betahistine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
346 5638-76-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • betahistine dihydrochloride
  • betahistine hydrochloride
  • betahistine methanesulfonate
  • betahistine dihydrobromide
  • betahistine
  • beta-histine
  • betahistine mesilate
  • merislon
  • betahistine mesylate
A histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.
  • Molecular weight: 136.20
  • Formula: C8H12N2
  • CLOGP: 0.08
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 24.92
  • ALOGS: -0.44
  • ROTB: 3

Drug dosage:

DoseUnitRoute
24 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 38 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 100 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -1.963 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.594 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 5.754 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 1.968 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 92.930 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 71.620 % High 1
herg hERG pIC50 3.852 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.552 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.614 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 90.640 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT2,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IRAK4,ITK,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK12,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 41
kinase-selectivity-class AXL,BRAF,CAMK2D,SIK2,STK33 5
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.570 High 1
mh-clint Mouse hepatocyte intrinsic clearance 6.823 High 1
mppb Mouse plasma protein binding (% unbound) 96.020 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.673 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 89.050 % High 1
rh-clint Rat hepatocyte intrinsic clearance 3.228 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 92.770 % High 1
rppb Rat plasma protein binding (% unbound) 92.590 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 788.860 uM High 1

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Parkinsonism 174.18 17.47 71 14922 13994 90599460
Hyponatraemia 156.12 17.47 148 14845 133390 90480064
Dementia 135.37 17.47 70 14923 23791 90589663
Blood cholesterol decreased 120.40 17.47 33 14960 1898 90611556
Atrioventricular block first degree 119.35 17.47 47 14946 8464 90604990
Peripheral circulatory failure 112.13 17.47 30 14963 1574 90611880
Multiple drug therapy 109.98 17.47 42 14951 6967 90606487
Hypoglycaemia 108.57 17.47 91 14902 69757 90543697
Fall 99.61 17.47 235 14758 481575 90131879
Dizziness 99.45 17.47 266 14727 589018 90024436
Melaena 98.44 17.47 65 14928 34732 90578722
Neuroglycopenia 97.94 17.47 25 14968 1090 90612364
Syncope 97.71 17.47 115 14878 132548 90480906
Pituitary tumour benign 94.86 17.47 28 14965 2104 90611350
Drug dependence 93.34 17.47 59 14934 29268 90584186
Gastric polyps 91.69 17.47 33 14960 4639 90608815
Cognitive disorder 90.85 17.47 82 14911 69325 90544129
Urinary retention 88.98 17.47 63 14930 37681 90575773
Initial insomnia 79.04 17.47 36 14957 9274 90604180
Bradykinesia 76.35 17.47 32 14961 6756 90606698
Stupor 75.90 17.47 30 14963 5452 90608002
Enthesopathy 75.56 17.47 35 14958 9369 90604085
Lichen planopilaris 70.71 17.47 14 14979 186 90613268
Hyperkalaemia 70.16 17.47 69 14924 64895 90548559
Diabetes mellitus inadequate control 68.13 17.47 41 14952 18643 90594811
Polyp 66.29 17.47 30 14963 7614 90605840
Palpitations 65.57 17.47 96 14897 136632 90476822
Vertigo 64.21 17.47 68 14925 69743 90543711
Vitamin B12 decreased 59.61 17.47 25 14968 5285 90608169
Blood creatine increased 59.33 17.47 27 14966 6940 90606514
Tenosynovitis 58.43 17.47 34 14959 14533 90598921
Dysuria 56.42 17.47 49 14944 39352 90574102
Hyperprolactinaemia 55.75 17.47 24 14969 5409 90608045
Hypotension 52.79 17.47 145 14848 325252 90288202
Osteoporosis 52.51 17.47 72 14921 96459 90516995
Hypotonia 52.10 17.47 29 14964 11397 90602057
Eye pruritus 51.77 17.47 41 14952 28986 90584468
Muscle rigidity 51.14 17.47 31 14962 14278 90599176
Secondary adrenocortical insufficiency 47.85 17.47 17 14976 2301 90611153
Neuropathy, ataxia, retinitis pigmentosa syndrome 46.10 17.47 8 14985 48 90613406
