New mutants to explore nicotinic receptor functions
Article Abstract:
Nicotinic receptors that are attached to ion-channels has been studied using recombinant DNA technology, affinity labelling and site-directed mutagenesis experiments. The results show that allosteric properties affect the functional behavior of these receptor-gated ion-channels. Moreover, photolabelling experiments on the mouse muscle utilizing channel blockers such as chlorpromazine and triphenylmethyl phosphonium reveal that amino acid alpha-, beta-, gamma- and delta-nicotinic acetylcholine receptor subunits have significant roles in ligand binding and ion translocation.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1992
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Pharmacological effects of drug conjugates: is morphine 6-glucuronide an exception?
Article Abstract:
The 6- and 3-glucuronide conjugates of morphine exhibit stronger pharmacological activity than natural morphine. Similarly, sulfate conjugates have been found to feature higher pharmacological activity than their unconjugated forms. The potency of these drugs is in contrast to the pharmacological effect that usually occurs in drug conjugates. It seems that certain factors such as receptor-drug interactions and chemical solubility affect drug conjugation processes and development with regards to the drug's chemical structure and pharmacological activity.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1992
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Pharmacological and functional diversity of neuronal nicotinic acetylcholine receptors
Article Abstract:
Oocyte expression studies show that the nicotinic receptor subunit gene family can exhibit pharmacologically and functionally varied receptor-gated ion channels. The combination of the neuronal alpha and beta subunits with differential subunit stoichiometries promotes the diversification of neuronal nicotinic receptors. This subunit combination has led to the introduction of a new neuronal nicotinic receptor class which features neither specific neuronal-bungarotoxin sensitivity nor specific neuronal-bungarotoxin insensitivity.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1991
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