Exaprolol is a beta blocker with vasodilating properties. It acts primarily as a selective beta1-adrenergic receptor antagonist, but also exhibits some beta2-blocking activity. Exaprolol is synthesized via a multi-step process involving the reaction of an appropriate amine with a substituted benzoic acid derivative. It is used in the treatment of hypertension, angina pectoris, and other cardiovascular conditions. Exaprolol's vasodilating effects are attributed to its ability to block the release of vasoconstricting substances such as renin and norepinephrine. This action contributes to its effectiveness in lowering blood pressure and improving blood flow to the heart. Exaprolol is studied to further understand its potential therapeutic applications in various cardiovascular diseases and to investigate its safety and efficacy in different patient populations.'
exaprolol: structure; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 65485 |
| CHEMBL ID | 2110841 |
| SCHEMBL ID | 614255 |
| MeSH ID | M0060370 |
| Synonym |
|---|
| 2-propanol, 1-(2-cyclohexylphenoxy)-3-((1-methylethyl)amino)- |
| brn 1993835 |
| esaprololo [dcit] |
| 1-isopropylamino-3-(2-cyclohexylphenoxy)-2-propanol |
| vulm 111 |
| exaprololum [inn-latin] |
| 1-(o-cyklohexyl)fenoxy-3-izopropyl(aminopropan-1-ol) [czech] |
| 1-(2-cyclohexylphenoxy)-3-((1-methylethyl)amino)-2-propanol |
| exaprolol [inn] |
| exaprolol |
| 1-(2-cyclohexylphenoxy)-3-(propan-2-ylamino)propan-2-ol |
| 55837-19-9 |
| 1-(o-cyklohexyl)fenoxy-3-izopropyl(aminopropan-1-ol) |
| esaprololo |
| unii-q4xx54i93r |
| q4xx54i93r , |
| exaprololum |
| (+/-)-1-(o-cyclohexylphenoxy)-3-(isopropylamino)-2-propanol |
| exaprolol [who-dd] |
| 2-propanol, 1-(2-cyclohexylphenoxy)-3-((1-methylethyl)amino)-,(+/-)- |
| SCHEMBL614255 |
| CHEMBL2110841 |
| ABXHHEZNIJUQFM-UHFFFAOYSA-N |
| Q15634015 |
| DTXSID20866509 |
Exaprolol has the appropriate lipophilicity for entry of the CNS and is claimed to be a very potent beta-adrenoceptor antagonist. It also has direct electrophysiological effects on cardiac (Purkinje) tissue, reducing the rate of rise of phase 0 of the action potential.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Exaprolol has the appropriate lipophilicity (log P + 1.6) for entry of the CNS and is claimed to be a very potent beta-adrenoceptor antagonist." | ( Synthesis and preliminary evaluation of (S)-[11C]-exaprolol, a novel beta-adrenoceptor ligand for PET. de Jong, JR; Dierckx, RA; Doorduin, J; Elsinga, PH; van Waarde, A, ) | 1.11 |
| "Exaprolol also has direct electrophysiological effects on cardiac (Purkinje) tissue, reducing the rate of rise of phase 0 of the action potential." | ( Aspects of the cardiovascular pharmacology of exaprolol. Hughes, B; Kane, KA; McDonald, FM; Parratt, JR, 1984) | 1.25 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Exaprolol-pretreated hearts revealed better postischaemic recovery of the left ventricular dP/dt max and stroke volume as well as improved efficiency in the transformation of chemical energy to mechanical work." | ( The influence of exaprolol upon the ischaemic rat heart and its interaction with sarcolemmal (Na+ + K+)-ATPase. Barta, E; Dzurba, A; Okolicány, J; Styk, J; Ziegelhöffer, A, 1989) | 1.34 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The inhibitory effect of EDTA, tetrodotoxine and suramine on histamine release after exaprolol explains the non-receptor mechanism of exaprolol effect, which confirms a possibility of induction of adverse effects of blockers of the beta-adrenergic receptor in the development of a bronchospasm." | ( [Analysis of the adverse effects of drugs at the cellular and subcellular levels]. Drábiková, K; Jakubovský, J; Nosál', R; Ondrias, K; Pecivová, J, 1990) | 0.5 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The pharmacokinetic parameters show an enhanced plasma elimination of both drugs at interrupted enterohepatic circulation compared to the control group." | ( The pharmacokinetics of exaprolol and propranolol in rats with interrupted enterohepatic circulation. Bezek, S; Durisová, M; Faberová, V; Misánikova, K; Motheová, O; Trnovec, T; Zemánek, M, ) | 0.44 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The absorption rate of the beta-adrenoceptor blocking drug, exaprolol, from the gastrointestinal tract was studied using in-situ methods in the rat and dog." | ( Absorption of exaprolol from the in-situ gastrointestinal tract of rats and dogs. Durisová, M; Faberova, V; Gabauer, I; Motheová, O; Nosálová, V; Styk, J; Trnovec, T; Zemánek, M, 1985) | 0.87 |
| "1 hr, respectively, were found; the bioavailability was 26." | ( Disposition of exaprolol, a new beta-blocker, in rats. Bezek, S; Durisová, M; Faberová, V; Tomcíková, O; Trnovec, T; Ujházy, E; Zemánek, M, ) | 0.48 |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 18 (69.23) | 18.7374 |
| 1990's | 8 (30.77) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (10.88) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 31 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||