Variation in Sensitivity of .ALPHA.1-Adrenoceptor Stimulants and .ALPHA.1-Adrenoceptor Mechanisms in Rabbit Arteries.
スポンサーリンク
概要
- 論文の詳細を見る
Sensitivity (pD<SUB>2</SUB> value, negative logarithm of the molar concentration producing the half maximum response) and affinity (pK<SUB>A</SUB> value, negative logarithm of dissociation constant) of norepinephrine were determined in 6 arteries from rabbits. A positive correlation was found in the pD<SUB>2</SUB> and pK<SUB>A</SUB> values of norepinephrine. The slope was not significantly different from 1. The pD<SUB>2</SUB> and pK<SUB>P</SUB> (a negative logarithm of dissociation constant of a partial agonist) values of tizanidine, an α<SUB>1</SUB>-partial agonist, were also determined. There were positive correlations between the pD<SUB>2</SUB> and pK<SUB>P</SUB> values of tizanidine and also between the two pD<SUB>2</SUB> values of norepinephrine and tizanidine. The slopes were not significantly different from 1. These results suggest that the regional differences in pD<SUB>2</SUB> values of norepinephrine and tizanidine in the arteries are partly due to the affinity and suggest that both drugs interact with one recognition site in the α<SUB>1</SUB>-adrenoceptors. The dissociation constants, KD values, and the maximum binding sites, B<SUB>max</SUB>, for [<SUP>125</SUP>I]-HEAT were also estimated by Scatchard analysis of the specific binding of [<SUP>125</SUP>I]-HEAT to the membrane fractions from rabbit arteries. The KD values for [<SUP>125</SUP>I]-HEAT were also identical. However, B<SUB>max</SUB> varied considerably among rabbit arteries. There was a positive correlation between the logarithm of B<SUB>max</SUB> and the pD<SUB>2</SUB> values for norepinephrine. The present results suggest that the regional difference in the pD<SUB>2</SUB> values for norepinephrine in rabbit arteries is due to variations in the affinities to the α<SUB>1</SUB>-adrenoceptors as well as the receptor densities.
- 公益社団法人 日本薬理学会の論文
著者
-
Koike Katsuo
Department Of Chemical Pharmacology Toho University Faculty Of Pharmaceutical Sciences
-
Takayanagi Issei
Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo:(correspo
-
Onozuka Shuji
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
関連論文
- The Characteristics of Endothelin Receptor Subtypes on Muscle Contraction and Neuro-transmission in Rat Vas Deferens
- The Effects of Several Vasopressin Receptor Antagonists on Normal Intraocular Pressure and the Intraocular Distribution of Vasopressin Receptor Subtypes
- THE ACTIONS OF SODIUM NITROPRUSSIDE AND DILTIAZEM ON CALCIUM-, POTASSIUM- AND HISTAMINE-INDUCED CONTRACTILE RESPONSES IN ISOLATED RABBIT BASILAR ARTERY, AORTA, TAENIA COLI AND TRACHEAL SMOOTH MUSCLE
