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Receptor antagonist article. This is not a forum for general discussion of the article's subject. |
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Agonists, inverse agonists, antagonists, functional selectivity. There are too many variations in individual definitions of all of these. I often hear inverse agonists being described as antagonists by knowledgable people in pharmacology, because when they were educated, there was nothing other than the on / off dogma associated with the terms. The problem in clarification extends too to binding sites of receptors. There should be a difference in name between agonists which work at the same binding site of a receptor and those which do not. I hereby motion that we raise this issue, whether it be here on wikipedia or in a conference to discuss this issue so that the confusion does not continue into the future.-- Carlwfbird 05:16, 26 September 2006 (UTC)
Does the non-competetive antagonist bind to a different site on the SAME RECEPTOR, or to a different receptor? Eddietoran 01:34, 31 January 2007 (UTC)
Agonists:- Drug displays both affinity and efficacy for a receptor Antagonists:- Drug displays affinity but no efficacy for a receptor
"A drug which attenuates the effect of an agonist." is not a complete sentence.
Suggestions:
"It can also be a drug which attenuates the effect of an agonist."
"It is a drug which attenuates the effect of an agonist." —Preceding unsigned comment added by Pammalamma ( talk • contribs) 18:18, 20 October 2007 (UTC)
--Pam C., technical editor —Preceding unsigned comment added by Pammalamma ( talk • contribs) 18:14, 20 October 2007 (UTC)
Is it just me or do these drugs sound like they allosterically inhibit the action of some receptors see: Surin et al Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists Neuropharmacology Volume 52, Issue 3, March 2007, Pages 744-754
Don't want to say they are incase it would be factually incorrect to do so at this point 140.203.12.241 16:14, 22 October 2007 (UTC)
Also note:
Since activation of the maximum agonist response does not require all receptors to be occupied then low concentrations of non-competitive antagonist (may not effect the ability of the agonist to produce its response but may affect the concentration required to do so) ( receptor occupancy theory see point in efficacy or Stephensn RP 1965 A modificaion of receptor theory. Br J Pharmacol 11:379-393)
This article has been selected as the current Pharmacology Collaboration of the Month. Dr. Cash 21:26, 31 October 2007 (UTC)
introduced the subsection antibiotics as antagonists of pathogens.
The following text:
Antibiotics act as antagonists which kill or inhibit the growth of pathogens that cause disease or illness. The pharmacodynamics of antibiotic action is different from the pharmacodyamics of other antagonists. [1] [2] The overall outcome of antibiotic action rather then the affintiy and efficacy of these chemotherapeutic agents is assessed. Different parameters are used to assess the activity and potency of antibiotics, the MIC or minimum inhibitory concentration of antibiotic required to completely inhibit visible growth of a micro-organism on agar or in broth. Also the MBC or minimum bactericidal concentration the concentration of antibiotic needed to kill an micro-organism on agar or in broth. The activity of antibiotics may also be time-dependant and depend on the duration of antibiotic exposure. The β lactam antibiotics, the penicillins and cephalosporins are a classic example of this. [2] Other antibiotic classes such as the quinolones and aminoglycosides lack this time-dependant effect. [2] Antibiotic effects can also persist once antibiotic has been removed or antibiotic treatment has cessed. The phenomenon is refered to the post-antibiotic effect. It represents the time taken for the micro-organism to recover after exposure to anibiotic treatment has cessed. [1] [2]
while current definitions of antagonists rely on determination of their affinity and efficacy at receptors, antibiotics are treated differently. Activity of antibiotics is assessed by direct measurement of their antimicrobial activity. Though these chemotherapeutic agents possess affinity and efficacy for their molecular targets these parameters are often ignored when determining their pharmacolgical usefulness. Was just wondering if you agree with my point of view. If not this subsection would not belong here so your free to remove it. Lilypink ( talk) 16:24, 18 November 2007 (UTC)
I would not advise including a section on antibiotics in this article, as overall, it's generally not related. Most antibiotics act by a variety of different mechanisms, usually directed at inhibiting the growth of bacteria (e.g. cell wall synthesis inhibitors, such as the beta-lactam antibiotics, or aminoglycosides, which interact at the ribosomal RNA A-site). Neither of these I would classify as a "receptor antagonist", and these are some of the more common. The above text would be misleading to the article, as it seems to say that antibiotics are a special classification of receptor antagonists, when in fact, they are completely different. I think it's best to keep the two separate. Dr. Cash ( talk) 19:10, 19 November 2007 (UTC)
Everything is referenced with seemingly reliable sources, the ones I cheched backed up the text in the article they were cited for. I can understand the text (I think - I changed the bits that were a little hard) and there are no spelling mistakes or other annoying things. It's a bit weak on images, but the one included is good.
Possible problem: Isn't ref 10 supposed to be PMID 13383117, because the current one leads to an article that doesn't exist on the homepage for Br J Pharmacol.
