{"id":52831,"date":"2025-08-05T08:30:07","date_gmt":"2025-08-05T08:30:07","guid":{"rendered":"https:\/\/rechemco.to\/?post_type=product&p=52831"},"modified":"2026-07-28T03:36:31","modified_gmt":"2026-07-28T03:36:31","slug":"nortilidine-hcl-eu","status":"publish","type":"product","link":"https:\/\/rechemco.to\/es\/nortilidine-hcl-eu\/","title":{"rendered":"Nortilidina HCL UE"},"content":{"rendered":"

Nortilidine: Active Opioid Metabolite of Tilidine with \u03bc\u2011Opioid Agonism & NMDA Modulation<\/strong><\/p>\n\n\n\n

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Descripci\u00f3n general<\/h4>\n\n\n\n

Nortilidine is the primary active metabolite<\/strong> of the opioid prodrug tilidine<\/strong>, produced in the liver through demethylation via CYP3A4 and CYP2C19 enzymes. Despite tilidine\u2019s low intrinsic potency, nortilidine exhibits analgesic efficacy comparable to morphine<\/strong>, underpinning tilidine\u2019s therapeutic action.<\/p>\n\n\n\n

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Chemical & Physical Properties<\/h4>\n\n\n\n
    \n
  • Nombre IUPAC<\/strong>: ethyl (1R,2S)-2-(methylamino)-1-phenylcyclohex-3-ene-1-carboxylate<\/li>\n\n\n\n
  • Molecular Formula<\/strong>: C\u2081\u2086H\u2082\u2081NO\u2082; Peso molecular<\/strong>: ~259.34 g\/mol<\/li>\n\n\n\n
  • Structural Info<\/strong>: Racemic mixture of two stereoisomers; the (1R,2S)-enantiomer exhibits NMDA receptor antagonism and additional dopaminergic activity.<\/li>\n<\/ul>\n\n\n\n
    \n\n\n\n

    Farmacodin\u00e1mica<\/h4>\n\n\n\n
      \n
    • \u03bc\u2011Opioid Receptor Agonism<\/strong>: Selective agonist at the Mu-opioid receptor with an IC\u2085\u2080 around 110\u202fnM\u2014over 100-fold more potent than tilidine itself (11\u202f\u03bcM), demonstrating high receptor selectivity.<\/li>\n\n\n\n
    • NMDA Antagonism<\/strong>: The (1R,2S)-isomer displays NMDA receptor antagonistic activity, unlike many opioids, which may contribute to mild dissociative and analgesic modulation.<\/li>\n\n\n\n
    • Dopamine Reuptake Inhibition<\/strong>: Reports indicate dopaminergic transporter inhibition, potentially influencing reinforcement effects.<\/li>\n<\/ul>\n\n\n\n
      \n\n\n\n

      Farmacocin\u00e9tica<\/h4>\n\n\n\n
        \n
      • Produced in vivo from tilidine via CYP3A4<\/strong> y CYP2C19<\/strong> enzymes.<\/li>\n\n\n\n
      • Nortilidine reaches peak plasma concentration within 25\u201350 minutes<\/strong> post-tilidine ingestion; elimination half-life is approximately 3\u20135 hours<\/strong>.<\/li>\n\n\n\n
      • Eliminated primarily via renal excretion<\/strong>; hepatic impairment may alter efficacy due to reduced formation from the prodrug.<\/li>\n<\/ul>\n\n\n\n
        \n\n\n\n

        Analgesic Efficacy<\/h4>\n\n\n\n

        Nortilidine is responsible for tilidine\u2019s clinical analgesia, with potency nearly equivalent to morphine<\/strong> despite being generated from a weak parent compound. Both analgesic and sedative effects arise predominantly via \u03bc-opioid receptor activation, reversible by naloxone.<\/p>\n\n\n\n

        \n\n\n\n

        Side Effects & Safety<\/h4>\n\n\n\n

        Common adverse effects reported with tilidine\/nortilidine use include nausea, dizziness, sedation, headache, increased sweating and fatigue. Because nortilidine is a potent opioid metabolite, risks include respiratory depression, constipation, tolerance, and dependence<\/strong> similar to other \u03bc\u2011agonists.
        The NMDA antagonism may also contribute to rare excitatory or dissociative side effects, especially at high doses or with repeated exposure.<\/p>\n\n\n\n

        \n\n\n\n

        Harm Reduction & Lab Handling<\/h4>\n\n\n\n

        As a research-grade active opioid metabolite, nortilidine requires careful dosing and handling. Key precautions include:<\/p>\n\n\n\n

          \n
        • Accurate analytical measurement (e.g., mg\u2011precision scales)<\/li>\n\n\n\n
        • Awareness of CYP-mediated formation from prodrugs<\/li>\n\n\n\n
        • Co-administration of naloxone in tilidine formulations may attenuate peripheral effects but does not inhibit central analgesia<\/li>\n\n\n\n
        • Monitor respiratory and CNS depression in in vivo models<\/li>\n<\/ul>\n\n\n\n
          \n\n\n\n

