1) La descarga del recurso depende de la página de origen
2) Para poder descargar el recurso, es necesario ser usuario registrado en Universia


Opción 1: Descargar recurso

Opción 2: Descargar recurso

Detalles del recurso

Descripción

A series of tethered quaternary ammonium derivatives of Tyr have been incorporated into the binding site of the nicotinic acetylcholine receptor (nAChR) using the in vivo nonsense suppression method, producing constitutively active (self-gating) receptors. We have incorporated primary, secondary, and tertiary amine tethered agonists to give receptors whose constitutive activity can be modulated by pH. Lowering the pH protonates the tethered amine, giving it a positive charge and allowing it to reversibly activate the receptor. Tertiary and secondary tethered amines, TyrO3T and TyrO3S, have been successfully incorporated at α149 in the nAChR. Constitutive currents at pH 5.5 are 6 times those at pH 9.0. The pK_a of TyrO3T in the binding site appears to be 6 or lower, differing substantially from its pK_a in solution (∼9.3). This local pK_a perturbation has substantial implications for pharmacological research on the nAChR:  of the tertiary agonists considered, noracetylcholine experiences this pK_a perturbation, while nicotine does not.

Pertenece a

Caltech Authors  

Autor(es)

Petersson, E. James -  Choi, Anita -  Dahan, David S. -  Lester, Henry A. -  Dougherty, Dennis A. - 

Id.: 69790716

Versión: 1.0

Estado: Final

Tipo:  application/pdf -  application/pdf - 

Tipo de recurso: Article  -  PeerReviewed  - 

Tipo de Interactividad: Expositivo

Nivel de Interactividad: muy bajo

Audiencia: Estudiante  -  Profesor  -  Autor  - 

Estructura: Atomic

Coste: no

Copyright: sí

Formatos:  application/pdf -  application/pdf - 

Requerimientos técnicos:  Browser: Any - 

Relación: [References] http://resolver.caltech.edu/CaltechAUTHORS:20170414-144546207
[References] http://authors.library.caltech.edu/76579/

Fecha de contribución: 15-abr-2017

Contacto:

Localización:
* Petersson, E. James and Choi, Anita and Dahan, David S. and Lester, Henry A. and Dougherty, Dennis A. (2002) A Perturbed pK_a at the Binding Site of the Nicotinic Acetylcholine Receptor: Implications for Nicotine Binding. Journal of the American Chemical Society, 124 (43). pp. 12662-12663. ISSN 0002-7863. http://resolver.caltech.edu/CaltechAUTHORS:20170414-144546207

Otros recursos del mismo autor(es)

  1. Acute Ethanol Administration Upregulates Synaptic α4-Subunit of Neuronal Nicotinic Acetylcholine Receptors within the Nucleus Accumbens and Amygdala Alcohol and nicotine are two of the most frequently abused drugs, with their comorbidity well descri...
  2. TC299423, a Novel Agonist for Nicotinic Acetylcholine Receptors (E)-5-(Pyrimidin-5-yl)-1,2,3,4,7,8-hexahydroazocine (TC299423) is a novel agonist for nicotinic acet...
  3. Nicotine in the Endoplasmic Reticulum Nicotine activates plasma membrane (PM) nicotinic receptors (nAChRs), but also permeates into the en...
  4. Region specific proteomic analysis of murine brain after chronic nicotine or menthol Nicotinic acetylcholine receptors (nAChRs) are pentameric cation channels that are expressed in the ...
  5. Spin control in organic molecules Magnetism has fascinated and served humanity for almost 3000 years. Since the discovery of the lodes...

Otros recursos de la mismacolección

  1. An experimental analysis of decision making procedures for discrete public goods: A case study of a problem in institutional design No abstract.
  2. Measurements of the associated production of a Z boson and b jets in pp collisions at √s = 8 TeV Measurements of the associated production of a Z boson with at least one jet originating from a b qu...
  3. Measurements of properties of the Higgs boson decaying into the four-lepton final state in pp collisions at √s = 13 TeV Properties of the Higgs boson are measured in the H → ZZ → 4ℓ (ℓ = e, μ) decay channel. A data sampl...
  4. Search for associated production of dark matter with a Higgs boson decaying to bb or γγ at √s = 13 TeV A search for dark matter is performed looking for events with large missing transverse momentum and ...
  5. Effects of transients in LIGO suspensions on searches for gravitational waves This paper presents an analysis of the transient behavior of the Advanced LIGO (Laser Interferometer...

Aviso de cookies: Usamos cookies propias y de terceros para mejorar nuestros servicios, para análisis estadístico y para mostrarle publicidad. Si continua navegando consideramos que acepta su uso en los términos establecidos en la Política de cookies.