1 Pharmacology and Structure-Activity Relationships of α2-Adrenoceptor Antagonists

No abstract is available for this paper.

• Publication year

  1986

• Venue

  Progress in Medicinal Chemistry

• Publication date

  Unknown publication date

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1016/S0079-6468(08)70339-4
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar

• No claims are published for this paper.

• No concepts are published for this paper.

• The alpha 2-adrenoceptor selectivities and haemodynamic effects of WY26392 and yohimbine in the anaesthetised dog.

  1985cited by this paper
• Structure affinity relationships for yohimbine analogs at central α-adrenoceptors

  1985cited by this paper
• N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin -2-yl)-N- methyl-2-hydroxyethane-sulfonamide: a potent and selective alpha 2-adrenoceptor antagonist.

  1985cited by this paper
• Selective interaction of DG-5128 with a low agonist affinity state of alpha-2 adrenoceptor.

  1985cited by this paper
• The effect of yohimbine, WY 26392 and idazoxan on sympathetic nerve activity.

  1985cited by this paper
• Why do people get fat?

  1985cited by this paper
• Binding of the imidazoline UK-14, 304, a putative full alpha 2-adrenoceptor agonist, to rat cerebral cortex membranes.

  1984cited by this paper
• The ocular hypotensive action of SK&F 86466 in the conscious rabbit.

  1984cited by this paper
• POTENTIAL ANTIDEPRESSANT AGENTS. α-ARYLOXY-BENZYL DERIVATIVES OF ETHANOLAMINE AND MORPHOLINE

  1984cited by this paper
• A study of the selectivity and potency of rauwolscine, RX 781094 and RS 21361 as antagonists of alpha-1 and alpha-2 adrenoceptors.

  1984cited by this paper
• Alpha2-adrenoceptor antagonism and other pharmacological antagonist properties of some substituted benzoquinolizines and yohimbine in vitro

  1984cited by this paper
• The selectivity of DG-5128 as an α2-adrenoceptor antagonist

  1984cited by this paper
• In vitro selectivity of lisuride and other ergot derivatives for α1- and α2-adrenoceptors

  1984cited by this paper
• Studies of the α2-adrenoceptor affinity and the α2- to α1-adrenoceptor selectivity of some substituted benzoquinolizines using receptor-binding techniques

  1984cited by this paper
• Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.

  1984cited by this paper
• Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.

  1984cited by this paper
• An investigation into the selectivity of a novel series of benzoquinolizines for α2‐adrenoceptors in vivo

  1984cited by this paper
• 2‐Alkyl analogues of idazoxan (RX 781094) with enhanced antagonist potency and selectivity at central α2‐adrenoceptors in the rat

  1984cited by this paper
• Selectivity and potency of 2‐alkyl analogues of the α2‐adrenoceptor antagonist idazoxan (RX 781094) in peripheral systems

  1984cited by this paper
• Alpha-adrenoreceptor reagents. 2. Effects of modification of the 1,4-benzodioxan ring system on alpha-adrenoreceptor activity.

  1984cited by this paper
• The classification of drugs and drug receptors in isolated tissues.

  1984cited by this paper
• Comparison of the α-adrenoceptor antagonist profiles of idazoxan (RX 781094), yohimbine, rauwolscine and corynanthine

  1984cited by this paper
• Seasonal variations in drug response and staircase phenomena in atrial muscle from a hibernating rodent (Spermophilus richardsonii)

  1983cited by this paper
• synthesis and antihypertensive activity of 2-sulfonamido- and 2-sulfamido-1,3,4,6,7,11b alpha-hexahydro-2H-benzo[a]quinolizines.

  1983cited by this paper
• Partial agonist effect of 2-[2-(1,4-Benzodioxanyl)]-2-imidazoline (RX 781094) at presynaptic α2-adrenoceptors in rabbit ear artery

  1983cited by this paper
• Separation of adrenergic and non‐adrenergic contractions to field stimulation in the rat vas deferens

  1983cited by this paper
• Sgd-101-75

  1983cited by this paper
• CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist.

  1983cited by this paper
• α2‐Adrenoceptor agonists induce mydriasis in the rat by an action within the central nervous system

  1983cited by this paper
• Studies on RX 781094: a selective, potent and specific antagonist of α2‐adrenoceptors

  1983cited by this paper
• alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.

