Dimenhydrinate

Summary

Dimenhydrinate (CHEMBL1200406) is an approved small molecule (ATC R06AA11); indicated across 3 conditions including allergic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R06AA11
• Indications: 3 conditions
• Clinical trials: 9
• Chemistry: 470 Da · C24H28ClN5O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1200406
Name	Dimenhydrinate
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	10660
ATC	R06AA11
Molecular formula	C24H28ClN5O3
Molecular weight	470
InChIKey	NFLLKCVHYJRNRH-UHFFFAOYSA-N

SMILES: CN1C2=C(C(=O)N(C1=O)C)NC(=N2)Cl.CN(C)CCOC(C1=CC=CC=C1)C2=CC=CC=C2

IUPAC name: 2-benzhydryloxy-N,N-dimethylethanamine;8-chloro-1,3-dimethyl-7H-purine-2,6-dione

Also known as: Antemin, Dimenhidrinato, Dimenhydrinate, Dramamine, NSC-117855, Vertigo-vomex s, SID11112942, SID17389041, SID26747407, DIMENHYDRINATE, SID144207521, Diphenhydramine; Dimenhydrinate

Patent coverage: 8,754 distinct patent families (26,424 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 21 (assay-derived). Sample: Prelamin-A/C, Inositol monophosphatase 1, Muscarinic acetylcholine receptor M4, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Alpha-2B adrenergic receptor, Muscarinic acetylcholine receptor M5, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter.

Bioactivity

ChEMBL activities: 36 potent at pChembl ≥ 5 of 38 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
LMNA	9	Potency	1	nM	CHEMBL_ACT_3624272
HRH1	7.43	Ki	37	nM	CHEMBL_ACT_7707126
CHRM4	7.1	Ki	80	nM	CHEMBL_ACT_7707160
CHRM3	7.02	Ki	95	nM	CHEMBL_ACT_7707158
CHRM1	6.96	Ki	109	nM	CHEMBL_ACT_7707154
CHRM2	6.79	Ki	164	nM	CHEMBL_ACT_7707156
HTR2A	6.7	Ki	198	nM	CHEMBL_ACT_7709337
CHRM5	6.64	Ki	227	nM	CHEMBL_ACT_7707162
HRH1	6.5	IC50	319	nM	CHEMBL_ACT_7707125
CHRM5	6.5	IC50	316	nM	CHEMBL_ACT_7707161
HTR2C	6.48	Ki	332	nM	CHEMBL_ACT_7709341
CHRM1	6.35	IC50	451	nM	CHEMBL_ACT_7707153
CHRM3	6.35	IC50	447	nM	CHEMBL_ACT_7707157
CHRM2	6.34	IC50	461	nM	CHEMBL_ACT_7707155
SIGMAR1	6.31	Ki	487	nM	CHEMBL_ACT_7709351
CHRM4	6.24	IC50	570	nM	CHEMBL_ACT_7707159
HTR2C	6.2	IC50	634	nM	CHEMBL_ACT_7709340
HTR2A	6.16	IC50	693	nM	CHEMBL_ACT_7709336
HTR2B	5.96	Ki	1097	nM	CHEMBL_ACT_7709339
SIGMAR1	5.94	IC50	1158	nM	CHEMBL_ACT_7709350
ADRA1D	5.85	Ki	1423	nM	CHEMBL_ACT_7704994
CYP2D6	5.82	IC50	1509	nM	CHEMBL_ACT_7707085
ADRA2A	5.79	Ki	1617	nM	CHEMBL_ACT_7704996
HTR2B	5.76	IC50	1724	nM	CHEMBL_ACT_7709338
SLC6A3	5.75	Ki	1784	nM	CHEMBL_ACT_7707100
SLC6A2	5.7	Ki	2020	nM	CHEMBL_ACT_7705008
SLC6A2	5.69	IC50	2037	nM	CHEMBL_ACT_7705007
SLC6A3	5.65	IC50	2245	nM	CHEMBL_ACT_7707099
ADRA2B	5.6	Ki	2491	nM	CHEMBL_ACT_7704998
ADRA1D	5.54	IC50	2894	nM	CHEMBL_ACT_7704993

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
allergic disease	4	MONDO:0005271	MONDO:0005271

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE4	3
Not specified	3
PHASE3	2
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00124787	PHASE4	COMPLETED	A Trial Comparing the Effect of Oral Dimenhydrinate Versus Placebo in Children With Gastroenteritis
NCT01890538	PHASE4	COMPLETED	Comparison of Efficacy Between Piracetam and Dimenhydrinate in Patients With Peripheral Vertigo
NCT02253524	PHASE4	COMPLETED	Comparison of Efficacy Dimenhydrinate and Metoclopramide in the Treatment of Nausea Due to Vertigo
NCT02112578	PHASE3	COMPLETED	Non Inferiority of Meclin® (Meclizine Chlorhydrate) Versus Dramin® (Dimenhydrinate) in Control of Acute Vertigo Symptoms From Peripheral Origin
NCT04606264	PHASE3	COMPLETED	Recommendations of Enhanced Recovery Interventions for Patient’s Clinical Team and Collection of Associated Data
NCT01543945	PHASE2	COMPLETED	Prevention Post Operative Nausea Vomiting in Ambulatory Gynecologic Laparoscopy
NCT00791960	Not specified	COMPLETED	Prophylactic Dimenhydrinate for Intraoperative Nausea and Vomiting
NCT05590936	Not specified	COMPLETED	Dimenydrinate vs Ondansetron for PONV (DONV)
NCT06395064	Not specified	UNKNOWN	The Effect of Dimenhydrinate on Postoperative Nausea and Vomiting After Abdominal Hysterectomy: Randomized-controlled Trial

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).