{"id":150,"date":"2016-03-07T14:53:07","date_gmt":"2016-03-07T13:53:07","guid":{"rendered":"https:\/\/filozofia.nett.to\/psychedelika\/understanding-psychoactive-substances-receptors-and-affinity\/"},"modified":"2026-02-04T14:56:40","modified_gmt":"2026-02-04T13:56:40","slug":"understanding-psychoactive-substances-receptors-and-affinity","status":"publish","type":"post","link":"https:\/\/filozofia.nett.to\/psychedelika\/en\/understanding-psychoactive-substances-receptors-and-affinity\/","title":{"rendered":"Understanding psychoactive substances: receptors and affinity"},"content":{"rendered":"<div id=\"ez-toc-container\" class=\"ez-toc-v2_0_83 counter-hierarchy ez-toc-counter ez-toc-grey ez-toc-container-direction\">\n<div class=\"ez-toc-title-container\">\n<p class=\"ez-toc-title\" style=\"cursor:inherit\">Table of Contents<\/p>\n<span class=\"ez-toc-title-toggle\"><a href=\"#\" class=\"ez-toc-pull-right ez-toc-btn ez-toc-btn-xs ez-toc-btn-default ez-toc-toggle\" aria-label=\"Toggle Table of Content\"><span class=\"ez-toc-js-icon-con\"><span class=\"\"><span class=\"eztoc-hide\" style=\"display:none;\">Toggle<\/span><span class=\"ez-toc-icon-toggle-span\"><svg style=\"fill: #999;color:#999\" xmlns=\"http:\/\/www.w3.org\/2000\/svg\" class=\"list-377408\" width=\"20px\" height=\"20px\" viewBox=\"0 0 24 24\" fill=\"none\"><path d=\"M6 6H4v2h2V6zm14 0H8v2h12V6zM4 11h2v2H4v-2zm16 0H8v2h12v-2zM4 16h2v2H4v-2zm16 0H8v2h12v-2z\" fill=\"currentColor\"><\/path><\/svg><svg style=\"fill: #999;color:#999\" class=\"arrow-unsorted-368013\" xmlns=\"http:\/\/www.w3.org\/2000\/svg\" width=\"10px\" height=\"10px\" viewBox=\"0 0 24 24\" version=\"1.2\" baseProfile=\"tiny\"><path d=\"M18.2 9.3l-6.2-6.3-6.2 6.3c-.2.2-.3.4-.3.7s.1.5.3.7c.2.2.4.3.7.3h11c.3 0 .5-.1.7-.3.2-.2.3-.5.3-.7s-.1-.5-.3-.7zM5.8 14.7l6.2 6.3 6.2-6.3c.2-.2.3-.5.3-.7s-.1-.5-.3-.7c-.2-.2-.4-.3-.7-.3h-11c-.3 0-.5.1-.7.3-.2.2-.3.5-.3.7s.1.5.3.7z\"\/><\/svg><\/span><\/span><\/span><\/a><\/span><\/div>\n<nav><ul class='ez-toc-list ez-toc-list-level-1 ' ><li class='ez-toc-page-1 ez-toc-heading-level-2'><a class=\"ez-toc-link ez-toc-heading-1\" href=\"https:\/\/filozofia.nett.to\/psychedelika\/en\/understanding-psychoactive-substances-receptors-and-affinity\/#Reuptake_inhibition\" >Reuptake inhibition<\/a><\/li><li class='ez-toc-page-1 ez-toc-heading-level-2'><a class=\"ez-toc-link ez-toc-heading-2\" href=\"https:\/\/filozofia.nett.to\/psychedelika\/en\/understanding-psychoactive-substances-receptors-and-affinity\/#Monoamine_oxidase_inhibitors_MAOIs\" >Monoamine oxidase inhibitors (MAOIs)<\/a><\/li><\/ul><\/nav><\/div>\n<p><strong>Affinity<\/strong><br \/> The strength of affinity is given in certain numerical units. The smaller the number, the higher the affinity. Affinity is measured in the amount at which the effects of a given psychoactive substance, for example, begin to manifest. The lower the content of the substance in the blood that causes psychoactive manifestations, the greater the strength of the substance. For psychoactive substances and psychiatric and neurological drugs, it is stated which receptors the substance acts on and with what high affinity. A large number of receptors are mainly affected by antipsychotic drugs.<br \/> Furthermore, it should be noted that all receptors (e.g., dopamine and serotonin receptors) are further divided into several types of receptors.<br \/> For example, dopamine receptors are divided into <strong>D1, D2, D3, D4, and D5<\/strong> receptors. GABA receptors are divided into <strong>GABA <sub>A<\/sub> and GABA <sub>B.<\/sub><\/strong><br \/> Serotonin receptors have an abbreviation created according to the chemical name: &quot; <strong>5-HT<\/strong> &quot;. Serotonin receptors are divided into <strong>5-HT1, 5-HT2, 5-HT3, 5-HT4<\/strong> , etc.<br \/> The <strong>5-HT1<\/strong> receptor is further divided into <strong>5-HT1A, 5-HT1B, 5-HT1D<\/strong> , etc.