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Nootropic α7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators
A selective α7 nAChR-positive allosteric modulator (PAM) from a library of GABAA receptor PAMs is generated, which corrects sensory-gating deficits and improves working memory, effects consistent with cognitive enhancement in rodent models.
Characterization of the anticonvulsant properties of Ganaxolone (CCD 1042; 3α-hydroxy-3β-methyl-5α-pregnan-20-one), a selective, high-affinity, steroid modulator of the γ-aminobutyric acid(A) receptor
Ganaxolone (CCD 1042) is a 3b-methyl-substituted analog of the endogenous neuroactive steroid 3a-hydroxy-5a-pregnan20-one. Ganaxolone inhibited binding of the g-aminobutyric acid (GABA)A
Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.
The conformationally restricted, cyclic, disulfide-containing, enkephalin analogs and the bis-Pen-containing analogs provide an order of magnitude increase in delta receptor selectivity.
Steroid modulation of the chloride ionophore in rat brain: structure-activity requirements, regional dependence and mechanism of action.
In vitro studies of steroids active at the gamma-aminobutyric acidA (GABAA) receptor regulated Cl- channel labeled by [35S]-t-butylbicyclophosphorothionate reveal additional structural requirements necessary for activity, providing additional support for the hypothesis that some of these steroids may be involved in the homeostatic regulation of brain excitability via the GABAA-BZ receptor complex.
Anxiolytic activity of the progesterone metabolite 5α-pregnan-3α-ol-20-one
Abstract 3α-hydroxylated pregnane steroids have been shown to possess anesthetic, hypnotic, anticonvulsant and anxiolytic properties. In this study, metabolites of progesterone and
The estrus cycle, sensitivity to convulsants and the anticonvulsant effect of a neuroactive steroid.
  • D. Finn, K. Gee
  • Chemistry, Medicine
    The Journal of pharmacology and experimental…
  • 1 October 1994
In vivo studies evaluated estrus cycle-related differences in sensitivity to convulsants and the anticonvulsant effect of 3 alpha, 5 alpha-P to find that females in estrus were more sensitive than females in diestrus 1 or males to (+)-bicuculline and methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3- carboxylate.
A putative receptor for neurosteroids on the GABAA receptor complex: the pharmacological properties and therapeutic potential of epalons.
Based upon some of the unique characteristics of the epalons relative to barbiturates and the BZs, it is plausible that the epAlons can be developed into a novel class of therapeutic agents for the treatment of anxiety, epilepsy, and insomnia.
CCD-3693: an orally bioavailable analog of the endogenous neuroactive steroid, pregnanolone, demonstrates potent sedative hypnotic actions in the rat.
In vitro binding studies and in vivo pharmacological data confirmed that CCD-3693 was orally active in standard tests of anxiety, anticonvulsant, loss-of-righting and passive avoidance, and appeared more intrinsically efficacious in promoting NREM sleep than the benzodiazepine ligands.
Anticonvulsant steroids and the GABA/benzodiazepine receptor-chloride ionophore complex
Based on the knowledge of the structure-activity requirements for the interaction of steroids with this novel recognition site, it is conceivable that the development of new anticonvulsant steroids with high therapeutic indices can be achieved.
Differential Responses of Expressed Recombinant Human γ‐Aminobutyric AcidA Receptors to Neurosteroids
The ability to screen synthetic molecules using expressed human receptors that selectively contain individual subunit subtype combinations may prove to be a powerful tool in the development of therapeutic agents that act as allosteric modulators of the GABAA receptor and other neurotransmitter receptors as well.