  1983cited by this paper
• The pharmacology of mianserin--an update.

  1983cited by this paper
• Evidence for pharmacological similarity between α2,‐adrenoceptors in the vas deferens and central nervous system of the rat

  1983cited by this paper
• Effects of (+)- and (−)-Mianserin on α-adrenoceptors and tyramine-induced tachycardia in rats

  1983cited by this paper
• α1‐Adrenoceptor agonist activity of α2‐adrenoceptor antagonists in the pithed rat preparation

  1983cited by this paper
• Electrophysiological demonstration of both α2-agonist and antagonist properties of RX 781094☆

  1983cited by this paper
• 6-Chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine: a potent and selective antagonist of alpha 2-adrenoceptors.

  1983cited by this paper
• Pyridinylpiperazines, a new class of selective alpha 2-adrenoceptor antagonists.

  1983cited by this paper
• Age-related changes in the control of hepatic cyclic AMP levels by alpha 1- and beta 2-adrenergic receptors in male rats.

  1983cited by this paper
• Differences in the applicability of the Easson-Stedman hypothesis to the α1- and α2-adrenergic effects of phenethylamines and imidazolines

  1983cited by this paper
• Binding of yohimbine stereoisomers to α‐adrenoceptors in rat liver and human platelets

  1983cited by this paper
• Piperazinylimidazo[1,2-a]pyrazines with selective affinity for in vitro alpha-adrenergic receptor subtypes.

  1983cited by this paper
• The effects of metal ions on the binding of a new alpha 2-adrenoceptor antagonist radioligand (3H)-RX 781094 in rat cerebral cortex.

  1983cited by this paper
• [3H]RX 781094: A new antagonist ligand labels α2-adrenoceptors in the rat brain cortex

  1983cited by this paper
• An examination of age-related changes in pre- and postsynaptic alpha-adrenoceptors in the rat isolated vas deferens.

  1983cited by this paper
• Selective alpha-2 blocking action of DG-5128 in the dog mesenteric artery and rat vas deferens.

  1983cited by this paper
• Yohimbine: a pharmacological probe for study of the alpha 2-adrenoreceptor.

  1983cited by this paper
• Evidence for more than one type of post-junctional α-Adrenoceptor

  1982cited by this paper
• Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.

  1982cited by this paper
• Presynaptic activity of the imidazolidine derivative ST 587, a highly selective alpha 1-adrenoceptor agonist.

  1982cited by this paper
• [3H]Rauwolscine and [3H]yohimbine binding to rat cerebral and human platelet membranes: possible heterogeneity of alpha 2-adrenoceptors.

  1982cited by this paper
• Nonhormonal pharmacological treatment of organic impotence.

  1982cited by this paper
• Comparative pharmacology of mianserin, its main metabolites and 6-azamianserin

  1982cited by this paper
• Binding characteristics of [3H]guanfacine to rat brain alpha-adrenoceptors. Comparison with [3H]clonidine.

  1982cited by this paper
• The Schild regression in the process of receptor classification.

  1982cited by this paper
• Stereospecific blockade of α2‐adrenoceptors by (+)‐butaclamol: implications for the characterization of dopamine receptors

  1982cited by this paper
• alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.

  1982cited by this paper
• Insulin releasing action of 2-[2-(4,5-dihydro-1H-imadazol-2-yl)-1-phenylethyl] pyridine dihydrochloride sesquihydrate (DG-5128), a new, orally effective hypoglycaemic agent.

  1982cited by this paper
• Comparison of crystallographic and quantum mechanical analysis with biological data on clonidine and some related analogues.

  1982cited by this paper
• Lowering of blood pressure in hypertensive rats by SKF 64139 and SKF 72223.

  1982cited by this paper
• Dietary Sodium and Renal α2-Adrenergic Receptors in Dahl Hypertensive Rats

  1982cited by this paper
• Stereochemical requirements of a2-adrenergic receptors for a-methyl substituted phenethylamines

  1982cited by this paper
• Characterization of physiological agonist selectivity of human fat cell α2-adrenoceptors: Adrenaline is the major stimulant of the α2-adrenoceptors

  1982cited by this paper
• Affinity chromatography of human platelet α2-adrenergic receptors

  1982cited by this paper
• α2‐Adrenoceptor‐blocking action of the phenylethanolamine‐N‐methyltransferase inhibitor SKF 64139

  1981cited by this paper
• Presynaptic adrenergic receptor sensitivity in depression. The effect of long-term desipramine treatment.

