*  DiVA - Search result
ALLO is a neurosteroid, produced in the CNS and a GABAA receptor agonist. ALLO modulates the general inhibitory system in the ... To avoid adverse effects when high dosages of GnRH agonists are used, add-back hormone replacement therapy is recommended. ... ALLO is a neurosteroid, produced in the CNS and a GABAA receptor agonist. ALLO modulates the general inhibitory system in the ... ALLO is a neurosteroid, produced in the CNS and a GABA(A) receptor agonist. ALLO modulates the general inhibitory system in the ...
  http://umu.diva-portal.org/smash/resultList.jsf?af=%5B%5D&aq=%5B%5B%7B%22personId%22%3A%22authority-person%3A4528%22%7D%5D%5D&aqe=%5B%5D&aq2=%5B%5B%5D%5D&language=en&query=
*  Plus it
2, application of a GABAB receptor agonist baclofen (25 μM) reduced the peak currents with an average 16.33 ± 2.88% (n = 7) ... In contrast, FK960 showed only modest inhibition on the reduction in Ca2+currents produced by baclofen, an agonist of GABAB ... Recently, an occluded inhibition of Ca2+ channels by activation of two types of transmitter receptor by opioid agonists and ... Inhibitory effect of FK960 was more robust than that induced by depolarizing prepulse, which resulted in the recovery from ...
  http://jpet.aspetjournals.org/content/308/1/120
*  Plus it
2004) Opioid receptor subtype antagonists differentially alter GABA agonist-induced feeding elicited from either the nucleus ... intra-VTA GABAA receptor antagonists produce conditioned place preference (Laviolette and van der Kooy, 2004; Laviolette et al ... inhibitory control of midbrain DA neurons can robustly control behavior. For example, microinjection of a GABAA receptor ... Because MOR agonists' ability to inhibit GABA release onto VTA DA neurons is implicated in reward, and the VP inputs synapse ...
  http://www.jneurosci.org/content/33/15/6454
*  Nitrazepam - Wikipedia
... causing an enhanced binding of GABA to GABAA receptors. GABA is a major inhibitory neurotransmitter in the brain, involved in ... It is an agonist for both central benzodiazepine receptors and to the peripheral-type benzodiazepine receptors found in rat ... and long-acting benzodiazepine-receptor agonists with different receptor selectivity on motor coordination and muscle ... Discontinuation of nitrazepam produced rebound insomnia after short-term single nightly dose therapy. Benzodiazepines require ...
  https://en.wikipedia.org/wiki/Nitrazepam
*  Muscimol - Wikipedia
Muscimol is a potent GABAA agonist, activating the receptor for the brain's principal inhibitory neurotransmitter, GABA. ... Pharmacology of gamma-aminobutyric acidA and gamma-aminobutyric acidB receptor agonists and antagonists". Molecular ... Muscimol is produced in the mushrooms Amanita muscaria (fly agaric) and Amanita pantherina, along with muscarine, muscazone, ... While muscimol is normally thought of as a selective GABAA agonist, it is also a partial agonist at the GABAA-rho receptor, and ...
  https://en.wikipedia.org/wiki/Muscimol
*  Brain stimulation reward - Wikipedia
... while kappa-opioid receptor (KOR) agonists generally produce a dysphoric state. Morphine, a MOR agonist, was one of the ... GABAergic transmission is inhibitory, and the two main receptors for GABA are GABAA and GABAB. Drugs which act on GABAA ... The effects of delta opioid receptor (DOR) agonists/antagonists on ICSS are less clear. One DOR agonist, SNC80, has been found ... Opioid receptor antagonists, such as naloxone, can reverse the effects of both opioid receptor agonists on ICSS responding and ...
  https://en.wikipedia.org/wiki/Brain_stimulation_reward
*  GABAB Receptors | China-Mainland | Sigma-Aldrich
... although they fail to produce any receptor functionality.. A variety of agonists and antagonists for the GABAB receptor have ... The GABAB receptor was first recognized over 20 years ago, although the selective agonist for the receptor, p-β-chloro-phenyl- ... Synaptic activation of the receptor in many brain regions produces a slow inhibitory post-synaptic potential (ipsp) contrasting ... Jones, K.A., et al., GABAB receptors function as a heteromeric assembly of the subunits GABABR1 and GABABR2., Nature, 396, 674- ...
  https://www.sigmaaldrich.com/china-mainland/zh/technical-documents/articles/biology/rbi-handbook/non-peptide-receptors-synthesis-and-metabolism/gabab-receptors.html
*  Cardiovascular response to group I metabotropic glutamate receptor activation in NTS | Regulatory, Integrative and Comparative...
