BOPINDOLOL FUMARATE

Details

Stereochemistry	RACEMIC
Molecular Formula	C23H28N2O3.C4H4O4
Molecular Weight	496.5522
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C\C(O)=O.CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)OC(=O)C3=CC=CC=C3

InChI

InChIKey=SRGXLPJWUNBTKJ-WLHGVMLRSA-N

InChI=1S/C23H28N2O3.C4H4O4/c1-16-13-19-20(25-16)11-8-12-21(19)27-15-18(14-24-23(2,3)4)28-22(26)17-9-6-5-7-10-17;5-3(6)1-2-4(7)8/h5-13,18,24-25H,14-15H2,1-4H3;1-2H,(H,5,6)(H,7,8)/b;2-1+

HIDE SMILES / InChI

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Molecular Formula	C23H28N2O3
Molecular Weight	380.48
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.1981.tb10708.x/epdf
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/11314603 | https://www.ncbi.nlm.nih.gov/pubmed/1706984

Bopindolol (4-[benzoyloxy-3-tertbutylaminopropoxy]-2-methylindole hydrogen malonate) is an indole beta-adrenoceptor antagonist bearing a benzoyl ester residue on the beta-carbon atom of the propanolamine side chain. Bopindolol is metabolized by esterase to benzoic acid and an active metabolite, 18-502 [4-(3-t-butylamino-2-hydroxypropoxy)-2-methyl indole], which is further metabolized to 20-785 [4-(3-t-butylaminopropoxy)-2-carboxyl indole]. Bopindolol produces sustained blockade of beta 1- and beta 2-adrenoceptors, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is used in the treatment of hypertension. In limited trials bopindolol has also successfully reduced symptoms in patients with angina pectoris, anxiety and essential tremor.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Beta-1 adrenergic receptor 163 Target ID: CHEMBL213 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11314603	Antagonist 2849	7.44 null [pKi]
Beta-2 adrenergic receptor 209 Target ID: CHEMBL210 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11314603	Antagonist 2849	7.33 null [pKi]
Serotonin 1a (5-HT1a) receptor 177 Target ID: CHEMBL273 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11314603	Interacts 323

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1706984 https://www.ncbi.nlm.nih.gov/pubmed/2889554	Primary		Approved 8583	BOPINDOLOL Approved Use Bopindolol is a nonselective beta-adrenoceptor antagonist with partial agonist activity which is used in the treatment of hypertension.

C_max

Value	Dose	Analyte	Population
1.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	7 mg single, transdermal dose: 7 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.2 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	21 mg single, transdermal dose: 21 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
7.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
7.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg 1 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg 1 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
51.38 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2868747/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
129.38 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2868747/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
40 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
153 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
234 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
232 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	7 mg single, transdermal dose: 7 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
353 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	14 mg single, transdermal dose: 14 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
547 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	21 mg single, transdermal dose: 21 mg route of administration: Transdermal experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
75 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
64 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678271/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
17.8 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
32.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
19.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
22.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg 1 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
42.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg 1 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
4.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2868747/	1 mg single, intravenous dose: 1 mg route of administration: Intravenous experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2868747/	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg 1 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1678272/	0.5 mg 1 times / day steady-state, oral dose: 0.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	PINDOLOL plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
4 mg 1 times / day multiple, oral Higher than recommended Dose: 4 mg, 1 times / day Route: oral Route: multiple Dose: 4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6127218/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6127218/	Disc. AE: Flatulence... AEs leading to discontinuation/dose reduction: Flatulence (7.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/6127218/
2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2866965/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2866965/	Sources: https://pubmed.ncbi.nlm.nih.gov/2866965/
2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2906897/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2906897/	Disc. AE: Anxiety... AEs leading to discontinuation/dose reduction: Anxiety (3.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/2906897/