- MaxiK channel-triggered negative feedback system is preserved in the urinary bladder smooth muscle from streptozotocin-induced diabetic rats
- Histopathological Study of Kidney Abnormalities in an Experimental SIADH Rat Model and Its Application to the Evaluation of the Pharmacologic Profile of VP-343, a Selective Vasopressin V_2 Receptor Antagonist
- The Therapeutic Efficacy of VP-343,a Selective Vasopressin V_2 Receptor Antagonist, in the Experimental SIADH Rat Model
- The Effects of β-Adrenoceptor Agonists on KCI-induced Rhythmic Contraction in the Ureter of Guinea Pig
- Chronotropic Effects of Optical Isomers of Ephedrine and Methylephedrine in the Isolated Rat Right Atria and in Vitro Assessment of Direct and Indirect Actions on β_1-Arenoceptors
- Assessment of Antihistaminic and Antimuscarinic Effects of Optical Isomers of Ephedrine and Methylephedrine by Receptor Binding Assay in Guinea Pig Ileal Muscle
- EFFECTS OF NICOTINE IN THE ISOLATED AIRWAY SMOOTH MUSCLE PREPARATIONS
- PHARMACOLOGICAL CHARACTERIZATION OF IONOPHORE X537A-INDUCED CONTRACTILE RESPONSES IN ISOLATED RABBIT TAENIA COLI AND AORTA
- Pharmacological Profile of VP-343,a Novel Selective Vasopressin V_2 Receptor Antagonist, in Rats
- Role of BK Channels in Testosterone-Induced Relaxation of the Aorta in Spontaneously Hypertensive Rats(Pharmacology)
- A POSSIBLE MECHANISM OF ACTION OF A BETA-ADRENERGIC PARTIAL AGONIST (CARTEOLOL) IN GUINEA PIG TAENIA CAECUM
- β-Adrenoceptors in the Detrusor of Guinea Pig Bladder
- Characteristics of Ca^ Oscillations in Ileal Longitudinal Muscle Cells of Guinea Pig
- Differences of Antagonism for a Selective α_-Adrenoceptor Antagonist BMY 7378 in the Rabbit Thoracic Aorta and Iliac Artery
- The β_2- and β_3-Adrenoceptor-Mediated Relaxation Induced by Isoprenaline and Salbutamol in Guinea Pig Taenia Caecum
- 平滑筋における薬物レセプターメカニズム : β-クロロエチルアミン親和性および非親和性レセプターメカニズム
- Signal Transduction Pathway Involved in β_3 - Adrenoceptor - Mediated Relaxation in Guinea Pig Taenia Caecum
- GREATER TENSION IS DEVELOPED AT THE SAME LEVEL OF CYTOSOLIC Ca^ CONCENTRATION IN THE PRESENCE OF CLONIDINE, AN ADRENERGIC PARTIAL AGONIST, THAN IN THE PRESENCE OF NOREPINEPHRINE
- Studies on the mechanisms underlying β-adrenoceptor-mediated relaxation of rat abdominal aorta
- Nitric Oxide (NO) Primarily Accounts for Endothelium-Dependent Component of β-Adrenoceptor-Activated Smooth Muscle Relaxation of Mouse Aorta in Response to Isoprenaline
- EFFECTS OF AGING ON ALPHA-1 AND-2 ADRENOCEPTOR MECHANISMS IN SMOOTH MUSCLES
- ALPHA_1-ADRENOCEPTOR MECHANISM AND AGING
- (+__-)-Pindolol Acts as a Partial Agonist at Atypical β-Adrenoceptors in the Guinea Pig Duodenum
