p(HBP:"alpha-3 beta-4 nAChR")

Entity

Name

alpha-3 beta-4 nAChR

Namespace

HBP

Namespace Version

20181221

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https://raw.githubusercontent.com/pharmacome/terminology/bd0996a28201cad363557315043c6392e31abf58/export/hbp-names.belns

This file encodes the article Mammalian Nicotinic Acetylcholine Receptors: From Structure to Function by Albuquerque et al, 2009

This document contains the curation of the review article Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system by Taly et al. 2009

Finally, bupropion (16, 294, 433) and UCI-30002 (514) are examples of synthetic compounds that act as noncompetitive inhibitors of different nAChRs, including those made up of the subunits alpha7, alpha4beta2, or alpha3beta4. Both compounds effectively decrease nicotine self-administration in rats (280, 514). Bupropion is presently approved as an adjunct therapy for smoking cessation. PubMed:19126755

Finally, bupropion (16, 294, 433) and UCI-30002 (514) are examples of synthetic compounds that act as noncompetitive inhibitors of different nAChRs, including those made up of the subunits alpha7, alpha4beta2, or alpha3beta4. Both compounds effectively decrease nicotine self-administration in rats (280, 514). Bupropion is presently approved as an adjunct therapy for smoking cessation. PubMed:19126755

When cRNAs encoding specific nAChR subunits are introduced into Xenopus oocytes, simple (alpha3beta4) as well as more complex (muscle alpha1beta1deltagamma) heteromeric receptors are assembled and expressed on the cell surface (341). In Xenopus oocytes, these heteromeric nAChRs are assembled and expressed with almost equivalent efficiencies as the homomeric 5HT3A receptor (341). PubMed:19126755

Such toxins are not limited to the muscle receptor as seen in the Taiwanese krate snake. This snake produces “neuronal bungarotoxin” (also referred to as 3.1 toxin or kappa-bungarotoxin; Ref. 286), which preferentially binds to and inactivates neuronal nAChRs that contain the alpha3 and beta4 subunits. In this case, the specificity of the toxin appears to in part be controlled by the subtype of beta nAChR subunit; beta2-containing nAChRs are less sensitive than beta4-containing nAChRs to inhibition by neuronal BGT. PubMed:19126755

For example, during a low degree of activation of alpha7 and alpha3beta4 nAChRs, Ca2+ can enter the cells through nAChRs or NMDA receptors and favor activation (i.e., phosphorylation) of the transcription factor CREB, which in turn modifies gene expression (82). PubMed:19126755