Narayanese ( talk) 15:15, 16 January 2008 (UTC)
{{PMC|1510558}}
to note that the full text of the original article is available free of charge.
Fvasconcellos (
t·
c) 15:23, 16 January 2008 (UTC)
I'm a college grad with a basic science (mostly physics) and heavy math background. In general I haven't had much trouble understanding writings about biochemistry, esp. neurotransmitters and psychiatric drugs, but this article was nearly incomprehensible due to the complete reliance on jargon that only a biochemist would understand. This article could be made a lot more understandable by including descriptions of how receptor antagonists work in plain English.
71.231.162.174 ( talk) 06:13, 22 May 2008 (UTC)
Please state where you feel the article fails to properly explain the topic and I'll try and clarify some of the issues raised. Thanks Lilypink ( talk) 14:52, 22 May 2008 (UTC)
I'd also like to point out that this is an extremely technical subject and a lot of the terminology is required to avoid confusion. It'd be the equivalent of me asking for the set theory article to be re-written so that somebody without graduate level maths could understand it. Oni no Akuma ( talk) 10:50, 6 January 2009 (UTC)
This whole part is rubbish:
"By definition, antagonists display no efficacy [1] to activate the receptors they bind. Antagonists do not maintain the ability to activate a receptor. Once bound, however, antagonists inhibit the function of agonists, inverse agonists, and partial agonists."
I deleted it, but just in case it comes back I advice to delete it.
Antagonist ligands has efficacy just like agonist has. It just means teh strength of effect,and not stimulus per se. —Preceding unsigned comment added by 209.2.211.170 ( talk) 12:49, 23 March 2011 (UTC)
I realise that much of this article will inevitably be technical. Nevertheless, it would be useful to have at least a few sentences in the lead that are understandable to a general audience. 86.176.208.182 ( talk) 22:11, 10 January 2014 (UTC)
What proteins would a CD4 receptor antagonist be made of? Nobody will tell me. Please help I'm going to cure aids. 73.19.14.179 ( talk) 05:49, 4 November 2022 (UTC)
This is the
talk page for discussing improvements to the
Receptor antagonist article. This is not a forum for general discussion of the article's subject. |
Article policies
|
Find sources: Google ( books · news · scholar · free images · WP refs) · FENS · JSTOR · TWL |
Receptor antagonist has been listed as one of the Natural sciences good articles under the good article criteria. If you can improve it further, please do so. If it no longer meets these criteria, you can reassess it. | ||||||||||
|
This article is rated GA-class on Wikipedia's
content assessment scale. It is of interest to the following WikiProjects: | |||||||||||||||||||||||||||
|
Agonists, inverse agonists, antagonists, functional selectivity. There are too many variations in individual definitions of all of these. I often hear inverse agonists being described as antagonists by knowledgable people in pharmacology, because when they were educated, there was nothing other than the on / off dogma associated with the terms. The problem in clarification extends too to binding sites of receptors. There should be a difference in name between agonists which work at the same binding site of a receptor and those which do not. I hereby motion that we raise this issue, whether it be here on wikipedia or in a conference to discuss this issue so that the confusion does not continue into the future.-- Carlwfbird 05:16, 26 September 2006 (UTC)
Does the non-competetive antagonist bind to a different site on the SAME RECEPTOR, or to a different receptor? Eddietoran 01:34, 31 January 2007 (UTC)
Agonists:- Drug displays both affinity and efficacy for a receptor Antagonists:- Drug displays affinity but no efficacy for a receptor
"A drug which attenuates the effect of an agonist." is not a complete sentence.
Suggestions:
"It can also be a drug which attenuates the effect of an agonist."
"It is a drug which attenuates the effect of an agonist." —Preceding unsigned comment added by Pammalamma ( talk • contribs) 18:18, 20 October 2007 (UTC)
--Pam C., technical editor —Preceding unsigned comment added by Pammalamma ( talk • contribs) 18:14, 20 October 2007 (UTC)
Is it just me or do these drugs sound like they allosterically inhibit the action of some receptors see: Surin et al Cyclothiazide selectively inhibits mGluR1 receptors interacting with a common allosteric site for non-competitive antagonists Neuropharmacology Volume 52, Issue 3, March 2007, Pages 744-754
Don't want to say they are incase it would be factually incorrect to do so at this point 140.203.12.241 16:14, 22 October 2007 (UTC)
Also note:
Since activation of the maximum agonist response does not require all receptors to be occupied then low concentrations of non-competitive antagonist (may not effect the ability of the agonist to produce its response but may affect the concentration required to do so) ( receptor occupancy theory see point in efficacy or Stephensn RP 1965 A modificaion of receptor theory. Br J Pharmacol 11:379-393)
This article has been selected as the current Pharmacology Collaboration of the Month. Dr. Cash 21:26, 31 October 2007 (UTC)
introduced the subsection antibiotics as antagonists of pathogens.