<br \/><br \/> Examples of the pharmacology and affinity of LSD and the antipsychotic clozapine to individual receptors<br \/> <a href=\"https:\/\/en.wikipedia.org\/wiki\/Lysergic_acid_diethylamide#Pharmacodynamics\" target=\"_blank\" rel=\"noopener\">https:\/\/en.wikipedia.org\/wiki\/Lysergic_acid_diethylamide#Pharmacodynamics<\/a><br \/> <a href=\"https:\/\/en.wikipedia.org\/wiki\/Clozapine#Mechanism_of_action\" target=\"_blank\" rel=\"noopener\">https:\/\/en.wikipedia.org\/wiki\/Clozapine#Mechanism_of_action<\/a><br \/><br \/> In relation to affinity, it is also important whether the receptor is acted upon as an agonist or antagonist, i.e., whether the activity of the receptors is increased or decreased by the receptor.<\/p><div style=\"line-height: 100%; margin-bottom: 0cm;\"> Affinity is expressed in numbers, the dissociation constant (K <sub>i<\/sub> ). There are no negative values, it is always stated with the affinity for a given type of receptor whether it is agonism or antagonism, i.e. it is an increase or decrease in the activity of the given receptor. Antagonism is sometimes also called inhibition. <div style=\"line-height: 100%; margin-bottom: 0cm;\"><div style=\"line-height: 100%; margin-bottom: 0cm;\"> There are several types, ways, and mechanisms by which the activity of a given receptor can be increased. For example, some substances act only on certain types of dopamine or serotonin receptors. Furthermore, the same substance can, for example, increase the activity of some types of serotonin receptors and decrease the activity of others. This is the case with some atypical antipsychotics.<div style=\"line-height: 100%; margin-bottom: 0cm;\"> <strong><span style=\"font-weight: normal;\">A very interesting antipsychotic is, for example,<\/span><\/strong> <strong><span style=\"font-weight: normal;\">aripiprazole<\/span><\/strong> <strong><span style=\"font-weight: normal;\"><a href=\"https:\/\/en.wikipedia.org\/wiki\/Aripiprazole#Pharmacology\" target=\"_blank\" rel=\"noopener\">https:\/\/en.wikipedia.org\/wiki\/Aripiprazole#Pharmacology<\/a><\/span><\/strong> <strong><span style=\"font-weight: normal;\">.<\/span><\/strong> <strong><span style=\"font-weight: normal;\">Although all antipsychotics reduce the activity of dopamine receptors, this one increases the activity of two types of dopamine receptors, and also reduces the activity of some types of serotonin receptors and increases the activity of others. And it is precisely because it reduces the activity of the types of serotonin receptors that are most responsible for psychotic symptoms that this is sufficient for the drug to have antipsychotic effects. It increases the activity of the types of serotonin receptors that are not responsible for psychotic symptoms.<\/span><\/strong> <div style=\"line-height: 100%; margin-bottom: 0cm;\"><h2 style=\"line-height: 100%; margin-bottom: 0cm;\"><span class=\"ez-toc-section\" id=\"Reuptake_inhibition\"><\/span> <strong><strong>Reuptake inhibition<\/strong><\/strong><span class=\"ez-toc-section-end\"><\/span><\/h2><div style=\"line-height: 100%; margin-bottom: 0cm;\"> <strong><span style=\"font-weight: normal;\">There are psychiatric drugs that are inhibitors of the reuptake of serotonin, noradrenaline, and dopamine. Sometimes, it can be the inhibition of the reuptake of more than one neurotransmitter. Drugs such as cocaine and methamphetamine also<\/span><\/strong> <strong><span style=\"font-weight: normal;\">inhibit<\/span><\/strong> <strong><span style=\"font-weight: normal;\">the<\/span><\/strong> <strong><span style=\"font-weight: normal;\">reuptake<\/span><\/strong> <strong><span style=\"font-weight: normal;\">of dopamine, noradrenaline, and serotonin at the same time, although each substance does so in a slightly different way.