BIOMAT Database Logo BIOMAT Database Logo

Intrinsic beta-sympathomimetic activity of dilevalol, R, R-isomer of labetalol. 1985

K Matsunaga, and K Nakamura, and M Ueda

The potency and selectivity of the intrinsic beta-sympathomimetic activity (ISA) of dilevalol were studied with isolated guinea-pig trachea and pithed rat. This drug relaxed the contracture of isolated guinea-pig tracheal preparation induced by histamine in a dose-dependent manner. The dose-response curves of dilevalol and labetalol were shifted to the right with propranolol pretreatment. 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 and shows more beta 2-adrenoceptor selectivity than pindolol.

UI MeSH Term Description Entries
D007741 Labetalol A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS. AH-5158,Albetol,Apo-Labetalol,Dilevalol,Labetalol Hydrochloride,Labetalol, (R,R)-Isomer,Labetolol,Normodyne,Presolol,R,R-Labetalol,SCH-19927,Trandate,AH 5158,AH5158,Apo Labetalol,ApoLabetalol,Hydrochloride, Labetalol,R,R Labetalol,SCH 19927,SCH19927
D008297 Male Males
D009126 Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position. Muscle Relaxations,Relaxation, Muscle,Relaxations, Muscle
D009130 Muscle, Smooth Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed) Muscle, Involuntary,Smooth Muscle,Involuntary Muscle,Involuntary Muscles,Muscles, Involuntary,Muscles, Smooth,Smooth Muscles
D010869 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) Prindolol,LB-46,Visken,LB 46,LB46
D011433 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. Dexpropranolol,AY-20694,Anaprilin,Anapriline,Avlocardyl,Betadren,Dociton,Inderal,Obsidan,Obzidan,Propanolol,Propranolol Hydrochloride,Rexigen,AY 20694,AY20694,Hydrochloride, Propranolol
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D001794 Blood Pressure PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS. Systolic Pressure,Diastolic Pressure,Pulse Pressure,Pressure, Blood,Pressure, Diastolic,Pressure, Pulse,Pressure, Systolic,Pressures, Systolic
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006339 Heart Rate The number of times the HEART VENTRICLES contract per unit of time, usually per minute. Cardiac Rate,Chronotropism, Cardiac,Heart Rate Control,Heartbeat,Pulse Rate,Cardiac Chronotropy,Cardiac Chronotropism,Cardiac Rates,Chronotropy, Cardiac,Control, Heart Rate,Heart Rates,Heartbeats,Pulse Rates,Rate Control, Heart,Rate, Cardiac,Rate, Heart,Rate, Pulse

Related Publications

K Matsunaga, and K Nakamura, and M Ueda
Intrinsic sympathomimetic activity of labetalol.
January 1986, Journal of cardiovascular pharmacology,
K Matsunaga, and K Nakamura, and M Ueda
Cellular electrophysiology and beta-adrenergic-blocking activity of dilevalol, the R,R-isomer of labetalol, on isolated canine cardiac tissues.
September 1989, Journal of cardiovascular pharmacology,
K Matsunaga, and K Nakamura, and M Ueda
Cardiac electrophysiologic actions of SCH 19927 (Dilevalol), the R,R-isomer of labetalol.
December 1986, The Journal of pharmacology and experimental therapeutics,
K Matsunaga, and K Nakamura, and M Ueda
Intravenous dilevalol. Effects of the R-R optical isomer of labetalol in patients with severe hypertension.
March 1988, Archives of internal medicine,
K Matsunaga, and K Nakamura, and M Ueda
Antifibrillatory efficacy of concomitant beta adrenergic receptor blockade with dilevalol, the R,R-isomer of labetalol, and muscarinic receptor blockade with methylscopolamine.
May 1987, The Journal of pharmacology and experimental therapeutics,
K Matsunaga, and K Nakamura, and M Ueda
[Intrinsic sympathomimetic activity of beta-blockers].
September 1978, La Nouvelle presse medicale,
K Matsunaga, and K Nakamura, and M Ueda
Beta blockers with intrinsic sympathomimetic activity.
January 1985, American family physician,
K Matsunaga, and K Nakamura, and M Ueda
Effects of dilevalol, an R, R-isomer of labetalol, on blood pressure and renal function in patients with mild-to-moderate essential hypertension.
January 1988, European journal of clinical pharmacology,
K Matsunaga, and K Nakamura, and M Ueda
Alpha and beta adrenoceptor blocking properties of labetalol and its R,R-isomer, SCH 19927.
August 1981, The Journal of pharmacology and experimental therapeutics,
K Matsunaga, and K Nakamura, and M Ueda
Relevance of intrinsic sympathomimetic activity for beta blockers.
September 1990, The American journal of cardiology,
Copied contents to your clipboard!