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Pharmacological screening of a new alpha-2 adrenergic receptor agonist, mafedine, in zebrafish

Neuroscience Letters, 2019
Pharmacological agents acting at alpha-2 adrenergic receptors are widely used in physiology and neuroscience research. Mounting evidence of their potential utility in clinical and experimental psychopharmacology, necessitates new models and novel model organisms for their screening. Here, we characterize behavioral effects of mafedine (6-oxo-1-phenyl-2-
Yuriy I. Sysoev   +5 more
openaire   +2 more sources

p-[125I]iodoclonidine is a partial agonist at the alpha 2-adrenergic receptor.

Molecular Pharmacology, 1990
The binding properties of p-[125I]iodoclonidine [( 125I]PIC) to human platelet membranes and the functional characteristics of PIC are reported. [125I]PIC bound rapidly and reversibly to platelet membranes, with a first-order association rate constant (kon) at room temperature of 8.0 +/- 2.7 x 10(6) M-1 sec-1 and a dissociation rate constant (koff) of ...
M A, Gerhardt, S M, Wade, R R, Neubig
openaire   +2 more sources

Effects of an Alpha-2 Adrenergic Receptor Agonist in Spinal Rats

1988
It is now several decades that diverse surgical and pharmacological treatments have been employed to prevent and/or ameliorate the sensory motor deficits which ensue an injury to the spinal cord. The restoration of impaired histological and physiologic parameters by compounds which are membrane stabilizers, antiinflammatory, and antioxidant, and which ...
N. E. Naftchi, R. Lehrer, J. A. Sleis
openaire   +1 more source

Peripheral nociceptive effects of α2-adrenergic receptor agonists in the rat

Neuroscience, 1995
We have previously shown that norepinephrine can produce hyperalgesia via an alpha 2-adrenergic receptor mechanism. The alpha 2-adrenergic receptor agonist clonidine has, however, also been shown to produce peripheral analgesia. In view of the multiple alpha 2-subtypes currently known (i.e.
S G, Khasar   +3 more
openaire   +2 more sources

[Selectivity of alpha 2-adrenergic agonists for the imidazoline-guanidine and alpha 2-adrenergic receptors].

Archives des maladies du coeur et des vaisseaux, 1989
Imidazolines have been proposed as highly selective drugs for alpha 2-adrenergic receptors. However, we have recently showed that the imidazoline ligand 3H-RX 781094 (idazoxan) binds to both alpha 2-receptors and imidazoline guanidinium receptive substance (IGRS) in rabbit renal proximal tubule.
V, Lachaud   +4 more
openaire   +1 more source

Management of Traumatic Brain Injury Sequelae With Alpha-2 Adrenergic Receptor Agonists

Journal of Head Trauma Rehabilitation
Objective: To describe clinical uses of the class of alpha-2 receptor agonist medications in the treatment of traumatic brain injury sequelae. Clinicians treating patients with traumatic brain injuries (TBI) will often see patients who have been prescribed alpha-2 agonists or may consider initiating use.
Jamie L. Ott, Thomas K. Watanabe
openaire   +2 more sources

Receptor interactions of imidazolines. IX. Cirazoline is an alpha-1 adrenergic agonist and an alpha-2 adrenergic antagonist.

The Journal of Pharmacology and Experimental Therapeutics, 1982
The alpha-1 and alpha-2 adrenergic effects of cirazoline were evaluated in guinea-pig aorta and field-stimulated guinea-pig ileum, respectively. Cirazoline was found to be a full agonist at alpha-1 receptors having an ED50, dissociation constant (KA) and relative efficacy similar to that of (-)-norepinephrine.
R R, Ruffolo, J E, Waddell
openaire   +2 more sources

Mechanism of agonist and antagonist binding to .alpha.2 adrenergic receptors: evidence for a precoupled receptor-guanine nucleotide protein complex

Biochemistry, 1988
The alpha 2 adrenergic receptor (AR) inhibits adenylate cyclase via an interaction with Ni, a guanine nucleotide binding protein. The early steps involved in the activation of the alpha 2 AR by agonists and the subsequent interaction with Ni are poorly understood.
R R, Neubig, R D, Gantzos, W J, Thomsen
openaire   +2 more sources

Structure—Activity Relationships for alpha-2 Adrenergic Receptor Agonists and Antagonists

1988
This chapter extends the discussion provided in Chapter 1 by providing an overview of the development of criteria for subclassification of alpha-adrenergic receptors into alpha-1 vs alpha-2 adrenergic receptor sybtypes and of more recent data suggesting the existence of subtypes of alpha-2 adrenergic receptors.
Robert R. Ruffolo   +3 more
openaire   +1 more source

Different sedimentation properties of agonist- and antagonist-labelled platelet alpha2 adrenergic receptors

Biochemical and Biophysical Research Communications, 1981
Abstract Alpha2 adrenergic receptors were solubilized from human platelet particulate preparations with digitonin. The solubilized alpha2 receptors retained the essential binding specificity characteristics of the membrane-bound receptors. The alpha2 receptors could be labelled in platelet membranes with either agonist ([3H]epinephrine) or antagonist
T, Michel   +3 more
openaire   +2 more sources

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