Compounds > cicloprolol

Page last updated: 2024-12-08

cicloprolol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

SL 75177-10: related to betaxolol [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	146294
CHEMBL ID	2110772
CHEBI ID	135377
SCHEMBL ID	634972
MeSH ID	M0152063

Synonyms (32)

Synonym
gtpl552
cicloprolol
CHEBI:135377
L000657
1-[4-[2-(cyclopropylmethoxy)ethoxy]phenoxy]-3-(propan-2-ylamino)propan-2-ol
2-propanol, 1-(4-(2-(cyclopropylmethoxy)ethoxy)phenoxy)-3-((1-methylethyl)amino)-
94651-09-9
63659-12-1
sl 75177-10
sl 75.177-10
91094-14-3
sl-75.177.10
sl 75-177-10
sl 75,177-10
1-(4-((2-cyclopropylmethoxy)ethoxy)phenoxy)-3-((1-methylethyl)amino)-2-propanol
1k2ach4u3r ,
sl 75117-10
(+-)-1-(p-(2-(cyclopropylmethoxy)ethoxy)phenoxy)-3-(isopropylamino)-2-propanol
cicloprololum
unii-1k2ach4u3r
cicloprolol [inn:ban]
SCHEMBL634972
(+/-)-1-(p-(2-(cyclopropylmethoxy)ethoxy)phenoxy)-3-(isopropylamino)-2-propanol
cicloprolol [inn]
2-propanol, 1-(4-(2-(cyclopropylmethoxy)ethoxy)phenoxy)-3-((1-methylethyl)amino)-, (+/-)-
cicloprolol [mart.]
CHEMBL2110772
sl 75.177-10 (9ci)
1-(4-(2-(cyclopropylmethoxy)ethoxy)phenoxy)-3-(propan-2-ylamino)propan-2-ol
Q15634018
DTXSID70867026
sl 75.177-10(9ci)

Research Excerpts

Overview

Cicloprolol is a partial beta 1-adrenoceptor agonist considered for the treatment of patients with coronary artery disease and impaired left ventricular function. Its haemodynamic and radionuclide (nuclear stethoscope) effects were determined in 22 patients.

Excerpt	Reference	Relevance
"Cicloprolol is a new beta-blocking agent with high selectivity for beta 1 receptors and high intrinsic sympathomimetic activity. "	( Combined invasive and noninvasive study of left ventricular systolic and diastolic function following acute administration of cicloprolol to subjects with normal cardiac function. Bonandi, L; Dei Cas, L; Ettori, F; Metra, M; Niccoli, L; Nodari, S; Visioli, O, 1992)	1.93
"1. Cicloprolol is a partial beta 1-adrenoceptor agonist considered for the treatment of patients with coronary artery disease and impaired left ventricular function. "	( Pharmacodynamic without pharmacokinetic interaction between cicloprolol, a partial beta 1-adrenoceptor agonist, and digoxin in healthy subjects. Bianchetti, G; De Lauture, D; Dessault, O; Julien, J; Kahan, A; Morselli, PL; Pinquier, JL; Rosenzweig, P; Strauch, G; Weber, S, 1990)	1.14
"Cicloprolol is a new cardioselective beta-blocking agent with partial agonist activity (intrinsic sympathomimetic activity, ISA). "	( Comparative effects of atenolol and cicloprolol on cardiac performance in coronary heart disease. Frais, MA; Reynolds, G; Sharma, SK; Silke, B; Taylor, SH; Verma, SP, 1989)	1.99
"Cicloprolol is a cardioselective beta-1 partial agonist; its haemodynamic and radionuclide (nuclear stethoscope) effects were determined in 22 patients with impaired left ventricular function due to coronary artery disease. "	( Haemodynamic dose-response actions of cicloprolol in left ventricular dysfunction due to ischaemic heart disease. Baig, W; Frais, MA; Jackson, NC; Reynolds, G; Sharma, SK; Silke, B; Taylor, SH; Verma, SP, 1987)	1.99

Effects

Excerpt	Reference	Relevance
"Cicloprolol has significant partial agonist activity at the beta 1-adrenoceptor as indicated by increases in heart rate and systolic blood pressure."	( Studies of the agonist and antagonist activity of cicloprolol in man. Burke, M; McCaffrey, PM; Riddell, JG; Shanks, RG, 1988)	1.25

Treatment

Excerpt	Reference	Relevance
"Treatment with cicloprolol should protect the heart against excessive stimulation, while providing a baseline level of sympathetic drive."	( An evaluation of the safety of the beta-modulator cicloprolol in chronic heart failure. Alfiero, R; Cocco, G; Pouleur, H, 1992)	0.88

Toxicity

Excerpt	Reference	Relevance
" Thus, short-term administration of cicloprolol is safe in moderate heart failure."	( An evaluation of the safety of the beta-modulator cicloprolol in chronic heart failure. Alfiero, R; Cocco, G; Pouleur, H, 1992)	0.81