Motor dysfunction 45.08 17.47 32 14961 19198 90594256
Oral pain 43.50 17.47 39 14954 32644 90580810
Hiatus hernia 43.47 17.47 35 14958 25326 90588128
Synovitis 42.94 17.47 3 14990 329749 90283705
Confabulation 42.47 17.47 10 14983 310 90613144
Swelling 42.07 17.47 9 14984 419049 90194405
Blood urea increased 41.89 17.47 37 14956 30376 90583078
Sinus bradycardia 41.57 17.47 29 14964 16923 90596531
Dopamine transporter scintigraphy abnormal 41.00 17.47 8 14985 98 90613356
Poor peripheral circulation 38.75 17.47 17 14976 4008 90609446
Metastases to fallopian tube 37.94 17.47 7 14986 62 90613392
Hypomagnesaemia 36.93 17.47 37 14956 35551 90577903
Micturition disorder 36.54 17.47 15 14978 3005 90610449
Arthropathy 36.48 17.47 8 14985 366234 90247220
Hyperreflexia 36.22 17.47 19 14974 6638 90606816
Wound 36.08 17.47 4 14989 302976 90310478
Infusion related reaction 36.08 17.47 12 14981 416768 90196686
Constipation 35.96 17.47 115 14878 280280 90333174
Atrial fibrillation 35.21 17.47 72 14921 133539 90479915
Pain 35.18 17.47 70 14923 996271 89617183
Rash 33.50 17.47 50 14943 796050 89817404
Lacrimation increased 33.49 17.47 31 14962 27031 90586423
Drug interaction 33.30 17.47 111 14882 276342 90337112
Sinusitis 33.16 17.47 8 14985 343080 90270374
Perseveration 33.12 17.47 8 14985 277 90613177
Therapy partial responder 32.74 17.47 28 14965 22015 90591439
Blood pressure decreased 32.19 17.47 50 14943 74845 90538609
Cerebellar ataxia 31.99 17.47 10 14983 912 90612542
Haemorrhoids 31.91 17.47 30 14963 26672 90586782
Hepatic enzyme increased 31.90 17.47 10 14983 360726 90252728
Scleritis 31.61 17.47 16 14977 5192 90608262
Labelled drug-drug interaction issue 30.01 17.47 12 14981 2246 90611208
Apraxia 29.99 17.47 12 14981 2250 90611204
Serum serotonin increased 29.79 17.47 7 14986 215 90613239
Drug intolerance 29.30 17.47 19 14974 447572 90165882
Metastases to bladder 29.25 17.47 7 14986 233 90613221
Blister 28.81 17.47 4 14989 254994 90358460
Endometrial cancer stage I 28.64 17.47 7 14986 255 90613199
Blood potassium increased 28.09 17.47 25 14968 20724 90592730
Orthostatic hypotension 27.07 17.47 34 14959 41793 90571661
Maternal exposure during pregnancy 26.85 17.47 13 14980 360050 90253404
Crystal arthropathy 26.60 17.47 7 14986 344 90613110
Depressed mood 26.60 17.47 37 14956 50185 90563269
Weight increased 25.68 17.47 19 14974 417908 90195546
Carcinoid tumour 25.25 17.47 7 14986 420 90613034
Peptic ulcer 25.24 17.47 14 14979 5461 90607993
Hyperglycaemia 24.71 17.47 36 14957 50934 90562520
Disorientation 24.11 17.47 33 14960 44081 90569373
Loss of control of legs 23.87 17.47 9 14984 1441 90612013
Metastases to ovary 23.79 17.47 7 14986 520 90612934
Joint swelling 23.78 17.47 29 14964 503271 90110183
Dropped head syndrome 23.56 17.47 6 14987 259 90613195
Serotonin syndrome 23.26 17.47 30 14963 37857 90575597
Oedema 22.96 17.47 3 14990 200292 90413162
Lethargy 22.85 17.47 39 14954 63100 90550354
Sputum discoloured 22.64 17.47 22 14971 20369 90593085
Injury 22.52 17.47 3 14990 197346 90416108
Pharyngeal mass 22.36 17.47 6 14987 318 90613136
Hypomenorrhoea 22.30 17.47 7 14986 647 90612807
Cardiospasm 22.13 17.47 11 14982 3435 90610019
Palmoplantar keratoderma 21.95 17.47 11 14982 3496 90609958
Death 21.88 17.47 26 14967 456525 90156929
Discomfort 21.87 17.47 9 14984 274326 90339128
Autoimmune thyroiditis 21.66 17.47 13 14980 5880 90607574
Subcutaneous haematoma 21.59 17.47 9 14984 1874 90611580
Basal ganglia haemorrhage 21.26 17.47 7 14986 754 90612700
Urine output decreased 20.77 17.47 17 14976 12586 90600868
Product administration error 19.57 17.47 23 14970 26400 90587054
Endometrial hyperplasia 19.53 17.47 7 14986 972 90612482
Sleep terror 19.45 17.47 11 14982 4453 90609001
Medication error 19.27 17.47 43 14950 84609 90528845
Pruritus genital 19.24 17.47 11 14982 4547 90608907
Nystagmus 19.22 17.47 13 14980 7214 90606240
Vision blurred 18.68 17.47 50 14943 110243 90503211
Brain injury 18.42 17.47 13 14980 7725 90605729
Lip swelling 18.32 17.47 27 14966 38583 90574871
Pericarditis 18.31 17.47 11 14982 270140 90343314
Carotid artery occlusion 18.30 17.47 12 14981 6330 90607124
Renal failure 17.93 17.47 55 14938 130952 90482502
Sedation 17.75 17.47 30 14963 48141 90565313