... or inhibition of GABA effects. Also in this study, equal concentrations of DHPG and the general mGluR agonist ACPD produced ... Both agonists have been shown to be selective for mGluRs and devoid of actions at other, non-mGluR, receptors (7,26). In the ... 1995) Multiple presynaptic metabotropic glutamate receptors modulate excitatory and inhibitory synaptic transmission in ... 1993) Activation of metabotropic glutamate receptors produces reciprocal regulation of ionotropic glutamate and GABA responses ...
  http://ajpregu.physiology.org/content/276/5/R1469
*  Characterization of the Potent and Highly Selective A2A Receptor Antagonists Preladenant and SCH 412348 [7-[2-[4-2,4...
A2A antagonists facilitate intrastriatal GABA release (Ferré et al., 1997), helping to restore the indirect inhibitory output ... 6B). SCH 412348 (0.01, 0.03, 1 mg/kg) produced a dose-dependent occupancy of striatal A2A receptors as measured by in an ex ... Maj J, Rogóz Z, Skuza G, and Kołodziejczyk K (1997) The behavioural effects of pramipexole, a novel dopamine receptor agonist. ... Cantor CR and Stern MB (2002) Dopamine agonists and sleep in Parkinson's disease. Neurology 58: S71-S78. ...
  http://jpet.aspetjournals.org/content/330/1/294.long
*  Communication networks in the brain: neurons, receptors, neurotransmitters, and alcohol. - Free Online Library
... receptors, neurotransmitters, and alcohol. by 'Alcohol Research & Health'; Health, general Alcoholism Health aspects ... receptors are sensitive to very low levels of extracellular GABA, and thus they often produce a continuous inhibitory tone that ... is a specific agonist for the AMPA receptor. (4) NMDA (N-methyl-D-aspartic acid) is a specific agonist at the NMDA receptor and ... Indeed, a number of synthetic agonists have been developed for this receptor, and they produce strong intoxication, movement ...
  https://www.thefreelibrary.com/Communication+networks+in+the+brain%3A+neurons%2C+receptors%2C+...-a0193246752
*  GABA receptor - Wikipedia
Further openings via GABA binding to the receptor then produce inhibitory responses. Over-excitation of this receptor induces ... Additional information on GABAB receptors has been reviewed elsewhere. GABA agonist GABA antagonist Kuffler SW, Edwards C ( ... This mechanism is responsible for the sedative effects of GABAA allosteric agonists. In addition, activation of GABA receptors ... Although the term "GABAС receptor" is frequently used, GABAС may be viewed as a variant within the GABAA receptor family. ...
  https://en.wikipedia.org/wiki/GABA_receptor
*  Recent Advances in the Visualization and Quantification of Benzodiazepine Receptors | Springer for Research & Development
... anticonvulsant and muscle relaxant effects of the benzodiazepines are mediated by the inhibitory neurotransmitter GABA (γ- ... either the affinity of GABA for its receptor or the coupling between the GABA receptor and the chloride channel. Mixed agonists ... agonists, which produce the characteristic therapeutic effects of the benzodiazepines; inverse agonists, which produce ... Photoaffinity labeling of benzodiazepine receptors with a partial inverse agonist. Eur. J. Pharmacol. (in press).Google Scholar ...
  https://rd.springer.com/chapter/10.1007/978-1-4613-2139-2_27
*  N,N′-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and Structurally Related Compounds: Novel...
