RECENT ADVANCES IN RECEPTOR CHEMISTRY

@inproceedings{Melchiorre1988RECENTAI,
  title={RECENT ADVANCES IN RECEPTOR CHEMISTRY},
  author={Carlo Melchiorre and Mario Giannella},
  year={1988}
}
Synthesis and Anticalcium Activity of New Compounds Containing the 2 , 3-Dihydro-l , 4-dioxino [ 2 , 3-blpyridine System
'~aboratori de Quimica Farmaceutica, Fac. Farmacia, Universitat de Barcelona, Avda. Diagonal 643, 08028 Barcelona (Spain). Telephone: 934024534; Fax: 934035941 ; E-mail: mdpujol @farmacia.far.ub.es.
The Camerino symposium series (1978–2013): a privileged observatory of receptorology development
TLDR
The organizers of the Camerino Receptor Symposia survey the development of receptorology, which sees the acceptance of terms such as G-protein, auto- and heteroreceptors, site-directed mutagenesis, chimeric receptors, constitutive activity, inverse agonism, and orphan receptors.
Clozapine, atypical antipsychotics, and the benefits of fast-off D2 dopamine receptor antagonism
TLDR
Simulations are presented to find out whether surmountable antagonism is necessary to allow sufficient D2 receptor stimulation by endogenous dopamine in the striatum during sub-second bursts in dopamine concentration or rather during much slower, activity-related increases thereof.
Chemical Modification of At Adenosine Receptors in Rat Brain Membranes
TLDR
It is concluded that agonists and antagonists oocupy different domains at the binding site, and the absence of bydrophilic amino acids frout the recognition site of the receptor apart from histidine suggests an explanation for the Iack of hydrophilic ligands with high affinity for At receptors.
Microbial glucosylmuramyldipeptides as efficient symbiotic adaptogenes and potential drugs for the therapy of senile disorders
I. Metchnikoff, awarded the Nobel Prize in 1908 for discovery of the protective role of phagocytosis and development of the cell theory of immunity, was also an enthusiast of the idea of increasing
Natural immuno adjuvant muramyl dipeptide as a substrate and regulator of cytochrome P-450 function
TLDR
It seems extremely interesting to investigate the possibility of direct interaction with the cytochrome P-450 molecule of a powerful natural immunoadjuvant, muramyl dipeptide (MDP), which is involved in the recognition of images of chemical compounds that have penetrated into the organism and prepares their encoding and introduction into the memory system.
Phenoxybenzamine and Benextramine, but Not 4-Diphenylacetoxy-N-[2-chloroethyl]piperidine Hydrochloride, Display Irreversible Noncompetitive Antagonism at G Protein-Coupled Receptors
TLDR
Benextramine noncompetitively inhibits agonist-induced responses at three different GPCR types that signal via three families of G proteins (Gi/o, Gs, and Gq/11), and the presence of significant irreversible noncompetitive antagonism may influence the interpretation of results under the experimental conditions used.
Selective muscarinic ligands (a review)
TLDR
It is shown that muscarinic cholinergic receptors (M-ChR), which provide for the innervation of the most varied organs and tissues, are identical, despite the fact that the effects produced when they are stimulated are extremely varied.
Structure-activity studies of new imidazolines on adrenoceptors of rat aorta and human platelets
TLDR
The action of new imidazolines on rat aorta appears to be mediated mainly by the activation of the α1-adrenoceptor, which indicates a slightly different mode of interaction of agonists with the transduction process.
Iodine labelling of sea anemone toxin II, and binding to normal and denervated diaphragm
TLDR
Sea anemone toxin II (ATX II) which keeps the activated sodium channels open, can be labelled at its histidine residues with 125I up to a specific radioactivity of 500 Ci/mmole, establishing the usefulness of 125I-ATX for labelling sodium channels in excitable membranes.
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