Effects of Mepivacaine on adrenergic neuroeffector junction of the isolated rabbit aorta. 1982

S Fukuda, and T Tsuji, and T Murakawa, and H Takeshita, and N Toda

The effect of mepivacaine on adrenergic neuroeffector junction was studied in the isolated rabbit aorta. Mepivacaine, 5 X 10(-5) to 5 X 10(-4) M, attenuated the contractile response to transmural neural stimulation, the attenuation being greater in the response at high frequency stimulations. The attenuation of the responses by mepivacaine was not prevented by prior application of cocaine. The concentration-response curve for norepinephrine was shifted to the right by mepivacaine, 5 X 10(-5) to 2 X 10(-3) M. The attenuation of the response to transmural stimulation was greater than that of the response to an equipotent concentration of exogenous norepinephrine. Pretreatment with mepivacaine, 5 X 10(-5) to 2 X 10(-3) M, protected alpha-adrenoceptors from persistent blockade by phenoxybenzamine in a dose-dependent manner. The contractile response to histamine was not significantly altered by mepivacaine in concentrations up to 5 X 10(-4) M. Mepivacaine, 5 X 10(-4) and 2 X 10(-3) M, decreased the response to high concentrations of KCl. Ca2+-induced contractions in aortic strips previously exposed to Ca2+-free media and depolarized by excess K+ were significantly inhibited by mepivacaine, 5 X 10(-4) and 2 X 10(-3) M. It may be concluded that mepivacaine causes vasodilation through an alpha-adrenoceptor antagonism in addition to a sympathetic nerve conduction blockade. High concentrations of mepivacaine appear to interfere with the transmembrane influx of calcium in the vascular smooth muscle.

UI MeSH Term Description Entries
D008297 Male Males
D008619 Mepivacaine A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168) Carbocaine,Carbocaïne,Isocaine,Isogaine,Meaverin,Mecain,Mepihexal,Mepivacain-Injektopas,Mepivacaina Braun,Mepivacaine Hydrochloride,Mepivacaine Monohydrochloride,Mepivastesin,Polocaine,Scandicain,Scandicaine,Scandinibsa,Scandonest,Mepivacain Injektopas
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D009451 Neuroeffector Junction The synapse between a neuron (presynaptic) and an effector cell other than another neuron (postsynaptic). Neuroeffector junctions include synapses onto muscles and onto secretory cells. Junction, Neuroeffector,Junctions, Neuroeffector,Neuroeffector Junctions
D009638 Norepinephrine Precursor of epinephrine that is secreted by the ADRENAL MEDULLA and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers, and of the diffuse projection system in the brain that arises from the LOCUS CERULEUS. It is also found in plants and is used pharmacologically as a sympathomimetic. Levarterenol,Levonorepinephrine,Noradrenaline,Arterenol,Levonor,Levophed,Levophed Bitartrate,Noradrenaline Bitartrate,Noradrénaline tartrate renaudin,Norepinephrin d-Tartrate (1:1),Norepinephrine Bitartrate,Norepinephrine Hydrochloride,Norepinephrine Hydrochloride, (+)-Isomer,Norepinephrine Hydrochloride, (+,-)-Isomer,Norepinephrine d-Tartrate (1:1),Norepinephrine l-Tartrate (1:1),Norepinephrine l-Tartrate (1:1), (+,-)-Isomer,Norepinephrine l-Tartrate (1:1), Monohydrate,Norepinephrine l-Tartrate (1:1), Monohydrate, (+)-Isomer,Norepinephrine l-Tartrate (1:2),Norepinephrine l-Tartrate, (+)-Isomer,Norepinephrine, (+)-Isomer,Norepinephrine, (+,-)-Isomer
D010643 Phenoxybenzamine An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. Dibenylene,Dibenyline,Dibenziran,Dibenzylin,Dibenzyline,Dibenzyran,Phenoxybenzamine Hydrochloride,Hydrochloride, Phenoxybenzamine
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D002118 Calcium A basic element found in nearly all tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes. Coagulation Factor IV,Factor IV,Blood Coagulation Factor IV,Calcium-40,Calcium 40,Factor IV, Coagulation
D004837 Epinephrine The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS. Adrenaline,4-(1-Hydroxy-2-(methylamino)ethyl)-1,2-benzenediol,Adrenaline Acid Tartrate,Adrenaline Bitartrate,Adrenaline Hydrochloride,Epifrin,Epinephrine Acetate,Epinephrine Bitartrate,Epinephrine Hydrochloride,Epinephrine Hydrogen Tartrate,Epitrate,Lyophrin,Medihaler-Epi,Acetate, Epinephrine
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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