- INTERACTIONS OF BEFUNOLOL, A BETA-ADRENERGIC PARTIAL AGONIST, AND ITS DERIVATIVES WITH HIGH AND LOW AFFINITY SITES IN BETA-ADRENOCEPTORS
- INTERACTION OF DYNORPHIN DERIVATIVE CONTAINING 3-NITRO-2-PYRIDINESULFENYL (Npys) GROUP WITH OPIOID RECEPTORS
- Comparison of the Inhibitory Effects of Docosahexaenoic Acid (DHA) on U46619-and Phenylephrine-Induced Contractions in Guinea-Pig Aorta(Pharmacology)
- Further Evidence that (±)-Carteolol-induced Relaxation is Mediated by β_2-Adrenoceptors but not by β_3-Adrenoceptors in the Guinea Pig Taenia Caecum
- MaxiK channel roles in blood vessel relaxations induced by endothelium-derived relaxing factors and their molecular mechanisms
- β1-Subunit of MaxiK Channel in Smooth Muscle : a Key Molecule Which Tunes Muscle Mechanical Activity
- β_1-Adrenoceptor-mediated relaxation with isoprenaline and the role of MaxiK channels in guinea-pig esophageal smooth muscle
- MaxiK Channel Mediates β_2-Adrenoceptor-activated Relaxation to Isoprenaline through cAMP-dependent and -independent Mechanisms in Guinea-pig Tracheal Smooth Muscle
- The β_3-Adrenoceptor-Mediated Relaxation Induced by Dopamine in Guinea Pig Taenia Caecum
- Effects of a New Positive Inotropic Agent with a Vasodilatory Action, 5-Methyl-6-(4-pyridyl)-2H-1,4-thiazin-3 (4H)-one (ZSY-27), on Calcium-Movement and Mechanical Response in Rabbit Thoracic Aorta
- EFFECTS OF SMOOTH MUSCLE STIMULANTS ON I-ISOPRENALINE-β-ADRENOCEPTOR INTERACTION IN TAENIA FROM GUINEA PIG CAECUM
- CHARACTERIZATION OF NOREPINEPHRINE-INDUCED CONTRACTILE RESPONSE IN ISOLATED RABBIT BASILAR ARTERY
- PHARMACOLOGICAL ACTIONS OF LEUKOTRIENES C_4,D_4 AND E_4 ON GUINEA PIG ISOLATED TAENIA CAECUM AS A PREPARATION TO STUDY LEUKOTRIENES
- THE ACTIONS OF D 600, ASPAMINOL AND PAPAVERINE ON CALCIUM-, POTASSIUM- AND HISTAMINE-INDUCED CONTRACTIONS OF ISOLATED RABBIT BASILAR ARTERY, AORTA, TAENIA COLI AND TRACHEAL SMOOTH MUSCLE
- Relationship between Cyclic Nucleotide Levels and 5-Methyl-6-(4-pyridyl)-2H-1,4-thiazin-3 (4H)-one (ZSY-27), a New Positive Inotropic Agent with a Vasodilatory Action, -Induced Relaxation of Rabbit Thoracic Aorta
- Effects of a New Positive Inotropic Agent with a Vasodilatory Action, 5-Methyl-6-(4-pyridyl)-2H-1,4-thiazin-3 (4H)-one (ZSY-27), on Agonists-Induced Contractions in the Isolated Rabbit Thoracic Aorta
- PHARMACOLOGICAL MULTIPLICITY OF RECEPTOR SITES FOR THE MAMMALIAN TACHYKININS IN RABBIT IRIS SPHINCTER MUSCLE
- Functional Contribution of Voltage-Dependent and Ca^2+-Activated K^+ (BK_ca) Channels to the Relaxation of Guinea-Pig Aorta in Response to Natriuretic Peptides
- EFFECTS OF A COMBINED STOMACHIC AND ITS INGREDIENTS ON RABBIT STOMACH MOTILITY IN SITU
- CALCIUM IONS AND RELAXATION OF INTESTINAL SMOOTH MUSCLE INDUCED BY PAPAVERINE AND ASPAMINOL