The high agonist-affinity state of the GABAB receptor can be directly labeled by the agonist radioligand [3H]APPA. We made use ... γS Binding by Agonists Activating Native and Recombinant GABAB Receptors. As shown in Fig. 2, GABA stimulated the binding of [ ... Whereas GABAA receptors form a chloride-permeable ion channel that elicits short-lasting inhibitory postsynaptic potentials, ... This effect is reversed by the competitive GABAB receptor antagonist CGP55845A and is produced most likely by enhancing the ...
  http://jpet.aspetjournals.org/content/307/1/322.long
*  Glycine blocks long-term potentiation of GABAergic synapses in the ventral tegmental area
GABAA receptor. GlyR. glycine receptor. HFS. high frequency stimulation. IPSC. inhibitory postsynaptic current. LTPGABA. long- ... an agonist of NMDA-type glutamate receptors. Thus, the blockade of LTPGABA by glycine is probably resulted from suppressing ... LTPGABA is known to be produced by a heterosynaptic mechanism, requiring the activation of postsynaptic NMDARs at glutamate ... The sources of endogenous GlyR agonists in the VTA are unclear. Glycine-releasing neurons are sparse in rostral areas of the ...
  http://pubmedcentralcanada.ca/pmcc/articles/PMC4753108/
*  benzo.org.uk : Benzodiazepine overdose: are specific antagonists useful? Dr C Heather Ashton, 1985
GABA) receptor complex. Occupation of these sites by benzodiazepines enhances the inhibitory (hyperpolarising) effects of GABA ... Yet others are termed "inverse agonists": they bind to benzodiazepine receptors but produce opposite, anxiogenic, stimulant, ... Of the benzodiazepine agonist-antagonists, the most studied is Ro 15-1788, a synthetic imidazodiazepine which has little ... Toffano G, Leon A, Massotti M, Guidotti A, Costa E. GABA-modulin, a regulatory protein for GABA receptors. In: Pepeu G, Kuhar ...
  https://www.benzo.org.uk/azbod1.htm
*  Patent US6862479 - Spinal cord stimulation as a therapy for sexual dysfunction - Google Patents
Inhibitory neurotransmitter agonists, such as GABA agonists (e.g., diazepam), generally have an inhibitory effect. Excitatory ... wherein the stimulating drug comprises one or more of an adrenergic receptor antagonist and a GABA agonist. ... SCU 160 is commanded to produce a series of inhibitory electrical stimulation pulses with gradually increasing amplitude up to ... wherein the stimulating drug comprises one or more of an adrenergic receptor agonist and a GABA antagonist. ...
  http://www.google.com/patents/US6862479?dq=snorkel
*  Allopregnanolone - Wikipedia
GABA) at GABAA receptor. Allopregnanolone has effects similar to those of other positive allosteric modulators of the GABA ... Endogenously produced allopregnanolone exerts a pivotal neurophysiological role by fine-tuning of GABAA receptor and modulating ... In addition, allopregnanolone has recently been found to be an agonist of the newly discovered membrane progesterone receptors ... While allopregnanolone, like other inhibitory neurosteroids such as THDOC, positively modulates all GABAA receptor isoforms, ...
  https://en.wikipedia.org/wiki/Allopregnanolone
*  Patente US7660631 - Methods and systems for electrical and/or drug stimulation as a therapy for ... - Google Patentes
... producing electrical pulses delivered via electrodes and/or producing drug infusion pulses, wherein the stimulating drug(s) are ... while inhibitory neurotransmitters (e.g., gamma-aminobutyric acid, a.k.a. GABA), agonists thereof, and agents that act to ... and/or nitric oxide or an agonist thereof, possibly in gradually increasing amounts, and possibly while producing a series of ... guanylyl cyclase NO receptor agonists, and cGMP. Therapeutic substances may include traditional agents used in intracavernosal ...