  1981cited by this paper
• Comparative study on the effects of a hypoglycemic 2-substituted-2-imidazoline derivative (DG-5128) and tolbutamide on insulin secretion from and insulin synthesis in the isolated rat pancreatic islets.

  1981cited by this paper
• Alpha 1- and alpha 2-adrenoceptors: pharmacology and clinical implications.

  1981cited by this paper
• The effect of selective α1- and α2-adrenoceptor stimulation on intraocular pressure in the conscious rabbit

  1981cited by this paper
• Pre- and postsynaptic alpha adrenoceptor selectivity studies with yohimbine and its two diastereoisomers rauwolscine and corynanthine in the anesthetized dog.

  1981cited by this paper
• Alpha-adrenoceptor subclassification.

  1981cited by this paper
• The tetracyclic antidepressant mianserin: evaluation of its blockade of presynaptic alpha-adrenoceptors in a self-stimulation model using clonidine.

  1981cited by this paper
• 2‐(2‐(1,4‐BENZODIOXANYL))‐2‐IMIDAZOLINE HYDROCHLORIDE

  1981cited by this paper
• Characterization of alpha-adrenoceptors participating in the central hypotensive and sedative effects of clonidine using yohimbine, rauwolscine and corynanthine.

  1981cited by this paper
• Functional characterization of central α-adrenoceptors by yohimbine diastereomers

  1981cited by this paper
• Presynaptic α‐block and inhibition of noradrenaline and 5‐hydroxytryptamine reuptake by a series of compounds related to mianserin

  1981cited by this paper
• Human platelet α2-adrenergic receptors: Labeling with 3H-yohimbine, a selective antagonist ligand

  1981cited by this paper
• α-Adrenoceptor subclassification

  1981cited by this paper
• The influence of drugs on disseminated intravascular coagulation (DIC). V. Effects of alpha-adrenoceptor blocking agents on thrombin-induced DIC in rats.

  1981cited by this paper
• Effects of acutely and chronically administered antidepressants on the clonidine-induced decrease in rat brain 3-methoxy-4-hydroxyphenylethylene-glycol sulphate content.

  1981cited by this paper
• Tetramine disulfides: a new tool in α-adrenergic pharmacology

  1981cited by this paper
• [3H]rauwolscine (α-yohimbine): A specific antagonist radioligand for brain α2-adrenergic receptors

  1981cited by this paper
• α2 andrenoreceptor affinity of some inhibitors of norepinephrine N-methyltransferase

  1981cited by this paper
• A further attempt to characterize the α2-adrenoceptor blocking properties of (imidazolyl-2)-2-benzodioxane 1–4 (170 150) in pithed rats

  1981cited by this paper
• MINI-REVIEW THE POSTSYNAPTIC α2-ADRENORECEPTOR

  1981cited by this paper
• An electropharmacological analyses of the effects of some drugs on neuromuscular transmission in the vas deferens of the guinea-pig.

  1981cited by this paper
• Acceleration of β-receptor desensitization in combined administration of antidepressants and phenoxybenzamine

  1981cited by this paper
• α2-Adrenoceptors modulating insulin release from isolated pancreatic islets

  1980cited by this paper
• Pharmacological properties of some "second generation" antidepressant drugs.

  1980cited by this paper
• Alpha-adrenergic receptor subtypes.

  1980cited by this paper
• Cyclic guanidines. X. Synthesis of 2-(2,2-disubstituted ethenyl- and ethyl)-2-imidazolines as potent hypoglycemics.

  1980cited by this paper
• Potentiation of responses to adrenergic nerve stimulation in isolated rat atria during chronic tricyclic antidepressant administration.

  1980cited by this paper
• Radioligand binding studies of adrenergic receptors: new insights into molecular and physiological regulation.