- Structure-Activity Relationship Studies of (±)- Terbutaline and (±)-Fenoterol on β_3-Adrenoceptors in the Guinea Pig Gastric Fundus
- DOPAMINE AND ITS ANTAGONISTS ON MOLLUSCAN SMOOTH MUSCLE
- DOPAMINE RECEPTOR IN ANTERIOR BYSSUS RETRACTOR MUSCLE OF MYTILUS EDULIS
- INHIBITORY ALPHA-ADRENERGIC ACTION OF PHENYLEPHRINE IN GUINEA PIG TAENIA CAECUM
- NONSPECIFIC INHIBITORY ACTION OF CHINOFORM ON GASTROINTESTINE
- INTERACTION OF MORPHINE-EPOXIDE WITH MULTIPLE OPIATE RECEPTORS
- INTERACTION OF MORPHINE AND CODEINE-EPOXIDES WITH OPIATE RECEPTOR
- SOME PHARMACOLOGICAL PROPERTIES OF MORPHINE-7,8-OXIDE (MORPHINE EPOXIDE)
- PHARMACOLOGICAL PROPERTIES OF CODEINE-7, 8-OXIDE (CODEINE EPOXIDE), A NEW METABOLITE OF CODEINE
- EFFECTS OF EPOXIDES OF HEROIN, MORPHINE AND CODEINE ON THE ELECTRICALLY STIMULATED GUINEA PIG ILEUM
- EFFECTS OF COCAINE ON Ca-MOBILITY IN MICROSOMAL FRACTION FROM RAT VAS DEFERENS
- EFFECTS OF ACETYLCHOLINE AND HISTAMINE ON MECHANICAL ACTIVITY OF RABBIT TAENIA COLI, Ca-INCORPORATION AND Ca-RELEASE IN ITS MICROSOMAL FRACTION
- NONSPECIFIC RELAXATION OF INTESTINAL SMOOTH MUSCLE INDUCED BY ANTISPASMODICS AND MOVEMENT OF CALCIUM IONS
- DRUG-INDUCED SMOOTH MUSCLE CONTRACTION WITH NO CHANGE IN THE LEVEL OF CYCLIC GMP
- INHIBITION OF Ca-MOVEMENT AND MECHANICAL MOVEMENT IN RABBIT TAENIA COLI BY A SMOOTH MUSCLE RELAXANT (SULOCTIDIL)
- EFFECTS OF SMOOTH MUSCLE RELAXANT (ASPAMINOL) ON Ca-UPTAKE BY MITOCHONDRIAL AND MICROSOMAL FRACTIONS FROM RAT UTERUS
- EFFECTS OF NONSPECIFIC SMOOTH MUSCLE RELAXANTS ON CALCIUM-UPTAKE BY MICROSOMAL FRACTION AND THEIR INHIBITORY ACTION IN RABBIT TAENIA COLI
- EFFECTS OF CALCIUM IONS AND MAGNESIUM IONS ON 5-HYDROXYTRYPTAMINE-RECEPTOR INTERACTION
- EFFECTS OF NONSPECIFIC SMOOTH MUSCLE RELAXANTS ON GLYCOGEN PHOSPHORYLASE ACTIVITY IN DEPOLARIZED TAENIA CAECUM OF GUINEA PIG
- EFFECTS OF NONSPECIFIC SMOOTH MUSCLE RELAXANTS ON TISSUE CONCENTRATIONS OF HIGH ENERGY PHOSPHATES AND MECHANICAL ACTIVITY OF NORMAL POLARIZED AND DEPOLARIZED INTESTINAL SMOOTH MUSCLES FROM GUINEA PIG
- ANTIPHOSPHODIESTERASE ACTIVITY AND NONSPECIFIC SMOOTH MUSCLE RELAXATION TESTED ON INTESTINAL SMOOTH MUSCLES
- EXTERNAL CALCIUM IONS AND MECHANICAL RESPONSES OF THE AORTA ISOLATED FROM THE CHOLESTEROL-FED RABBIT
- RELAXING ACTION OF SYNTHETIC ANTISPASMODICS ON THE INTESTINAL SMOOTH MUSCLE OF GUINEA PIG
- INTRACELLULAR CYCLIC ADENOSINE 3, 5-MONOPHOSPHATE AND RELAXING EFFECTS OF ISOPRENALINE AND PAPAVERINE ON SMOOTH MUSCLE OF INTESTINE
- POSSIBLE MECHANISMS OF STIMULATORY ACTION OF PAPAVERINE ON CALCIUM-UPTAKE BY RAT UTERINE MICROSOMAL FRACTION
- EFFECTS OF ANTI-ASTHMATIC DRUGS ON AIRWAY RESISTANCE AND PLASMA LEVEL OF CYCLIC AMP IN GUINEA PIG
