A regional difference in alpha 1-adrenoceptor mechanism in canine veins. 1987

I Takayanagi, and K Koike, and R Noguchi, and M Ogishima, and F Takiguchi, and T Sato
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.

The pD2-values for noradrenaline obtained from the veins of the body wall were quite different from those embryogenetically related to the digestive tract. Therefore, the difference in the post-junctional alpha 1-adrenoceptor mechanism was studied in venous smooth muscle preparations from the canine. The helical and longitudinal strips of the lateral saphenous, femoral and portal veins, and the inferior vena cava were prepared and set in an organ bath apparatus. The longitudinal strips of the lateral saphenous and femoral veins, and inferior vena cava did not or little respond to noradrenaline. The pD2-values for noradrenaline differed considerably among the veins, while the pA2-values for prazosin against noradrenaline were identical in all veins used. Negative log of dissociation constants, pKA-values, for noradrenaline obtained by the partial irreversible blockade of alpha 1-adrenoceptors with phenoxybenzamine were very similar in all the veins. Efficacies which were calculated by the same method differed considerably among the veins. The dissociation constants, KD-value and the maximum binding sites, Bmax-values for [3H]-prazosin were also estimated by Scatchard analysis of the specific binding of [3H]-prazosin to the microsomal fractions from veins. The KD-values for [3H]-prazosin were also identical. However, Bmax-values varied considerably among the veins. The Bmax-values are proportional to the 50% effective concentrations, whose negative logs were the pD2-values, and to the efficacies. The present results suggest that the regional difference in the pD2-values for noradrenaline in the canine veins is not due to the affinities to the alpha 1-adrenoceptors but to the receptor densities.

UI MeSH Term Description Entries
D008297 Male Males
D008861 Microsomes Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed) Microsome
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
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
D011224 Prazosin A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION. Furazosin,Minipress,Pratsiol,Prazosin HCL,Prazosin Hydrochloride,HCL, Prazosin,Hydrochloride, Prazosin
D011942 Receptors, Adrenergic, alpha One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation. Adrenergic alpha-Receptor,Adrenergic alpha-Receptors,Receptors, alpha-Adrenergic,alpha-Adrenergic Receptor,alpha-Adrenergic Receptors,Receptor, Adrenergic, alpha,Adrenergic alpha Receptor,Adrenergic alpha Receptors,Receptor, alpha-Adrenergic,Receptors, alpha Adrenergic,alpha Adrenergic Receptor,alpha Adrenergic Receptors,alpha-Receptor, Adrenergic,alpha-Receptors, Adrenergic
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog
D005260 Female Females
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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