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Desensitization of the Neurokinin 1 Receptor Is Mediated by the Receptor Carboxy-Terminal Region, but Is Not Caused by Receptor Internalization
Desensitization of the Neurokinin 1 Receptor Is Mediated by the Receptor Carboxy-Terminal Region, but Is Not Caused by Receptor Internalization
- Source :
- Journal of Neurochemistry. 67:2362-2372
- Publication Year :
- 2002
- Publisher :
- Wiley, 2002.
-
Abstract
- The carboxy-terminal cytoplasmic regions of the rat neurokinin 1 (substance P) and neurokinin 2 (neurokinin A) receptors have been exchanged to determine if this region of the neurokinin 1 receptor is involved in its desensitization. When expressed at similar levels in stably transfected Chinese hamster ovary (CHO) cell lines, receptors containing the carboxy-terminal region of the neurokinin 1 receptor desensitized significantly more (as measured by reduction of the inositol 1,4,5-trisphosphate response) when preexposed for 1 min to 1 microM neurokinin, indicating a role for the carboxy-terminal region of the neurokinin 1 receptor in its desensitization. Measurement of receptor internalization using radiolabeled neurokinins (0.3 nM) indicated that approximately 75-80% of the receptors were internalized in each cell line after 10 min at 37 degrees C, with no observable correlation between neurokinin receptor desensitization and internalization. Measurement of loss of receptor surface sites for cell lines CHO NK1 and CHO NK1NK2 following exposure to 1 microM substance P also indicated no obvious relationship between the percent desensitization and percent of receptors internalized. Also, two inhibitors of neurokinin 1 receptor internalization, phenylarsine oxide and hyperosmolar sucrose, did not inhibit neurokinin 1 receptor desensitization. The protein kinase inhibitors Ro 31-8220, staurosporine, and Zn2+ had no effect on neurokinin 1 receptor desensitization, indicating that the kinases affected by these agents are not rate-limiting in neurokinin 1 receptor desensitization in this system.
- Subjects :
- Cytoplasm
medicine.medical_specialty
Recombinant Fusion Proteins
medicine.medical_treatment
media_common.quotation_subject
Substance P
CHO Cells
Inositol 1,4,5-Trisphosphate
Pharmacology
Biology
Transfection
Sensitivity and Specificity
Biochemistry
Cellular and Molecular Neuroscience
chemistry.chemical_compound
Cricetinae
Internal medicine
Homologous desensitization
Tachykinin receptor 1
medicine
Enzyme-linked receptor
Animals
Receptor
Internalization
Desensitization (medicine)
media_common
musculoskeletal, neural, and ocular physiology
Phosphotransferases
Biological Transport
Receptors, Neurokinin-2
Receptors, Neurokinin-1
respiratory system
biological factors
Protein Structure, Tertiary
Rats
Endocrinology
nervous system
chemistry
Neurokinin A
circulatory and respiratory physiology
Subjects
Details
- ISSN :
- 14714159 and 00223042
- Volume :
- 67
- Database :
- OpenAIRE
- Journal :
- Journal of Neurochemistry
- Accession number :
- edsair.doi.dedup.....05807e96dd27899d8a5254a75e481098
- Full Text :
- https://doi.org/10.1046/j.1471-4159.1996.67062362.x