U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 191 - 200 of 203 results

Status:
Possibly Marketed Outside US
Source:
Japan:Tulobuterol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Tulobuterol is a long-acting beta2-adrenergic receptor agonist. Tulobuterol has almost no effects on blood pressure and heart rate and is highly selective for the tracheal muscle. It is indicated to improve symptoms such as respiratory distress caused by airway obstruction of bronchial asthma, bronchitis, chronic obstructive pulmonary disease (COPD) and emphysema. Serious side effects detected were: tremor, palpitations and serum potassium level decrease.
Alprenolol is a beta adrenoreceptor blocking agent and 5HT1A antagonist, developed by AstraZeneca and now available as generic drug. It is used for treatment of hypertension, angina pectoris due to coronary atherosclerosis and acute myocardial infarction.
Status:
Possibly Marketed Outside US
Source:
Japan:Clorprenaline Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Clorprenaline is a β2-adrenergic receptor agonist. As a bronchodilator it has been used for the treatment of bronchial asthma, bronchitis and other respiratory diseases. It is a potential new lean meat-boosting feed additive because it can promote animal muscular mass growth and decrease fat accumulation.
Dilevalol, the RR-stereoisomer of labetalol, is a non-cardioselective β-adrenoceptor antagonist with substantial partial β2-agonist and negligible α1-blocking activity. Reduction in blood pressure during dilevalol administration is associated with peripheral vasodilatation, and heart rate remains essentially unchanged. Following oral administration, dilevalol is completely absorbed. Once-daily administration is possible, due to a long elimination half-life. In vitro and in vivo animal studies and results obtained in humans reveal that dilevalol is a nonselective blocker of β1- and β2-adrenoceptors, with a similar potency to propranolol, but has negligible antagonistic activity at α1-receptors. Dilevalol, the R,R′ stereoisomer, makes up 25% of racemic labetalol, the drug, approved by FDA for the treatment of hypertension. The relaxing potency of dilevalol was approximately 4.7 times more potent than that of labetalol. Dilevalol markedly reduced the diastolic blood pressure with only a slight increase of heart rate In pithed rats, while isoproterenol and pindolol caused moderate to marked positive chronotropic effects in proportion to their hypotensive effects. These results suggest that dilevalol has more potent ISA than labetalol. In contrast to labetalol, dilevalol possesses little, if any, alpha-adrenergic blocking activity. The compound is 3 to 10 times less potent than labetalol at α1-adrenergic receptors under a variety of experimental conditions. Moreover, it is 300- to 1000-fold less potent at alpha1-adrenergic receptors compared with β1-adrenergic receptors. The pA2 values for dilevalol as an α antagonist range from 5.9 to 6.4. Because maximal plasma concentrations of the drug after administration of a 400-mg dose are approximately 0.5 pmol, it is doubtful that alpha blockade is involved in the antihypertensive response to dilevalol in humans.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)



Hexoprenaline is a selective beta2-adrenoreceptor agonist indicated for use in the treatment of bronchospasm associated with obstructive airways diseases, including asthma, bronchitis and emphysema. In many countries the drug is used as tocolytic agent (under the trade name gynipral).
Status:
Possibly Marketed Outside US
Source:
UK NHS:Dopexamine hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dopexamine hydrochloride is a synthetic catecholamine, structurally related to dopamine, with marked intrinsic agonist activity at beta 2-adrenoceptors, lesser agonist activity at dopamine DA1- and DA2-receptors and beta 1-adrenoceptors, and an inhibitory action on the neuronal catecholamine uptake mechanism. The drug is administered by intravenous infusion, and is characterized by a rapid onset and short duration of action. Dopexamine is being tested as a treatment for heart failure and sepsis.
Status:
Possibly Marketed Outside US
Source:
Japan:Procaterol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Procaterol is a beta2-adrenoreceptor agonist. It is a bronchodilator that may be administered orally or by aerosol inhalation for the treatment of dyspnea caused by bronchial asthma, chronic bronchitis, and pulmonary emphysema. The drug is not approved in the USA, but is available in Japan, Indonesia, and other countries worldwide.
(-)-Propranolol is a small molecule β-adrenergic receptor antagonist and the active isomer of (±)-Propranolol preparations. (-)-Propranolol blocks the binding of epinephrine, norepinephrine, and other endogenous catecholamines to the β-adrenergic receptor, impeding increases in cardiac flow velocity and general stimulation of the sympathetic nervous system signaled by the association of these molecules to the β-adrenergic receptor. In addition to blockade of agonist binding, antagonism of the β-adrenergic receptor by (-)-Propranolol produces negative chronotropic and inotropic action, effectively dampening the force and rate of cardiac contraction. These negative chronotropic and inotropic effects correlate to a demonstrated suppression of adrenaline-induced cardiac arrhythmia by (-)-Propranolol. Suppression of β-adrenergic receptor activation by (-)-Propranolol has been widely exploited in counteracting situations sensitive to heightened cardiac activity including hypertension, angina pectoris, and cardiac ischemia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Reproterol is a short-acting β2 adrenoreceptor agonist used in the treatment of asthma. Reproterol increases the generation of cAMP in isolated peripheral blood monocytes in vitro more effectively than does orciprenaline. In the presence of the highly potent but nonselective ß-antagonist, propranolol, the cAMP-generating action of reproterol was inhibited only partially. Reproterol has gained wide use when it was licensed as a fixed combination therapy with cromoglycate. Until today, the bronchodilator effects of reproterol and the bronchoprotective and anti-inflammatory actions of cromoglycate combined in one inhaler remain the successful fixed combination of a disease-modifying and symptomatic drug for the treatment of asthma.
Status:
Possibly Marketed Outside US
Source:
Japan:Procaterol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Procaterol is a beta2-adrenoreceptor agonist. It is a bronchodilator that may be administered orally or by aerosol inhalation for the treatment of dyspnea caused by bronchial asthma, chronic bronchitis, and pulmonary emphysema. The drug is not approved in the USA, but is available in Japan, Indonesia, and other countries worldwide.

Showing 191 - 200 of 203 results