          Research & Forensic Applications<\/h4>\n\n\n\n

          Nortilidine is routinely included as a reference standard in forensic toxicology<\/strong> for confirming tilidine use, as well as in mechanistic studies involving \u03bc-opioid signaling and NMDA modulation. Its dual activity makes it a tool for exploring opioid potency, structure-activity relationships, and analgesic vs excitatory risk balance<\/strong>.<\/p>\n\n\n\n

          \n\n\n\n

          Legal & Regulatory Status<\/h4>\n\n\n\n

          While tilidine is medically approved in several countries (often combined with naloxone to deter misuse), nortilidine itself is not marketed<\/strong> and may fall under controlled-analogue laws depending on jurisdiction. Laboratory or research usage must comply with local opioid regulations.<\/p>\n\n\n\n

          \n\n\n\n

          Resumen<\/h4>\n\n\n\n

          Nortilidine is the key pharmacologically active metabolite<\/strong> of tilidine, combining potent opioid analgesic activity<\/strong> con NMDA receptor antagonism<\/strong> and dopaminergic involvement. With morphine-equivalent efficacy, rapid onset, and moderate duration, it plays a critical role in tilidine\u2019s effects. As a potent and multifaceted compound, it demands precise handling and clear understanding in both clinical pharmacology and research settings.<\/p>\n\n\n\n

          \n\n\n\n

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          \u2022 Pureza 99%<\/p>","protected":false},"excerpt":{"rendered":"

          Nortilidine \u2013 Active Opioid Metabolite of Tilidine<\/h2>\n

          Nortilidine<\/strong> is the principal active metabolite of the prodrug tilidine. It acts as a potent \u03bc-opioid receptor agonist<\/strong>, with analgesic efficacy comparable to morphine. Certain enantiomers also exhibit NMDA receptor antagonism<\/strong> y dopamine transporter inhibition<\/strong>, contributing to a complex pharmacological profile.<\/p>\n

            \n
          • Generated via CYP3A4 and CYP2C19 demethylation of tilidine<\/li>\n
          • Analgesia onset within 25\u201350\u202fminutes; effect lasts ~4\u20136\u202fhours<\/li>\n
          • Effects reversible by naloxone\u2014pure opioid action<\/li>\n
          • Used as forensic reference standard and in opioid mechanism research<\/li>\n<\/ul>\n

            For analytical or laboratory research use only. Not intended for human or veterinary consumption.<\/em><\/p>\n

            Plazo medio de entrega: 10 d\u00edas laborables.<\/p>\n

            Todos los productos de EU Retail s\u00f3lo pueden enviarse a pa\u00edses de la UE. <\/strong>
            Todas las drogas de dise\u00f1o vendidas en este sitio web est\u00e1n destinadas a la investigaci\u00f3n y a aplicaciones forenses.<\/strong><\/p>\n

            ATENCI\u00d3N
            <\/b>EN CASO DE P\u00c9RDIDA, DIRECCI\u00d3N INCORRECTA O CUALQUIER OTRO PROBLEMA, PARA ESTE PRODUCTO NO SE PERMITE NING\u00daN REENV\u00cdO O REEMBOLSO<\/p>","protected":false},"featured_media":52830,"comment_status":"open","ping_status":"closed","template":"","meta":[],"product_brand":[],"product_cat":[15],"product_tag":[1622,1633,1621,1623,1626,1627,1630,1637,1628,1629,1631,1571,495,1635,1625,1636,1624,1634,1620,1632],"class_list":["post-52831","product","type-product","status-publish","has-post-thumbnail","product_cat-out-of-stock","product_tag-analgesic-innovation","product_tag-chronic-pain-management","product_tag-g-protein-biased-opioid","product_tag-mu-opioid-receptor-agonist","product_tag-neuropathic-pain-relief","product_tag-novel-pain-therapeutics","product_tag-opioid-dependence-reduction","product_tag-opioid-harm-reduction","product_tag-opioid-pharmacodynamics","product_tag-opioid-pharmacokinetics","product_tag-opioid-receptor-signaling","product_tag-opioid-research","product_tag-opioid-tolerance","product_tag-opioid-induced-constipation","product_tag-oral-opioid-bioavailability","product_tag-reduced-opioid-side-effects","product_tag-respiratory-depression-mitigation","product_tag-safer-opioid-alternatives","product_tag-sr-17018","product_tag--arrestin-2","first","instock","shipping-taxable","purchasable","product-type-variable"],"_links":{"self":[{"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/product\/52831","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/product"}],"about":[{"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/types\/product"}],"replies":[{"embeddable":true,"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/comments?post=52831"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/media\/52830"}],"wp:attachment":[{"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/media?parent=52831"}],"wp:term":[{"taxonomy":"product_brand","embeddable":true,"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/product_brand?post=52831"},{"taxonomy":"product_cat","embeddable":true,"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/product_cat?post=52831"},{"taxonomy":"product_tag","embeddable":true,"href":"https:\/\/rechemco.to\/es\/wp-json\/wp\/v2\/product_tag?post=52831"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}