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
serotonin receptor antagonists (mostly 5-HT2)	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
Coma	199.77	31.27	102	5462	64262	63419196
Camptocormia	173.41	31.27	29	5535	280	63483178
Pleurothotonus	153.06	31.27	33	5531	1316	63482142
Hyponatraemia	149.82	31.27	103	5461	111797	63371661
Toxicity to various agents	123.85	31.27	129	5435	247121	63236337
Somnolence	109.27	31.27	104	5460	178581	63304877
Hepatocellular injury	104.44	31.27	50	5514	27331	63456127
Fall	102.11	31.27	147	5417	392187	63091271
Agranulocytosis	99.23	31.27	47	5517	25087	63458371
Cholestasis	98.04	31.27	49	5515	29385	63454073
Drug interaction	92.79	31.27	107	5457	229024	63254434
Poisoning deliberate	91.12	31.27	35	5529	11183	63472275
Bradypnoea	76.33	31.27	23	5541	3527	63479931
Thymus disorder	73.88	31.27	14	5550	287	63483171
Bradycardia	69.79	31.27	55	5509	73172	63410286
Altered state of consciousness	63.97	31.27	35	5529	25195	63458263
Acute kidney injury	62.95	31.27	95	5469	263320	63220138
Miosis	59.91	31.27	23	5541	7330	63476128
Drug reaction with eosinophilia and systemic symptoms	59.46	31.27	37	5527	33799	63449659
Drug abuse	55.56	31.27	48	5516	72470	63410988
Sedation complication	54.99	31.27	26	5538	13796	63469662
Blood lactic acid	52.82	31.27	9	5555	98	63483360
Brain death	52.02	31.27	17	5547	3393	63480065
Housebound	51.93	31.27	10	5554	224	63483234
Extrapyramidal disorder	46.83	31.27	23	5541	13261	63470197
Vertigo	46.60	31.27	40	5524	59847	63423611
Oesophageal food impaction	46.46	31.27	9	5555	208	63483250
Confusional state	45.10	31.27	77	5487	236303	63247155
Cutaneous lymphoma	42.50	31.27	8	5556	158	63483300
Morbid thoughts	42.17	31.27	10	5554	613	63482845
Oesophageal achalasia	39.23	31.27	9	5555	477	63482981
Rash	37.96	31.27	3	5561	560868	62922590
Wrong patient received product	37.74	31.27	12	5552	2195	63481263
Limbic encephalitis	36.99	31.27	8	5556	323	63483135
Disturbance in attention	34.88	31.27	28	5536	38161	63445297
Hepatitis	33.87	31.27	28	5536	39760	63443698
Drug-device interaction	33.43	31.27	6	5558	90	63483368
Behaviour disorder	33.37	31.27	12	5552	3187	63480271
Foetal alcohol syndrome	32.28	31.27	5	5559	28	63483430
Herbal interaction	31.99	31.27	6	5558	116	63483342

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	100.10	26.17	22	3837	758	34952314
Coma	89.08	26.17	58	3801	45620	34907452
Brain scan abnormal	86.69	26.17	20	3839	860	34952212
Somnolence	62.87	26.17	69	3790	111047	34842025
Areflexia	62.20	26.17	20	3839	3011	34950061
Ischaemic stroke	58.62	26.17	32	3827	18218	34934854
Hepatocellular injury	52.77	26.17	32	3827	22179	34930893
Respiratory distress	49.98	26.17	37	3822	35628	34917444
Hemiplegia	45.97	26.17	20	3839	6952	34946120
Poikiloderma	45.88	26.17	9	3850	175	34952897
Cholestasis	44.73	26.17	31	3828	26917	34926155
Reticulocytosis	42.11	26.17	9	3850	271	34952801
Adenomatous polyposis coli	40.95	26.17	8	3851	152	34952920
Facial paralysis	40.61	26.17	21	3838	10713	34942359
Pneumonia aspiration	38.56	26.17	34	3825	41869	34911203
Initial insomnia	38.22	26.17	14	3845	3110	34949962
Lichenoid keratosis	37.34	26.17	13	3846	2495	34950577
Wrong patient received product	36.62	26.17	13	3846	2641	34950431
Hepatic cytolysis	34.71	26.17	21	3838	14475	34938597
Blood glucose fluctuation	34.71	26.17	14	3845	4030	34949042
Poisoning deliberate	34.51	26.17	17	3842	7827	34945245
Agranulocytosis	34.00	26.17	25	3834	23796	34929276
Meningioma	31.62	26.17	10	3849	1426	34951646
Anti-platelet antibody positive	31.46	26.17	7	3852	255	34952817
Haptoglobin decreased	30.95	26.17	8	3851	554	34952518
Benign soft tissue neoplasm	30.61	26.17	6	3853	116	34952956
Restlessness	30.32	26.17	24	3835	25458	34927614
Blood bilirubin unconjugated increased	30.17	26.17	8	3851	612	34952460
Reduced facial expression	29.96	26.17	9	3850	1082	34951990
Coombs direct test positive	29.79	26.17	7	3852	326	34952746
Dry mouth	28.79	26.17	25	3834	30140	34922932
Dissociative disorder	27.41	26.17	7	3852	462	34952610
Cholangitis	27.23	26.17	15	3844	8674	34944398
Withdrawal syndrome	27.16	26.17	17	3842	12438	34940634
Dependence on oxygen therapy	27.06	26.17	6	3853	215	34952857