<\/span><\/strong><div style=\"line-height: 100%; margin-bottom: 0cm;\"> <strong><a href=\"https:\/\/en.wikipedia.org\/wiki\/Cocaine#Pharmacology\" target=\"_blank\" rel=\"noopener\"><span style=\"font-weight: normal;\">https:\/\/en.wikipedia.org\/wiki\/Cocaine#Pharmacology<\/span><\/a><\/strong><div style=\"line-height: 100%; margin-bottom: 0cm;\"> <strong><a href=\"https:\/\/en.wikipedia.org\/wiki\/Methamphetamine#Pharmacology\" target=\"_blank\" rel=\"noopener\"><span style=\"font-weight: normal;\">https:\/\/en.wikipedia.org\/wiki\/Methamphetamine#Pharmacology<\/span><\/a><\/strong><div style=\"line-height: 100%; margin-bottom: 0cm;\"> <strong><span style=\"font-weight: normal;\">Reuptake inhibition is characterized by<\/span><\/strong> <strong><span style=\"text-decoration: underline;\"><span style=\"font-weight: normal;\">increasing<\/span><\/span><\/strong> <strong><span style=\"text-decoration: underline;\"><span style=\"font-weight: normal;\">the<\/span><\/span><\/strong> <strong><span style=\"font-weight: normal;\">activity<\/span><\/strong> <strong><span style=\"text-decoration: underline;\"><span style=\"font-weight: normal;\">of all types<\/span><\/span><\/strong> <strong><span style=\"font-weight: normal;\">of receptors bound to the neurotransmitter<\/span><\/strong> <strong><span style=\"font-weight: normal;\">evenly<\/span><\/strong> <strong><span style=\"font-weight: normal;\">.<\/span><\/strong> <strong><span style=\"font-weight: normal;\">Other psychoactive substances mainly act only on some types of receptors of the neurotransmitter (e.g. LSD).<\/span><\/strong> <strong><span style=\"font-weight: normal;\">Reuptake inhibition never reduces the activity of the given receptor.<\/span><\/strong> <div style=\"line-height: 100%; margin-bottom: 0cm;\"><h2 style=\"line-height: 100%; margin-bottom: 0cm;\"><span class=\"ez-toc-section\" id=\"Monoamine_oxidase_inhibitors_MAOIs\"><\/span> <strong><strong>Monoamine oxidase inhibitors (MAOIs)<\/strong><\/strong><span class=\"ez-toc-section-end\"><\/span><\/h2><div style=\"line-height: 100%; margin-bottom: 0cm;\"> <strong><span style=\"font-weight: normal;\">MAOIs have many common features, or are very similar in their final effect to reuptake inhibitors. They also evenly increase the activity of all types of receptors of a given neurotransmitter. These are receptors bound to serotonin, dopamine and noradrenaline.<\/span><\/strong> <strong><span style=\"font-weight: normal;\">Monoamine<\/span><\/strong> <strong><span style=\"font-weight: normal;\">oxidase<\/span><\/strong> <strong><span style=\"font-weight: normal;\">inhibitors<\/span><\/strong> <strong><span style=\"font-weight: normal;\">are divided into two types: MAOI-A and MAOI-B. MAOI-<\/span><\/strong> <strong><span style=\"font-weight: normal;\">A mainly increases the activity of serotonin and noradrenaline receptors and to a lesser extent increases the activity of dopamine receptors, MAOI-B mainly increases the activity of dopamine receptors and to a lesser extent increases the activity of serotonin and dopamine receptors.<\/span><\/strong>","protected":false},"excerpt":{"rendered":"The strength of affinity is given in certain numerical units. The smaller the number, the higher the affinity. Affinity is measured in the amount at which the effects of a given psychoactive substance begin to manifest. The lower the content of the substance in the blood that causes psychoactive manifestations, the greater the strength of the substance.","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[11],"tags":[],"class_list":["post-150","post","type-post","status-publish","format-standard","hentry","category-psychedelics"],"_links":{"self":[{"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/posts\/150","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/comments?post=150"}],"version-history":[{"count":0,"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/posts\/150\/revisions"}],"wp:attachment":[{"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/media?parent=150"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/categories?post=150"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/filozofia.nett.to\/psychedelika\/wp-json\/wp\/v2\/tags?post=150"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}