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Soft tissue mass 139.78 22.55 30 4403 982 42615920
Oesophageal perforation 139.36 22.55 31 4402 1202 42615700
Multimorbidity 136.37 22.55 29 4404 908 42615994
Superinfection 107.88 22.55 30 4403 2921 42613981
Transplant failure 102.83 22.55 31 4402 4013 42612889
Immunosuppressant drug level increased 94.24 22.55 34 4399 7697 42609205
Oesophageal carcinoma 93.85 22.55 36 4397 9660 42607242
Lung consolidation 83.77 22.55 30 4403 6647 42610255
Inflammatory marker increased 83.42 22.55 30 4403 6726 42610176
Rales 68.21 22.55 30 4403 11370 42605532
Myocardial ischaemia 66.99 22.55 34 4399 17728 42599174
Cardiomegaly 57.19 22.55 30 4403 16736 42600166
Labelled drug-drug interaction medication error 53.48 22.55 28 4405 15554 42601348
Anticoagulation drug level above therapeutic 49.65 22.55 16 4417 2574 42614328
Hypoglycaemia 48.43 22.55 44 4389 59810 42557092
Lower respiratory tract infection 47.17 22.55 37 4396 41169 42575733
Drug level increased 40.03 22.55 28 4405 26172 42590730
Hepatitis acute 36.23 22.55 18 4415 8957 42607945
Haemoptysis 31.69 22.55 31 4402 46136 42570766
Product prescribing error 31.06 22.55 24 4409 26088 42590814
Vertigo 29.24 22.55 26 4407 34321 42582581
Productive cough 28.82 22.55 31 4402 51536 42565366
Loss of proprioception 28.08 22.55 7 4426 445 42616457
Dysphagia 27.82 22.55 36 4397 72683 42544219
Intercepted medication error 27.20 22.55 7 4426 506 42616396
Vascular dementia 26.76 22.55 7 4426 539 42616363
Ascites 26.42 22.55 31 4402 56647 42560255
Malaise 26.42 22.55 64 4369 212092 42404810
Renal impairment 24.10 22.55 42 4391 110186 42506716
Atrial thrombosis 23.37 22.55 9 4424 2435 42614467