  1980cited by this paper
• EVALUATION OF THE SELECTIVITY OF α-ADRENORECEPTOR BLOCKING DRUGS FOR POSTSYNAPTIC α1- AND α2-ADRENORECEPTORS IN A SIMPLE ANIMAL MODEL

  1980cited by this paper
• An examination of factors influencing adrenergic transmission in the pithed rat, with special reference to noradrenaline uptake mechanisms and post-junctional α-adrenoceptors

  1980cited by this paper
• Cardio-selective beta adrenergic stimulation with prenalterol in the conscious dog.

  1980cited by this paper
• Functional evidence for subsensitivity of noradrenergic alpha 2 receptors after chronic desipramine treatment.

  1980cited by this paper
• Rapid desensitization of cerebral cortical beta-adrenergic receptors induced by desmethylimipramine and phenoxybenzamine.

  1980cited by this paper
• The blockade of α2-adrenoceptors by the PNMT inhibitor SK&F 64139

  1980cited by this paper
• COMPARISON OF MIANSERIN WITH DESIPRAMINE, MAPROTILINE AND PHENTOLAMINE ON CARDIAC PRESYNAPTIC AND VASCULAR POSTSYNAPTIC α‐ADRENOCEPTORS AND NORADRENALINE REUPTAKE IN PITHED NORMOTENSIVE RATS

  1980cited by this paper

• Synthesis & biological evaluation of neuroprotective molecules with polycyclic scaffolds

  2017cites this paper
• Synthesis and biological studies of yohimbine derivatives on human α2C-adrenergic receptors

  2005cites this paper
• Variable selection and specification of robust QSAR models from multicollinear data: arylpiperazinyl derivatives with affinity and selectivity for α2-adrenoceptors

  2004cites this paper
• &agr;-1 and &agr;-2 Adrenergic Antagonists Relieve Thermal Hyperalgesia in Experimental Mononeuropathy from Chronic Constriction Injury

  2001cites this paper
• The vascular effects of topical and intravenous alpha2-adrenoceptor agonist clonidine on canine pial microcirculation.

  1998cites this paper
• Current Research in Anesthesia and Trends in Clinical Applications

  1997cites this paper
• Synthesis of Benzodioxinopyrroles as selective α2-adrenoceptor antagonists

  1995cites this paper
• Mechanisms of Dexmedetomidine-Induced Cerebrovascular Effects in Canine In Vivo Experiments

  1995cites this paper
• Biochemical Strategies for the Development of Antidepressants

  1994cites this paper
• Nomenclature and Methodology

  1993cites this paper
• The pharmacology of RS‐15385‐197, a potent and selective α2‐adrenoceptor antagonist

  1993cites this paper
• Third‐generation antidepressants

  1993cites this paper
• Heterogeneity of α2-Adrenoceptors: Clinical Aspects

  1992cites this paper
• Heterocycles with a Benzothiadiazeypine Moiety. I. Synthesis of Pyrrolo[1,2-b]-s-triazolo[3,4-d] [1,2,5]benzothiadiazepine 5,5-Dioxide

  1992cites this paper
• Synthesis, anticonvulsant and antihypertensive activity of diastereomeric 9,10-dimethoxy-1,3,4,6,7,11b-hexahydrospiro-[benzo[a]quinolizin-2,4-imidazolidine]2',5'-diones

  1992cites this paper
• Synthesis of 1′-substituted and 1′,3′-disubstituted (±)-2R*, 11bS*-9,10-Dimethoxy-1,3,4,6,7,11 b-Hexahydrospiro-[benzo[a]quinolizin-2,5′-imidazolidine]-2′,4′-diones

  1991cites this paper
• Synthesis of new fenmetazole analogues with potential mixed α2-adrenergic antagonistic activity and noradrenaline-uptake inhibiting properties

  1991cites this paper
• Molecular aspects of the receptor activation by imidazolines: an overview.

  1991cites this paper
• Research of potential antidepressant drugs with α2-adrenoreceptor antagonist and NA-uptake inhibiting properties: synthesis of 2-(1-hydroxy-2-phenoxy-2-phenyl)ethyl-4,5-dihydro-1H-imidazole derivatives

  1990cites this paper
• Alpha-Adrenoceptors in Arrhythmogenesis

  1989cites this paper
• Chapter 3. Antidepressant Agents

  1989cites this paper
• Chapter 3 Antidepressant Agents

  1987cites this paper