	29547864
Facial paralysis	42.99	25.69	21	3209	9608	29561689
Reticulocytosis	42.43	25.69	9	3221	264	29571033
Adenomatous polyposis coli	41.09	25.69	8	3222	151	29571146
Initial insomnia	39.99	25.69	14	3216	2761	29568536
Lichenoid keratosis	39.32	25.69	13	3217	2157	29569140
Hepatocellular injury	39.24	25.69	26	3204	21217	29550080
Agranulocytosis	37.82	25.69	25	3205	20315	29550982
Hepatic cytolysis	36.65	25.69	18	3212	8329	29562968
Poisoning deliberate	36.52	25.69	16	3214	5715	29565582
Blood glucose fluctuation	36.45	25.69	14	3216	3583	29567714
Dry mouth	36.26	25.69	25	3205	21759	29549538
Pneumonia aspiration	34.47	25.69	30	3200	36707	29534590
Meningioma	32.41	25.69	10	3220	1330	29569967
Anti-platelet antibody positive	32.15	25.69	7	3223	233	29571064
Haptoglobin decreased	31.41	25.69	8	3222	528	29570769
Blood bilirubin unconjugated increased	31.08	25.69	8	3222	551	29570746
Disease recurrence	30.65	25.69	20	3210	15894	29555403
Coombs direct test positive	30.48	25.69	7	3223	298	29570999
Dependence on oxygen therapy	28.49	25.69	6	3224	170	29571127
Idiopathic intracranial hypertension	25.83	25.69	7	3223	588	29570709

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Coma	233.97	25.32	143	8071	87472	64403046
Camptocormia	149.75	25.32	29	8185	452	64490066
Somnolence	133.11	25.32	146	8068	203499	64287019
Poisoning deliberate	127.32	25.32	52	8162	13406	64477112
Hepatocellular injury	120.97	25.32	74	8140	45161	64445357
Pleurothotonus	118.52	25.32	32	8182	2270	64488248
Cholestasis	106.35	25.32	68	8146	44804	64445714
Agranulocytosis	105.95	25.32	64	8150	38165	64452353
Hyponatraemia	89.31	25.32	102	8112	148237	64342281
Fall	87.76	25.32	175	8039	416651	64073867
Cerebral artery thrombosis	80.14	25.32	20	8194	1039	64489479
Brain scan abnormal	73.32	25.32	19	8195	1149	64489369
Miosis	66.83	25.32	33	8181	13233	64477285
Toxicity to various agents	66.29	25.32	144	8070	363369	64127149
Drug interaction	63.26	25.32	141	8073	361942	64128576
Bradypnoea	63.05	25.32	24	8190	5135	64485383
Bradycardia	62.33	25.32	76	8138	118143	64372375
Altered state of consciousness	58.16	25.32	44	8170	37858	64452660
Respiratory distress	57.54	25.32	50	8164	52281	64438237
Acute kidney injury	56.28	25.32	154	8060	449086	64041432
Behaviour disorder	55.40	25.32	21	8193	4441	64486077
Thymus disorder	54.30	25.32	11	8203	218	64490300
Extrapyramidal disorder	52.25	25.32	32	8182	19520	64470998
Pneumonia aspiration	50.31	25.32	49	8165	59222	64431296
Hepatic cytolysis	48.11	25.32	27	8187	14022	64476496
Areflexia	46.15	25.32	19	8195	4988	64485530
Dry mouth	44.04	25.32	46	8168	60372	64430146
Brain death	43.30	25.32	18	8196	4843	64485675
Vertigo	43.14	25.32	45	8169	58966	64431552
Housebound	41.36	25.32	10	8204	455	64490063
Sedation complication	41.26	25.32	22	8192	10332	64480186
Gamma-glutamyltransferase increased	40.96	25.32	40	8174	48470	64442048
Ischaemic stroke	40.80	25.32	32	8182	29003	64461515
Poikiloderma	39.21	25.32	9	8205	326	64490192
Adenomatous polyposis coli	38.15	25.32	8	8206	189	64490329
Blood lactic acid	36.32	25.32	9	8205	454	64490064
Confusional state	36.11	25.32	93	8121	261051	64229467
Cutaneous lymphoma	36.09	25.32	8	8206	247	64490271
Reticulocytosis	35.63	25.32	9	8205	491	64490027
Oesophageal food impaction	33.75	25.32	8	8206	334	64490184
Wrong patient received product	33.74	25.32	14	8200	3748	64486770
Arthralgia	32.85	25.32	8	8206	442252	64048266
Morbid thoughts	32.30	25.32	9	8205	717	64489801
Lichenoid keratosis	31.92	25.32	13	8201	3321	64487197
Drug-device interaction	31.85	25.32	6	8208	80	64490438
Hemiplegia	31.84	25.32	20	8194	12748	64477770
Generalised anxiety disorder	31.15	25.32	11	8203	1904	64488614
Initial insomnia	30.91	25.32	15	8199	5789	64484729
Anti-platelet antibody positive	30.02	25.32	7	8207	272	64490246
Limbic encephalitis	28.40	25.32	8	8206	663	64489855
Oesophageal achalasia	28.18	25.32	8	8206	682	64489836
Coombs direct test positive	27.62	25.32	7	8207	387	64490131
Blood glucose fluctuation	27.59	25.32	14	8200	5941	64484577
Suicide attempt	27.10	25.32	39	8175	70968	64419550
Facial paralysis	26.85	25.32	21	8193	18945	64471573
Overdose	26.48	25.32	61	8153	159505	64331013
Persecutory delusion	25.99	25.32	12	8202	4146	64486372
Blood bilirubin unconjugated increased	25.94	25.32	8	8206	909	64489609
Headache	25.81	25.32	18	8196	529449	63961069