Dosage Studied

Excerpt	Relevance	Reference
" Its haemodynamic profile was compared with that of atenolol (cardioselective; no ISA) in a comparative dose-response study of 24 ischaemic patients with diminished cardiac reserve."	( Comparative effects of atenolol and cicloprolol on cardiac performance in coronary heart disease. Frais, MA; Reynolds, G; Sharma, SK; Silke, B; Taylor, SH; Verma, SP, 1989)	0.55
" In order to mimic the intrinsic effects of the partial agonist drugs, control dose-response curves for isoproterenol were determined in pithed rats in which the base-line heart rate was elevated by thoracic spinal cord stimulation."	( Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol. Cavero, I; Hicks, PE; Langer, SZ; Lefevre-Borg, F; Manoury, P, 1987)	0.49
"2 mg/kg dosage were assessed during supine bicycle exercise and compared with a control exercise period."	( Haemodynamic dose-response actions of cicloprolol in left ventricular dysfunction due to ischaemic heart disease. Baig, W; Frais, MA; Jackson, NC; Reynolds, G; Sharma, SK; Silke, B; Taylor, SH; Verma, SP, 1987)	0.54

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

Class	Description
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (2)

Assay ID	Title	Year	Journal	Article
AID1346250	Human beta2-adrenoceptor (Adrenoceptors)	1999	European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3	LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
AID1346260	Human beta1-adrenoceptor (Adrenoceptors)	1999	European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3	LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	7 (53.85)	18.7374
1990's	6 (46.15)	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]

Market Indicators

Research Demand Index: 11.29

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.

Metric	This Compound (vs All)
Research Demand Index	11.29 (24.57)
Research Supply Index	3.14 (2.92)
Research Growth Index	4.42 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.29)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	6 (37.50%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	10 (62.50%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
albuterol Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).	3.35	1	1	phenols; phenylethanolamines; secondary amino compound	beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic
atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.	9.62	3	2	ethanolamines; monocarboxylic acid amide; propanolamine	anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic
betaxolol [no description available]	2.38	2	0	propanolamine	antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent
bupranolol Bupranolol: An adrenergic-beta-2 antagonist that has been used for cardiac arrhythmia, angina pectoris, hypertension, glaucoma, and as an antithrombotic.	2	1	0	aromatic ether
cgp 20712a [no description available]	2	1	0	imidazoles
cgp 12177 CGP 12177 : A benzimidazole that is benzimidazol-2-one substituted at position 4 by a 3-(tert-butylamino)-2-hydroxypropoxy group.	2	1	0	aromatic ether; benzimidazoles; secondary alcohol; secondary amino compound	beta-adrenergic antagonist
isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.	2.37	2	0	catechols; secondary alcohol; secondary amino compound	beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent
metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.	2	1	0	aromatic ether; propanolamine; secondary alcohol; secondary amino compound	antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic
pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.	4.05	3	1	indoles; secondary amine	antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; serotonergic antagonist; vasodilator agent
practolol Practolol: A beta-1 adrenergic antagonist that has been used in the emergency treatment of CARDIAC ARRYTHMIAS.. practolol : N-(4-Hydroxyphenyl)acetamide in which the hydrogen of the phenolic hydroxy group is substituted by a 3-(isopropylaminoamino)-2-hydroxypropyl group. A selective beta blocker, it has been used in the emergency treatment of cardiac arrhythmias.	2	1	0	acetamides; ethanolamines; propanolamine; secondary alcohol; secondary amino compound	anti-arrhythmia drug; beta-adrenergic antagonist
propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.	2.38	2	0	naphthalenes; propanolamine; secondary amine	anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic
reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.	1.97	1	0	alkaloid ester; methyl ester; yohimban alkaloid	adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic
prenalterol Prenalterol: A partial adrenergic agonist with functional beta 1-receptor specificity and inotropic effect. It is effective in the treatment of acute CARDIAC FAILURE, postmyocardial infarction low-output syndrome, SHOCK, and reducing ORTHOSTATIC HYPOTENSION in the SHY-RAGER SYNDROME.	8.76	2	1	aromatic ether
xamoterol Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist.	2.37	2	0	morpholines
digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.	8.36	1	1	cardenolide glycoside; steroid saponin	anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope

Condition	Relationship Strength	Studies	Trials
Chronic Illness [description not available]	3.36	1	1
Cardiac Output, Low A state of subnormal or depressed cardiac output at rest or during stress. It is a characteristic of CARDIOVASCULAR DISEASES, including congenital, valvular, rheumatic, hypertensive, coronary, and cardiomyopathic. The serious form of low cardiac output is characterized by marked reduction in STROKE VOLUME, and systemic vasoconstriction resulting in cold, pale, and sometimes cyanotic extremities.	3.36	1	1
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	3.36	1	1
Angor Pectoris [description not available]	2.38	2	0
Angina Pectoris The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION.	2.38	2	0
Uremia A clinical syndrome associated with the retention of renal waste products or uremic toxins in the blood. It is usually the result of RENAL INSUFFICIENCY. Most uremic toxins are end products of protein or nitrogen CATABOLISM, such as UREA or CREATININE. Severe uremia can lead to multiple organ dysfunctions with a constellation of symptoms.	1.97	1	0
Coronary Heart Disease [description not available]	8.76	2	1
Coronary Disease An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.	3.76	2	1
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	1.97	1	0
Cardiovascular Stroke [description not available]	1.97	1	0
Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).	1.97	1	0
Intraocular Pressure The pressure of the fluids in the eye.	8.35	1	1
Cardiac Failure [description not available]	6.97	1	0
Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.	1.97	1	0

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