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hypoglycaemia 132.19 16.37 130 19175 115974 110454020
Parkinsonism 130.83 16.37 68 19237 22119 110547875
Hyponatraemia 130.77 16.37 175 19130 217478 110352516
Dizziness 114.74 16.37 323 18982 697870 109872124
Oesophageal perforation 109.53 16.37 30 19275 1629 110568365
Blood cholesterol decreased 107.51 16.37 33 19272 2683 110567311
Soft tissue mass 107.17 16.37 29 19276 1504 110568490
Peripheral circulatory failure 106.79 16.37 30 19275 1789 110568205
Dementia 103.28 16.37 66 19239 31607 110538387
Multimorbidity 102.74 16.37 28 19277 1492 110568502
Multiple drug therapy 102.32 16.37 42 19263 7972 110562022
Fall 101.83 16.37 282 19023 603200 109966794
Atrioventricular block first degree 96.70 16.37 48 19257 14177 110555817
Neuroglycopenia 96.35 16.37 25 19280 1101 110568893
Pituitary tumour benign 89.45 16.37 29 19276 2818 110567176
Vertigo 87.38 16.37 91 19214 86779 110483215
Gastric polyps 84.58 16.37 33 19272 5490 110564504
Syncope 82.84 16.37 136 19169 202400 110367594
Transplant failure 73.54 16.37 30 19275 5605 110564389
Initial insomnia 73.42 16.37 36 19269 10353 110559641
Drug dependence 72.29 16.37 64 19241 49956 110520038
Lichen planopilaris 72.23 16.37 14 19291 156 110569838
Cognitive disorder 71.19 16.37 82 19223 87429 110482565
Urinary retention 70.07 16.37 73 19232 69610 110500384
Superinfection 69.50 16.37 29 19276 5734 110564260
Palpitations 67.92 16.37 109 19196 159103 110410891
Oesophageal carcinoma 67.01 16.37 35 19270 11489 110558505
Stupor 65.56 16.37 31 19274 8234 110561760
Vitamin B12 decreased 61.88 16.37 26 19279 5231 110564763
Immunosuppressant drug level increased 60.82 16.37 33 19272 11691 110558303
Bradykinesia 60.56 16.37 32 19273 10756 110559238
Enthesopathy 58.90 16.37 33 19272 12445 110557549
Melaena 56.88 16.37 65 19240 68692 110501302
Polyp 54.31 16.37 29 19276 9951 110560043
Diabetes mellitus inadequate control 53.09 16.37 43 19262 29732 110540262
Lung consolidation 52.99 16.37 29 19276 10447 110559547
Hyperkalaemia 52.56 16.37 89 19216 135707 110434287
Osteoporosis 52.13 16.37 70 19235 87082 110482912
Inflammatory marker increased 51.80 16.37 32 19273 14437 110555557
Hyperprolactinaemia 50.13 16.37 24 19281 6551 110563443
Tenosynovitis 48.34 16.37 32 19273 16251 110553743
Eye pruritus 47.48 16.37 42 19263 32733 110537261
Neuropathy, ataxia, retinitis pigmentosa syndrome 45.67 16.37 8 19297 48 110569946
Blood creatine increased 45.15 16.37 27 19278 11494 110558500
Hypotonia 42.10 16.37 29 19276 15716 110554278
Dysuria 41.68 16.37 52 19253 60179 110509815
Muscle rigidity 41.36 16.37 34 19271 23997 110545997
Death 41.04 16.37 37 19268 698832 109871162
Constipation 40.61 16.37 146 19159 357640 110212354
Cardiomegaly 39.57 16.37 36 19269 29094 110540900
Hiatus hernia 39.24 16.37 35 19270 27571 110542423
Metastases to fallopian tube 37.67 16.37 7 19298 61 110569933
Sinus bradycardia 37.27 16.37 35 19270 29448 110540546
Confabulation 37.09 16.37 10 19295 511 110569483
Motor dysfunction 36.80 16.37 32 19273 24374 110545620
Secondary adrenocortical insufficiency 36.30 16.37 17 19288 4417 110565577
Myocardial ischaemia 36.29 16.37 33 19272 26651 110543343
Lacrimation increased 35.82 16.37 35 19270 30915 110539079
Hypomagnesaemia 35.35 16.37 48 19257 60322 110509672
Drug interaction 34.89 16.37 176 19129 500007 110069987
Oral pain 33.70 16.37 37 19268 37407 110532587
Rales 32.48 16.37 30 19275 24709 110545285
Endometrial cancer stage I 30.39 16.37 7 19298 186 110569808
Labelled drug-drug interaction medication error 29.99 16.37 31 19274 29271 110540723
Anticoagulation drug level above therapeutic 29.63 16.37 15 19290 4615 110565379
Perseveration 29.48 16.37 8 19297 419 110569575
Arthropathy 29.45 16.37 7 19298 287515 110282479
Micturition disorder 29.42 16.37 15 19290 4683 110565311
Hyperreflexia 29.03 16.37 19 19286 9466 110560528
Crystal arthropathy 28.21 16.37 7 19298 257 110569737
Orthostatic hypotension 27.74 16.37 45 19260 66204 110503790
Vascular dementia 27.31 16.37 9 19296 920 110569074
Sinusitis 27.09 16.37 9 19296 296679 110273315
Hypotension 27.02 16.37 170 19135 523679 110046315
Malaise 26.97 16.37 205 19100 671614 109898380
Blister 26.55 16.37 4 19301 227372 110342622
Metastases to bladder 26.39 16.37 7 19298 336 110569658
Serum serotonin increased 25.64 16.37 7 19298 375 110569619
Hepatic enzyme increased 25.58 16.37 12 19293 320880 110249114
Metastases to ovary 25.33 16.37 7 19298 393 110569601
Blood urea increased 25.31 16.37 39 19266 54918 110515076
Disease progression 24.87 16.37 6 19299 244028 110325966
Apraxia 24.22 16.37 12 19293 3528 110566466
Hypomenorrhoea 23.96 16.37 7 19298 480 110569514
Infusion related reaction 23.78 16.37 19 19286 381143 110188851
Blood pressure decreased 23.62 16.37 58 19247 115033 110454961
Cerebellar ataxia 23.49 16.37 10 19295 2078 110567916
Haemorrhoids 23.41 16.37 30 19275 35642 110534352
Loss of control of legs 23.28 16.37 10 19295 2122 110567872
Drug intolerance 23.26 16.37 22 19283 406490 110163504
Carcinoid tumour 22.58 16.37 7 19298 588 110569406
Labelled drug-drug interaction issue 22.55 16.37 12 19293 4089 110565905
Autoimmune thyroiditis 22.45 16.37 14 19291 6420 110563574
Lethargy 22.30 16.37 50 19255 93526 110476468
Oedema 21.72 16.37 5 19300 209971 110360023
Lentigo maligna 21.64 16.37 7 19298 675 110569319
Lactic acidosis 21.46 16.37 49 19256 92762 110477232
Endometrial hyperplasia 21.44 16.37 7 19298 695 110569299
Femur fracture 21.10 16.37 32 19273 44437 110525557
Pharyngeal mass 21.10 16.37 6 19299 374 110569620
Depressed mood 21.10 16.37 38 19267 60771 110509223
Injury 20.96 16.37 3 19302 177262 110392732
Off label use 20.91 16.37 165 19140 1500020 109069974
Weight increased 20.38 16.37 26 19279 419618 110150376
Peptic ulcer 20.29 16.37 14 19291 7605 110562389
Pain 20.16 16.37 92 19213 954863 109615131
Loss of proprioception 19.63 16.37 7 19298 907 110569087
Vestibular neuronitis 19.34 16.37 7 19298 946 110569048
Sputum discoloured 19.13 16.37 24 19281 27921 110542073
Product prescribing error 19.00 16.37 33 19272 51298 110518696
Joint swelling 18.97 16.37 30 19275 442815 110127179
Dropped head syndrome 18.93 16.37 6 19299 542 110569452
Irritable bowel syndrome 18.91 16.37 3 19302 164212 110405782
Maternal exposure during pregnancy 18.15 16.37 11 19294 254872 110315122
Renal impairment 18.13 16.37 73 19232 188372 110381622
Completed suicide 17.91 16.37 10 19295 242371 110327623
Psoriatic arthropathy 17.90 16.37 6 19299 196755 110373239
Calcium deficiency 17.88 16.37 7 19298 1175 110568819
Therapy non-responder 17.83 16.37 3 19302 157304 110412690
Cardiospasm 17.82 16.37 11 19294 4956 110565038
Vision blurred 17.56 16.37 56 19249 128966 110441028
Blood potassium increased 17.32 16.37 25 19280 33224 110536770
Subcutaneous haematoma 17.02 16.37 9 19296 3027 110566967
Palmoplantar keratoderma 17.00 16.37 11 19294 5376 110564618
Drug level increased 16.78 16.37 30 19275 47689 110522305