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N06AX03	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D000317	Adrenergic alpha-Antagonists
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D018687	Antidepressive Agents, Second-Generation
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D011619	Psychotropic Drugs
MeSH PA	D018490	Serotonin Agents
MeSH PA	D012702	Serotonin Antagonists
CHEBI has role	CHEBI:176497	geroprotectors
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:35640	adrenergic uptake inhibitors
CHEBI has role	CHEBI:35678	histamine agonists
CHEBI has role	CHEBI:35717	hypnotics
CHEBI has role	CHEBI:37890	alpha-adrenergic receptor blockaders
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:48279	serotonin antagonists
CHEBI has role	CHEBI:76779	post-proline endopeptidase inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Major depressive disorder	indication	370143000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.2	Basic
pKa2	1.03	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])	Mechanism action	Bioact source	MoA source
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	8.17		WOMBAT-PK	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	8.12		WOMBAT-PK	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	8.52		WOMBAT-PK	IUPHAR
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.40		PDSP
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Kd	7.15		WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.13		WOMBAT-PK
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	7.18		WOMBAT-PK
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	7.06		WOMBAT-PK
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		IC50	6.39		CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	7.57		WOMBAT-PK
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	5.55		CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	9.25		WOMBAT-PK
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	6.00		DRUG MATRIX
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		EC50	6.13		WOMBAT-PK
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	6.47		DRUG MATRIX
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.42		DRUG MATRIX
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.53		DRUG MATRIX
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	6.54		DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	6.64		DRUG MATRIX
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	7.53		WOMBAT-PK
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	6.99		WOMBAT-PK
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	8.42		WOMBAT-PK
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	5.03		PDSP
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		IC50	5.48		CHEMBL
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	ANTAGONIST	Ki	7.50		IUPHAR
5-hydroxytryptamine receptor 3A	Ion channel	P46098	5HT3A_HUMAN		Ki	6.21		DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	ANTAGONIST	Ki	7.40		IUPHAR
5-hydroxytryptamine receptor 1F	GPCR	P30939	5HT1F_HUMAN		Ki	8.06		WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	5.26		CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6		WOMBAT-PK
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	5.66		CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	8.32		WOMBAT-PK
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	7.18		DRUG MATRIX
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	5.33		CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	10.15		CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		Ki	9.07		CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Ki	6.08		CHEMBL
Sodium-dependent serotonin transporter	Transporter		SC6A4_RAT		IC50	5.54		CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	8.82		CHEMBL
Transporter	Transporter		Q9WTR4_RAT		Ki	7.59		CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT		Ki	7.20		CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_MOUSE	ANTAGONIST	Ki	7		IUPHAR
D(1A) dopamine receptor	GPCR		DRD1_RAT		Ki	5.85		CHEMBL
5-hydroxytryptamine receptor 2C	GPCR		5HT2C_RAT		Ki	8.85		CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		Ki	7.37		CHEMBL
D(3) dopamine receptor	GPCR		DRD3_RAT		Ki	5.82		CHEMBL
Alpha-2A adrenergic receptor	GPCR		ADA2A_BOVIN		Ki	7.77		CHEMBL
Muscarinic acetylcholine receptor M5	GPCR		ACM5_RAT		IC50	5.72		CHEMBL
5-hydroxytryptamine receptor 6	GPCR		5HT6R_RAT	ANTAGONIST	Ki	7.40		IUPHAR
Serotonin 3 (5-HT3) receptor	Ion channel		5HT3A_RAT 5HT3B_RAT		Ki	7.15		CHEMBL
Serotonin 1 (5-HT1) receptor	GPCR		5HT1A_RAT 5HT1B_RAT 5HT1D_RAT 5HT1F_RAT		Ki	6.24		CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		Ki	7.21		CHEMBL
Cerebral cortex alpha adrenergic receptor	GPCR		ADA1A_BOVIN ADA2A_BOVIN		IC50	8.22		CHEMBL
Serotonin 2 (5-HT2) receptor	GPCR		5HT2C_RAT 5HT2A_RAT 5HT2B_RAT		Ki	8.96		CHEMBL
Serotonin 3 receptor (5HT3)	Ion channel		5HT3A_MOUSE 5HT3B_MOUSE		Ki	6.60		CHEMBL
G-protein coupled receptor	GPCR		Q9NG02_APIME		IC50	4.14		CHEMBL
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_MOUSE	ANTAGONIST	Ki	8.30		IUPHAR

External reference:

ID	Source
D01358	KEGG_DRUG
21535-47-7	SECONDARY_CAS_RN
4027429	VANDF
C0025912	UMLSCUI
CHEBI:51137	CHEBI
CHEMBL6437	ChEMBL_ID
CHEMBL544428	ChEMBL_ID
DB06148	DRUGBANK_ID
D008803	MESH_DESCRIPTOR_UI
4184	PUBCHEM_CID
135	IUPHAR_LIGAND_ID
2543	INN_ID
250PJI13LM	UNII
203127	RXNORM
18113	MMSL
004006	NDDF
004007	NDDF
387565003	SNOMEDCT_US
395795008	SNOMEDCT_US
96200003	SNOMEDCT_US

Pharmaceutical products:

None