Target type: molecularfunction
Combining with a calcitonin gene-related polypeptide (CGRP) to initiate a change in cell activity. [GOC:mah, PMID:12037140]
Calcitonin gene-related peptide receptor (CGRP-R) activity is a molecular function associated with G protein-coupled receptors (GPCRs) that mediate the cellular effects of calcitonin gene-related peptide (CGRP). CGRP is a neuropeptide that plays a diverse range of physiological roles, primarily in the central and peripheral nervous systems.
CGRP-R activity is characterized by the following key steps:
1. **Ligand Binding:** CGRP binds to its specific receptor, the CGRP-R, which is a heterodimer composed of two subunits: calcitonin receptor-like receptor (CLR) and receptor activity modifying protein 1 (RAMP1).
2. **Signal Transduction:** Upon ligand binding, the CGRP-R undergoes a conformational change, activating its associated G protein. The most commonly linked G protein is Gs, which stimulates the production of cyclic adenosine monophosphate (cAMP).
3. **Cellular Responses:** Elevated cAMP levels activate downstream signaling pathways, leading to a variety of cellular responses. These responses include:
- **Vasodilation:** CGRP-R activation promotes relaxation of smooth muscle cells, particularly in blood vessels, resulting in vasodilation.
- **Pain Modulation:** CGRP plays a crucial role in the transmission and perception of pain. CGRP-R activation in the peripheral nervous system can contribute to the development of inflammatory pain.
- **Neuroprotection:** CGRP has neuroprotective effects, protecting neurons from damage caused by various stressors.
- **Other Effects:** CGRP-R activity also influences other physiological processes, including inflammation, bone metabolism, and cardiovascular function.
Overall, CGRP-R activity is essential for mediating the diverse biological actions of CGRP. It plays a critical role in a wide range of physiological processes, including vasodilation, pain modulation, and neuroprotection.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Calcitonin gene-related peptide type 1 receptor | A calcitonin gene-related peptide type 1 receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16602] | Homo sapiens (human) |
| Calcitonin receptor | A calcitonin receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P30988] | Homo sapiens (human) |
| Receptor activity-modifying protein 1 | A receptor activity-modifying protein 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O60894] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| haloperidol | haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279) | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| azaperone | azaperone : An N-arylpiperazine that is 2-(piperazin-1-yl)pyridine in which the amino hydrogen is replaced by a 3-(4-fluobenzoyl)propyl group. Used mainly as a tranquiliser for pigs and elephants. Azaperone: A butyrophenone used in the treatment of PSYCHOSES. | aminopyridine; aromatic ketone; monofluorobenzenes; N-alkylpiperazine; N-arylpiperazine; tertiary amino compound | antipsychotic agent; dopaminergic antagonist |
| telcagepant | telcagepant: structure in first source | ||
| mk 3207 | |||
| bms 694153 | |||
| (5s,6s,9r)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5h-cyclohepta(b)pyridin-9-yl 4-(2-oxo-2,3-dihydro-1h-imidazo(4,5-b)pyridin-1-yl)piperidine-1-carboxylate | |||
| mk-8825 | |||
| atogepant | atogepant : A secondary carboxamide resulting from the formal condensation of the carboxy group of (3'S)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxylic acid with the amino group of (3S,5S,6R)-3-amino-6-methyl-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-2-one. It is a selective oral, small-molecule antagonist of calcitonin gene-related peptide (CGRP) receptor that has been approved for the treatment of migraine. | azaspiro compound; organic heterotetracyclic compound; piperidones; secondary carboxamide; trifluorobenzene | calcitonin gene-related peptide receptor antagonist |