AEs

AE	Significance	Dose	Population
Flatulence	7.7% Disc. AE	4 mg 1 times / day multiple, oral Higher than recommended Dose: 4 mg, 1 times / day Route: oral Route: multiple Dose: 4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/6127218/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/6127218/
Anxiety	3.3% Disc. AE	2 mg 1 times / day multiple, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: multiple Dose: 2 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2906897/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/2906897/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2E1 1060 CYP2C19 2057 CYP2A6 879 CYP19A1 429	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM1Nzk5NSJ9fQ==	no [IC50 >10 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM1Nzk5NSJ9fQ==	no [IC50 >10 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM1Nzk5NSJ9fQ==	no [IC50 >10 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM1Nzk5NSJ9fQ==	no [IC50 >10 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDM1Nzk5NSJ9fQ==	no [IC50 >10 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMzU3OTk1In19	no [IC50 >10 uM]
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/44112#section=BioAssay-Results	no
CYP3A4 2633	inducer 1966 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/44112#section=BioAssay-Results Page: 141.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMzU3OTk1In19	yes [IC50 5.4764 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/44112#section=BioAssay-Results Page: 140 \| 141	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMzU3OTk1In19

PubMed

Title	Date	PubMed
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.	2011-07-14	21599003
Management of hyperuricemia in gout: focus on febuxostat.	2010-02-02	20169038
Chiral separations of some beta-adrenergic agonists and antagonists on AmyCoat column by HPLC.	2010-01	19208401
Role of chemical structure in stereoselective recognition of beta-blockers by cyclodextrins in capillary zone electrophoresis.	2008-04-24	18022245
Transdermal delivery of beta-blockers.	2006-05	16640500
Role of chemical structure in stereoselective recognition of beta-blockers and H1-antihistamines by human serum transferrin in capillary zone electrophoresis.	2006-04	16609932
Determination of bopindolol using the flow injection technique coupled with solid phase extraction.	2003-12-04	14656606
Determination of bopindolol by sequential injection technique with spectrophotometric detection.	2003-10	14505739
Spin trapping study of reactive oxygen species formation during bopindolol peroxidation.	2002-10-15	12209459
Determination of bopindolol in pharmaceuticals by capillary isotachophoresis.	2002-05-15	12008130
Effect of vasodilatory beta-adrenoceptor blockers on cardiovascular haemodynamics in anaesthetized rats.	2002-03	11906483
Bopindolol: pharmacological basis and clinical implications.	2001	11314603
Comparison of chlorthalidone, propranolol and bopindolol in six-month treatment of arterial hypertension.	1998	9675624
Hypotensive effect of bopindolol in pithed rats.	1993-03	8097742
[Multicenter study of isradipine in the treatment of hypertension].	1992-04	1352927
Bopindolol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy.	1991-01	1706984
Beta-blockers and psychic stress: a double-blind, placebo-controlled study of bopindolol vs lorazepam and butalbital in surgical patients.	1985-09	2865218

Patents

Sample Use Guides

In Vivo Use Guide

antihypertensive effects of bopindolol 0.5 to 4 mg are sustained for more than 24 hours after once daily dosing

Route of Administration: Oral

In Vitro Use Guide

In guinea-pig isolated atria bopindolol at concentrations between 3.2 nM and 2 uM produced an inhibition of the positive chronotropic and inotropic effects of adrenaline

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:36:43 GMT 2025` Edited by `admin` on `Mon Mar 31 18:36:43 GMT 2025`
Record UNII	GM76OF8LS3
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

2-PROPANOL, 1-((1,1-DIMETHYLETHYL)AMINO)-3-((2-METHYL-1H-INDOL-4-YL)OXY)-, 2-BENZOATE, 2-BUTENEDIOATE (1:1)

Preferred Name

English

BOPINDOLOL FUMARATE

Common Name

English

2-PROPANOL, 1-((1,1-DIMETHYLETHYL)AMINO)-3-((2-METHYL-1H-INDOL-4-YL)OXY)-, BENZOATE (ESTER), (2E)-2-BUTENEDIOATE (1:1) (SALT)

Common Name

English

Bopindolol fumarate [WHO-DD]

Common Name

English

2-PROPANOL, 1-((1,1-DIMETHYLETHYL)AMINO)-3-((2-METHYL-1H-INDOL-4-YL)OXY)-, BENZOATE (ESTER), (E)-2-BUTENEDIOATE (1:1) (SALT)

Common Name

English

BOPINDOLOL HYDROGEN FUMARATE

Common Name

English

Code System Code Type Description

CAS

79125-22-7