The following text:
Antibiotics act as antagonists which kill or inhibit the growth of pathogens that cause disease or illness. The pharmacodynamics of antibiotic action is different from the pharmacodyamics of other antagonists. [1] [2] The overall outcome of antibiotic action rather then the affintiy and efficacy of these chemotherapeutic agents is assessed. Different parameters are used to assess the activity and potency of antibiotics, the MIC or minimum inhibitory concentration of antibiotic required to completely inhibit visible growth of a micro-organism on agar or in broth. Also the MBC or minimum bactericidal concentration the concentration of antibiotic needed to kill an micro-organism on agar or in broth. The activity of antibiotics may also be time-dependant and depend on the duration of antibiotic exposure. The β lactam antibiotics, the penicillins and cephalosporins are a classic example of this. [2] Other antibiotic classes such as the quinolones and aminoglycosides lack this time-dependant effect. [2] Antibiotic effects can also persist once antibiotic has been removed or antibiotic treatment has cessed. The phenomenon is refered to the post-antibiotic effect. It represents the time taken for the micro-organism to recover after exposure to anibiotic treatment has cessed. [1] [2]
while current definitions of antagonists rely on determination of their affinity and efficacy at receptors, antibiotics are treated differently. Activity of antibiotics is assessed by direct measurement of their antimicrobial activity. Though these chemotherapeutic agents possess affinity and efficacy for their molecular targets these parameters are often ignored when determining their pharmacolgical usefulness. Was just wondering if you agree with my point of view. If not this subsection would not belong here so your free to remove it. Lilypink ( talk) 16:24, 18 November 2007 (UTC)
I would not advise including a section on antibiotics in this article, as overall, it's generally not related. Most antibiotics act by a variety of different mechanisms, usually directed at inhibiting the growth of bacteria (e.g. cell wall synthesis inhibitors, such as the beta-lactam antibiotics, or aminoglycosides, which interact at the ribosomal RNA A-site). Neither of these I would classify as a "receptor antagonist", and these are some of the more common. The above text would be misleading to the article, as it seems to say that antibiotics are a special classification of receptor antagonists, when in fact, they are completely different. I think it's best to keep the two separate. Dr. Cash ( talk) 19:10, 19 November 2007 (UTC)
Everything is referenced with seemingly reliable sources, the ones I cheched backed up the text in the article they were cited for. I can understand the text (I think - I changed the bits that were a little hard) and there are no spelling mistakes or other annoying things. It's a bit weak on images, but the one included is good.
Possible problem: Isn't ref 10 supposed to be PMID 13383117, because the current one leads to an article that doesn't exist on the homepage for Br J Pharmacol.
Narayanese ( talk) 15:15, 16 January 2008 (UTC)
{{PMC|1510558}}
to note that the full text of the original article is available free of charge.
Fvasconcellos (
t·
c) 15:23, 16 January 2008 (UTC)
I'm a college grad with a basic science (mostly physics) and heavy math background. In general I haven't had much trouble understanding writings about biochemistry, esp. neurotransmitters and psychiatric drugs, but this article was nearly incomprehensible due to the complete reliance on jargon that only a biochemist would understand. This article could be made a lot more understandable by including descriptions of how receptor antagonists work in plain English.
71.231.162.174 ( talk) 06:13, 22 May 2008 (UTC)
Please state where you feel the article fails to properly explain the topic and I'll try and clarify some of the issues raised. Thanks Lilypink ( talk) 14:52, 22 May 2008 (UTC)
I'd also like to point out that this is an extremely technical subject and a lot of the terminology is required to avoid confusion. It'd be the equivalent of me asking for the set theory article to be re-written so that somebody without graduate level maths could understand it. Oni no Akuma ( talk) 10:50, 6 January 2009 (UTC)
This whole part is rubbish:
"By definition, antagonists display no efficacy [1] to activate the receptors they bind. Antagonists do not maintain the ability to activate a receptor. Once bound, however, antagonists inhibit the function of agonists, inverse agonists, and partial agonists."
I deleted it, but just in case it comes back I advice to delete it.
Antagonist ligands has efficacy just like agonist has. It just means teh strength of effect,and not stimulus per se. —Preceding unsigned comment added by 209.2.211.170 ( talk) 12:49, 23 March 2011 (UTC)
I realise that much of this article will inevitably be technical. Nevertheless, it would be useful to have at least a few sentences in the lead that are understandable to a general audience. 86.176.208.182 ( talk) 22:11, 10 January 2014 (UTC)
What proteins would a CD4 receptor antagonist be made of? Nobody will tell me. Please help I'm going to cure aids. 73.19.14.179 ( talk) 05:49, 4 November 2022 (UTC)