• 1991
  • The quinuclidine CP-96345 was the first nonpeptide NK 1 receptor antagonist reported by Pfizer in 1991, although its utility was limited by toxicity due to nonselective ion channel blockade. (sigmaaldrich.com)
  • mechanisms
  • However, the exact mechanisms by which nuclear receptor-cofactor interactions result in tissue-specific gene regulation are unclear. (sigmaaldrich.com)
  • Our results suggest that activation of the dopaminergic system, especially via D2 receptors may be required for the development of MAP-associated anticipatory activity increases and that N-methyl-D-aspartate receptors and sigma receptor mechanisms are also involved in the development of this behavior. (aspetjournals.org)
  • synaptic
  • Pharmacological assessments demonstrated that CamKIIαNampt(-/-) mice also display dysfunction of synaptic GluN2B (NR2B)-containing N-methyl-d-aspartate receptors (NMDARs) prior to changes in NMDAR subunit expression. (sigmaaldrich.com)
  • Synaptic activation of the receptor in many brain regions produces a slow inhibitory post-synaptic potential (ipsp) contrasting with the fast ipsp produced by GABA A receptor activation. (sigmaaldrich.com)
  • The GABA B receptor is not only located post-synaptically, but is also present on pre-synaptic terminals where its activation modulates the release of neurotransmitters. (sigmaaldrich.com)
  • neurotransmitters
  • When this effect ceases due to metabolism of cocaine, depletion of associated neurotransmitters, and receptor down-regulation (tachyphylaxis), the cocaine user may experience dysphoria, or a "crash" after the initial high. (wikipedia.org)
  • Activation
  • Despite the association between BLT receptors and the activation of inflammatory cells, disappointing clinical findings suggest that selective BLT receptor antagonists are of limited use in the treatment of asthma. (sigmaaldrich.com)
  • This is clearly evident in spinal cord where activation of the receptor on primary afferent terminals appears to be important in the modulation of nociceptive inputs, and on terminals of monosynaptic inputs to motoneurons in the production of muscle relaxation. (sigmaaldrich.com)
  • indications
  • Other possible indications of NK 1 receptor antagonists include skin disorders, inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS). (sigmaaldrich.com)
  • inflammatory
  • CysLT receptors mediate a range of other pro-inflammatory effects, such as constriction of airways and vascular smooth muscle, increased endothelial membrane permeability, leading to plasma exudation and edema, and an enhanced secretion of thick, viscous mucus. (sigmaaldrich.com)
  • roles
  • The sigma-2 receptor takes part in a number of normal-function roles, including cell proliferation, and non-neuronal, and neuronal signaling. (wikipedia.org)
  • gene
  • The control of target gene expression by nuclear receptors requires the recruitment of multiple cofactors. (sigmaaldrich.com)
  • Interestingly, the promoter for the BLT 1 receptor was later found to lie in the open reading frame of the gene for the BLT 2 receptor. (sigmaaldrich.com)
  • In humans, the σ1 receptor is encoded by the SIGMAR1 gene. (wikipedia.org)
  • The receptor has recently been identified with TMEM97, a protein for which gene and protein sequence is available that had been known to be involved in cholesterol homeostasis. (wikipedia.org)
  • interaction
  • Thus, this study introduces regulation of selective autophagy as a new role of Hrr25 and, together with other recent studies, reveals that different selective autophagy-related pathways are regulated by a uniform mechanism: phosphoregulation of the receptor-adaptor interaction. (sigmaaldrich.com)
  • found
  • Sigma-2 receptors have been found to be highly expressed in proliferating cells, including tumor cells, and to play a role in the differentiation, morphology, and survival of those cells. (wikipedia.org)
  • exclusively
  • LT receptors may couple, albeit not exclusively, via G i to inhibit adenylate cyclase, and G q/11 to modulate inositol phospholipid hydrolysis and calcium mobilization. (sigmaaldrich.com)
  • Type
  • σ-receptors were once thought to be a type of opioid receptor, because the d- stereoisomers of the benzomorphan class of opioid drugs reduced coughing, as do some other opioid derivatives such as dextromethorphan[clarification needed]. (wikipedia.org)