  http://www.google.es/patents/US7660631?dq=flatulence
*  Overdose - Drugs of Abuse - Renal and Urology News
Tolerance develops with chronic use as excitatory NMDA receptors are upregulated and inhibitory GABA receptors are down- ... Ethanol acts as a GABAergic agonist that, by acting on the GABA Areceptor, enables transmembrane flux of chloride ions ... Long-acting opiate receptor agonists with low euphoric effects such as methadone and buprenorphine can be prescribed as part of ... can produce deafness, injury to the fetus, and metabolic acidosis.. Paint pigment. inhalation can result in chronic lung ...
  https://www.renalandurologynews.com/pediatrics/overdose--drugs-of-abuse/article/624764/
*  GABAA receptor - Wikipedia
Orthosteric agonists: GABA, gaboxadol, isoguvacine, muscimol, progabide, piperidine-4-sulfonic acid (partial agonist). ... The minimal requirement to produce a GABA-gated ion channel is the inclusion of an α and a β subunit. The most common GABAA ... This potentiates the inhibitory effect of the available GABA leading to sedative and anxiolytic effects.[citation needed] ... 4-Iodopropofol GABA receptor GABAB receptor GABAA-ρ receptor Gephyrin Glycine receptor GABAA receptor positive allosteric ...
  https://en.wikipedia.org/wiki/GABAA_receptor
*  GABA receptor agonist - Wikipedia
A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative ... Alcohol is an indirect GABA agonist. GABA is the major inhibitory neurotransmitter in the brain, and GABA-like drugs are used ... binding to GABA receptors and inhibiting neuronal signaling. GABA agonists at the US National Library of Medicine Medical ... GABA-α and GABAreceptors produce sedative and hypnotic effects and have anti-convulsion properties. GABAreceptors too ...
  https://en.wikipedia.org/wiki/GABA_receptor_agonist
*  Ligand-gated ion channel - Wikipedia
GABA receptors are major inhibitory neurotransmitter expressed in the major interneurons in animal cortex. GABAA receptors are ... which acts as a selective agonist at these receptors. When the NMDA receptor is activated by the binding of two co-agonists, ... They activate an intracellular second messenger cascade to produce an excitatory/inhibitory response. They are found in mammals ... GABA (gamma-aminobutyric acid), the endogenous ligand for these receptors, is the major inhibitory neurotransmitter in the ...
  https://en.wikipedia.org/wiki/Ligand-gated_ion_channel
*  Pentobarbital Enhances GABAergic Neurotransmission to Cardiac Parasympathetic Neurons, Which Is Prevented by Expression of...
8,12,16 Expression of the ε subunit alone does not produce functional GABAAor glycine receptors, indicating that this subunit ... of the ε subunit into the native GABAAreceptors in these neurons and confers barbiturate insensitivity to the inhibitory ... or holding current in the absence of an agonist. 15,16 This current is likely caused by the increased spontaneous single- ... results are unclear but could be due to different methods for examining potentiation with exogenous application of agonists. ...
  http://anesthesiology.pubs.asahq.org/article.aspx?articleid=1944163
*  Receptor Subtypes Involved in the Presynaptic and Postsynaptic Actions of Dopamine on Striatal Interneurons | Journal of...
D2 receptors mediate the inhibitory action of DA on GABAergic inputs to striatal interneurons. GABA-mediated inputs to both LA ... receptor agonist quinpirole in two distinct mutants lacking D2L receptors and expressing variable contents of D2S receptors. ... striatal LA interneurons already argued that D5 receptors mediate the electrophysiological actions of D1-like receptor agonists ... action potentials evoked in an FS interneuron have been found capable of producing stronger GABA-mediated synaptic events in ...
  http://www.jneurosci.org/content/23/15/6245
*  GABAA receptor positive allosteric modulator - Wikipedia
However, they have no effect if GABA or another agonist is not present. Unlike GABAA receptor agonists, GABAA PAMs do not bind ... GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open ... Exchanging S for O atom in position 2 produces thiobarbiturates, which are more lipid-soluble than the oxybarbiturates. In ... GABA agonist GABA antagonist GABA receptor López-Muñoz F, Ucha-Udabe R, Alamo C (Dec 2005). "The history of barbiturates a ...
  https://en.wikipedia.org/wiki/GABAA_receptor_positive_allosteric_modulator