Confirming the early studies of Jouvet and Raul Hernandez-Peon, numerous investigations have found prompt and sustained increases inREM sleepsigns when cholinergicagonistdrugs are microinjected into the pontinebrain stemof cats. The behavioral syndrome produced by this treatment is indistinguishable from th...
Cholinergic agonist and antagonist drugs modulate the growth hormone response to growth hormone-releasing hormone in the rat: evidence for mediation by som... Recently, data have been presented showing that muscarinic cholinergic agonists or antagonists can modulate, in opposite ways, GH-releasing hormo...
While drugs targeting cholinergic receptors have been demonstrated to show efficacy in preclinical models, the large range of side effects impede clinical application. Inhibitors of the acetylcholine esterase, such as Rivastigmine and Neostigmine, which enhance the bioavailability of this neurotransmitter at...
Microinjection of the GABAA receptor agonist muscimol into the Rpa decreases body temperature [39]. As stimulation of DMH cholinergic neurons decreased elevated iBAT temperature, it is possible that DMH cholinergic neurons provide inhibitory input to neurons in the Rpa. Endogenous ACh binds to both...
to prevent muscarinic receptor activation by nicotine-induced endogenous ACh release68. This ensured only the actions of nAChRs were measured and provided standardized background experimental conditions for both nicotine and ACh experiments. Other bath-applied drugs were similarly dissolved in aCSF at the...
Drugs affecting nicotinic receptors The first thing that comes to mind when nicotine is mentioned is tobacco, addiction and smoking cessation. Efforts to produce drugs to aid in this addiction (e.g. gum, spray, patches) target nicotinic receptors.Vareniclinefor smoking cessation is among the recent...
The development of M1 receptor PET ligands commenced with the synthesis of the agonist tracers [11C]xanomeline (18) and [11C]butylthio-TZTP (19).81 These tracers exhibited high affinity (K i < 10 nM) to M1 receptors and high selectivity toward M2 receptors.82 In preclinical studie...
Other bath-applied drugs were similarly dissolved in aCSF at the desired concentration (nicotine (300 nM in tLTP experiments, 10 mM in two-photon imaging experiments; Sigma-Aldrich), ACh (1 mM; Sigma-Aldrich), Galanthamine (0.1 or 1 mM; Tocris Bioscience), DHbE (10 mM; Tocris Bioscience)...
As expected, when wildtype mice were given the M1R allosteric agonist VU0357017 by systemic injection, they self-administered less cocaine than controls (Figs. 6C,D). In sharp contrast, in the CDGI knockouts, self-administration of cocaine was unaffected by VU0357017 agonist treatment (Figs. ...
sex and diet of the patient; the time of administration, route of administration, and rate of excretion of the specific compound employed; the duration of the treatment; drugs used in combination or coincidentally with the specific compound employed; and like factors well known in the medical art...