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	265.84	24.77	159	9295	100490	79634444
Somnolence	167.63	24.77	172	9282	238809	79496125
Camptocormia	151.40	24.77	29	9425	459	79734475
Hepatocellular injury	138.07	24.77	80	9374	47513	79687421
Poisoning deliberate	130.08	24.77	57	9397	18771	79716163
Cholestasis	128.79	24.77	79	9375	52030	79682904
Agranulocytosis	118.30	24.77	71	9383	44959	79689975
Pleurothotonus	117.97	24.77	32	9422	2484	79732450
Hyponatraemia	112.03	24.77	121	9333	177727	79557207
Fall	97.24	24.77	192	9262	487437	79247497
Drug interaction	90.71	24.77	170	9284	415013	79319921
Toxicity to various agents	82.76	24.77	165	9289	421375	79313559
Cerebral artery thrombosis	80.61	24.77	20	9434	1091	79733843
Brain scan abnormal	73.80	24.77	19	9435	1204	79733730
Miosis	72.37	24.77	36	9418	15753	79719181
Drug reaction with eosinophilia and systemic symptoms	71.61	24.77	60	9394	64184	79670750
Thymus disorder	69.84	24.77	14	9440	283	79734651
Wrong patient received product	67.31	24.77	24	9430	4594	79730340
Acute kidney injury	64.84	24.77	170	9284	519234	79215700
Altered state of consciousness	64.02	24.77	48	9406	43774	79691160
Ischaemic stroke	63.91	24.77	43	9411	33088	79701846
Respiratory distress	61.96	24.77	53	9401	58286	79676648
Bradycardia	61.49	24.77	78	9376	135479	79599455
Bradypnoea	60.99	24.77	24	9430	6028	79728906
Confusional state	57.00	24.77	120	9334	317877	79417057
Hepatic cytolysis	56.63	24.77	37	9417	27114	79707820
Drug abuse	56.17	24.77	82	9372	162609	79572325
Pneumonia aspiration	55.67	24.77	53	9401	66914	79668020
Extrapyramidal disorder	49.99	24.77	32	9422	22647	79712287
Behaviour disorder	49.79	24.77	21	9433	6292	79728642
Sedation complication	47.16	24.77	27	9427	15642	79719292
Areflexia	45.63	24.77	19	9435	5515	79729419
Vertigo	45.15	24.77	48	9406	69034	79665900
Suicide attempt	44.54	24.77	52	9402	82880	79652054
Brain death	41.84	24.77	18	9436	5659	79729275
Housebound	41.84	24.77	10	9444	466	79734468
Gamma-glutamyltransferase increased	39.33	24.77	40	9414	54640	79680294
Arthralgia	38.83	24.77	10	9444	571793	79163141
Oesophageal food impaction	38.38	24.77	9	9445	386	79734548
Poikiloderma	38.20	24.77	9	9445	394	79734540
Blood lactic acid	36.96	24.77	9	9445	454	79734480
Adenomatous polyposis coli	36.82	24.77	8	9446	242	79734692
Morbid thoughts	36.66	24.77	10	9444	792	79734142
Cutaneous lymphoma	36.26	24.77	8	9446	260	79734674
Reticulocytosis	36.11	24.77	9	9445	500	79734434
Initial insomnia	35.32	24.77	17	9437	6921	79728013
Suicidal ideation	34.70	24.77	44	9410	76296	79658638
Disturbance in attention	34.44	24.77	36	9418	50765	79684169
Dry mouth	32.74	24.77	46	9408	87973	79646961
Oesophageal achalasia	32.14	24.77	9	9445	785	79734149
Drug-device interaction	31.87	24.77	6	9448	86	79734848
Withdrawal syndrome	31.81	24.77	26	9428	26828	79708106
Hepatitis	31.69	24.77	36	9418	55691	79679243
Headache	30.59	24.77	20	9434	653752	79081182
Generalised anxiety disorder	30.44	24.77	11	9443	2186	79732748
Lichenoid keratosis	30.35	24.77	13	9441	4044	79730890
Hemiplegia	30.27	24.77	20	9434	14919	79720015
Benign soft tissue neoplasm	29.71	24.77	6	9448	126	79734808
Anti-platelet antibody positive	29.44	24.77	7	9447	319	79734615
Rash	29.43	24.77	16	9438	578342	79156592
Hallucination, visual	29.29	24.77	27	9427	32702	79702232
Pain in extremity	27.51	24.77	5	9449	364533	79370401
Coombs direct test positive	27.49	24.77	7	9447	424	79734510
Single umbilical artery	27.45	24.77	4	9450	9	79734925
Dissociative disorder	27.37	24.77	8	9446	813	79734121
Rhabdomyolysis	27.24	24.77	46	9408	103085	79631849
Blood glucose fluctuation	27.01	24.77	14	9440	6668	79728266
Limbic encephalitis	26.87	24.77	8	9446	867	79734067
Disorientation	26.67	24.77	35	9419	62741	79672193
Facial paralysis	26.23	24.77	21	9433	21051	79713883
Overdose	25.68	24.77	63	9391	184143	79550791
Blood bilirubin unconjugated increased	25.53	24.77	8	9446	1029	79733905
Exposure via transplant	25.00	24.77	4	9450	20	79734914
Rash maculo-papular	24.97	24.77	32	9422	56046	79678888
Persecutory delusion	24.90	24.77	12	9442	4897	79730037

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