- RELATIONSHIP BETWEEN THE Ba-INDUCED CONTRACTION AND CYCLIC AMP LEVELS IN THE ISOLATED LONGITUDINAL SMOOTH MUSCLE FROM GUINEA PIG ILEUM
- Adrenaline produces the relaxation of guinea-pig airway smooth muscle primarily through the mediation of β_2-adrenoceptors
- Phospholipase C Inhibitors Suppress Spontaneous Mechanical Activity of Guinea Pig Urinary Bladder Smooth Muscle(Pharmacology)
- The β_2- and β_3-Adrenoceptor-Mediated Relaxation Induced by Fenoterol in Guinea Pig Taenia Caecum
- A DUAL ACTION OF MUSCARINIC PARTIAL AGONISTS ON PUPIL SIZE OF RABBIT
- The β_3-Adrenoceptor-Mediated Relaxation Induced by Epinephrine in Guinea Pig Taenia Caecum
- Partial Agonistic Effects of Carteolol on Atypical β-Adrenoceptors in the Guinea Pig Gastric Fundus
- H2 Receptor-Mediated Positive Inotropic Effect of Histamine in Neonatal Guinea-Pig Left Atria
- RELATIONSHIP BETWEEN INTRINSIC ACTIVITY OF β-ADRENOCEPTOR AGONIST AND AMOUNT OF SPARE RECEPTORS IN GUINEA PIG TAENIA CAECUM
- PHARMACOLOGICAL PROPERTIES OF ACETYLCHOLINE RECEPTOR IN MOLLUSCAN SMOOTH MUSCLE
- INTERACTIONS OF SOME PARTIAL AGONISTS WITH BETAADRENOCEPTOR IN GUINEA-PIG TAENIA CAECUM
- Effects of aging on α_1-adrenoceptor mechanisms in the isolated mouse aortic preparation
- α_1-Adrenoceptors in the Guinea Pig Thoracic Aorta
- Update on Angiogenic Potential of Neural Stem Cells
- A DIFFERENCE IN PHARMACOLOGICAL ACTION OF R (+) AND S (-) ISOMERS OF BEFUNOLOL, BETA-ADRENOCEPTOR BLOCKER
- INTERACTION OF THE PARTIAL AGONISTS WITH BETA-ADRENOCEPTOR IN GUINEA-PIG TAENIA CAECUM
- BETA-ADRENOCEPTOR MECHANISMS IN GUINEA PIG TAENIA CAECUM
- A difference in alpha-adrenoceptor mechanisms in vasa deferential isolated from young and old rats.
- Variation in Sensitivity of .ALPHA.1-Adrenoceptor Stimulants and .ALPHA.1-Adrenoceptor Mechanisms in Rabbit Arteries.
- A Difference in Receptor Mechanisms for Muscarinic Full and Partial Agonists.
- Effect of ageing on .ALPHA.1A-adrenoceptor mechanisms in rabbit isolated bronchial preparations.
- INTERACTIONS OF R (+)- AND S (-)-ISOMERS OF BETA-ADRENERGIC PARTIAL AGONISTS, BEFUNOLOL AND CARTEOLOL, WITH BETAADRENOCEPTORS
- Characterization of Subtype of Propylbenzilylcholine Mustard (PrBCM)-Sensitive and-Resistant Muscarinic Cholinoceptors in Guinea Pig Ileal Muscle.
- Involvement of .BETA.3-Adrenoceptor in the Relaxation Response in Guinea Pig Taenia Caecum.
- A possible mechanism in interaction of a partial agonist with .BETA.-adrenoceptor in guinea-pig taenia caecum: Effects of Gpp(NH)p on its two different binding sites.
- Evidence for release of prostaglandin F2.ALPHA. in contractile response of guinea pig trachea to norepinephrine.
- Effect of aging on the response of guinea pig trachea to isoprenaline.
- Update on Angiogenic Potential of Neural Stem Cells