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07CA01 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
ANTIVERTIGO PREPARATIONS
Antivertigo preparations
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents
MeSH PA D017442 Histamine Agonists
MeSH PA D018377 Neurotransmitter Agents
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:71173 H<small><sub>1</sub></small>-receptor agonist
CHEBI has role CHEBI:74518 anti-obesity agent
CHEBI has role CHEBI:35469 antidepressant

Related Drugs by ATC class:

N07CA Antivertigo preparations 3 drugs
acetylleucinecinnarizineflunarizine

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

DiseaseRelationSNOMED_IDDOID
Ménière's disease indication 13445001 DOID:9849




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.53 Basic
pKa2 3.77 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Histamine H3 receptor GPCR INVERSE AGONIST EC50 9.52 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Histamine H3 receptor GPCR Ki 5.69 CHEMBL

External reference:

IDSource
4027336 VUID
N0000179397 NUI
D01592 KEGG_DRUG
5579-84-0 SECONDARY_CAS_RN
1511 RXNORM
C0005301 UMLSCUI
CHEBI:35677 CHEBI
CHEMBL4298035 ChEMBL_ID
CHEMBL24441 ChEMBL_ID
2366 PUBCHEM_CID
DB06698 DRUGBANK_ID
CHEMBL1446813 ChEMBL_ID
D001621 MESH_DESCRIPTOR_UI
1502 INN_ID
11937 IUPHAR_LIGAND_ID
54856-23-4 SECONDARY_CAS_RN
X32KK4201D UNII
NOCODE MMSL
4027336 VANDF
4033254 VANDF
000702 NDDF
004531 NDDF
005313 NDDF
006923 NDDF
322052003 SNOMEDCT_US
350631001 SNOMEDCT_US
418067008 SNOMEDCT_US
708177006 SNOMEDCT_US

Pharmaceutical products:

None