Parethoxycaine
Parethoxycaine (Intracaine) is an ester-type local anesthetic that possesses dual activities as a non-selective inhibitor and agonist potentiator in smooth muscle, while acting as a mixed-type inhibitor of cytochrome c oxidase at the enzyme level. Parethoxycaine non-competitively inhibits the contraction of guinea pig ileal longitudinal muscle by interfering with transmembrane Ca2+ transport (blocking K+/CD responses in an equi-effective manner), and potentiates norepinephrine (NA) responses in rat vas deferens by blocking NA uptake and promoting Ca2+ mobilization (increasing the maximum amplitude without affecting K+ responses). Parethoxycaine inhibits the activity of purified cytochrome c oxidase in a concentration-dependent manner, and can be used in research focusing on Ca2+ signal transduction, smooth muscle contraction regulation, and mitochondrial energy metabolism.
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- No. CAS: 94-23-5
- Fòrmula: C15H23NO3
- Peso molecular:265.35
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Almacenamiento:
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Actividad biológica
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Cytochrome c oxidase 7.0 mM (Ki, Parethoxycaine competitively inhibits at 10 mM.) |
Cytochrome c oxidase 11.6 mM (Ki, Parethoxycaine exhibits mixed-type inhibition at 12 mM.) |
Parethoxycaine (10-13 mM) inhibits the activity of purified cytochrome c oxidase in a concentration-dependent manner, acting as a competitive inhibitor (Ki = 7.0 mM) at 10 mM and a mixed-type inhibitor (Ki = 11.6 mM) at 13 mM[1].
Parethoxycaine (30 min) non-competitively and equi-potently inhibits the contractile responses induced by CD and K+ in the longitudinal muscle of guinea pig ileum (with comparable potency against CD and K+), with an ID50 value ranging from 110 to 310 µM[2].
Parethoxycaine (50-100 µM; 30 min) enhances norepinephrine (NA)-induced contractile responses in rat vas deferens and shifts the concentration-response curve of NA to the left; however, PC itself has no enhancing effect on K+-induced contractile responses, while its MeBr derivative can enhance both NA- and K+-induced responses[2].
Parethoxycaine (50 µM; 30 min) shifts the calcium dose-response curve to the left in norepinephrine-depolarized, calcium-depleted rat vas deferens, but has no effect on calcium-induced contraction in potassium-depolarized rat vas deferens[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 94-23-5
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Peso molecular 265.35
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Fòrmula C15H23NO3
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SMILES
O=C(C1=CC=C(C=C1)OCC)OCCN(CC)CC
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Synonyms
Intracaine
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Casanovas AM, et al. Inhibition of cytochrome oxidase activity by local anaesthetics. Biochemical pharmacology. 1983 Sep 15;32(18):2715-9. [Content Brief]
[2]. Triggle CR, et al. Calcium antagonists and contractile responses in rat vas deferens and guinea pig ileal smooth muscle. Canadian journal of physiology and pharmacology. 1979 Aug;57(8):804-18. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Parethoxycaine Related Classifications
HY-184034 Related Classifications
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