Calcitonin gene-related peptide. A 37-amino acid peptide derived from the calcitonin gene. It occurs as a result of alternative processing of mRNA from the calcitonin gene. The neuropeptide is widely distributed in neural tissue of the brain, gut, perivascular nerves, and other tissue. The peptide produces multiple biological effects and has both circulatory and neurotransmitter modes of action. In particular, it is a potent endogenous vasodilator.
A peptide hormone that lowers calcium concentration in the blood. In humans, it is released by thyroid cells and acts to decrease the formation and absorptive activity of osteoclasts. Its role in regulating plasma calcium is much greater in children and in certain diseases than in normal adults.
Bethanechol compounds are parasympathomimetic agents that directly stimulate muscarinic receptors, primarily used to treat urinary retention and nonobstructive bladder dysfunction by increasing bladder contractility and decreasing post-void residual volume.
A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
A 36-amino acid peptide present in many organs and in many sympathetic noradrenergic neurons. It has vasoconstrictor and natriuretic activity and regulates local blood flow, glandular secretion, and smooth muscle activity. The peptide also stimulates feeding and drinking behavior and influences secretion of pituitary hormones.
Peptides released by NEURONS as intercellular messengers. Many neuropeptides are also hormones released by non-neuronal cells.
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
Slender processes of NEURONS, including the AXONS and their glial envelopes (MYELIN SHEATH). Nerve fibers conduct nerve impulses to and from the CENTRAL NERVOUS SYSTEM.
A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
Cell surface proteins that bind calcitonin and trigger intracellular changes which influence the behavior of cells. Calcitonin receptors outside the nervous system mediate the role of calcitonin in calcium homeostasis. The role of calcitonin receptors in the brain is not well understood.
Cell surface proteins that bind CALCITONIN GENE-RELATED PEPTIDE with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the CENTRAL NERVOUS SYSTEM and the periphery. They are formed via the heterodimerization of the CALCITONIN RECEPTOR-LIKE PROTEIN and RECEPTOR ACTIVITY-MODIFYING PROTEIN 1.
Tumors or cancer of the THYROID GLAND.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
A receptor protein that is associated with RECEPTOR ACTIVITY-MODIFYING PROTEINS. When bound to RECEPTOR ACTIVITY-MODIFYING PROTEIN 1 it forms the CALCITONIN GENE-RELATED RECEPTOR. When bound to RECEPTOR ACTIVITY-MODIFYING PROTEIN 2 or RECEPTOR ACTIVITY-MODIFYING PROTEIN 3 it forms the ADRENOMEDULLIN RECEPTOR.
A molluscan neuroactive peptide which induces a fast excitatory depolarizing response due to direct activation of amiloride-sensitive SODIUM CHANNELS. (From Nature 1995; 378(6558): 730-3)
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
A category of nucleic acid sequences that function as units of heredity and which code for the basic instructions for the development, reproduction, and maintenance of organisms.
A method (first developed by E.M. Southern) for detection of DNA that has been electrophoretically separated and immobilized by blotting on nitrocellulose or other type of paper or nylon membrane followed by hybridization with labeled NUCLEIC ACID PROBES.
Peptides composed of between two and twelve amino acids.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
A naturally occurring dipeptide neuropeptide found in muscles.
A collection of cloned peptides, or chemically synthesized peptides, frequently consisting of all possible combinations of amino acids making up an n-amino acid peptide.
A ubiquitously expressed, secreted protein with bone resorption and renal calcium reabsorption activities that are similar to PARATHYROID HORMONE. It does not circulate in appreciable amounts in normal subjects, but rather exerts its biological actions locally. Overexpression of parathyroid hormone-related protein by tumor cells results in humoral calcemia of malignancy.
A 27-amino acid peptide with histidine at the N-terminal and isoleucine amide at the C-terminal. The exact amino acid composition of the peptide is species dependent. The peptide is secreted in the intestine, but is found in the nervous system, many organs, and in the majority of peripheral tissues. It has a wide range of biological actions, affecting the cardiovascular, gastrointestinal, respiratory, and central nervous systems.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
A tetradecapeptide originally obtained from the skins of toads Bombina bombina and B. variegata. It is also an endogenous neurotransmitter in many animals including mammals. Bombesin affects vascular and other smooth muscle, gastric secretion, and renal circulation and function.

Interaction of amylin with calcitonin gene-related peptide receptors in the microvasculature of the hamster cheek pouch in vivo. (1/248)

1. This study used intravital microscopy to investigate the receptors stimulated by amylin which shares around 50% sequence homology with the vasodilator calcitonin gene-related peptide (CGRP) in the hamster cheek pouch microvasculature in vivo. 2. Receptor agonists dilated arterioles (diameters 20-40 microm). The -log of the concentrations (+/- s.e.mean; n = 8) causing 50% increase in arteriole diameter were: human betaCGRP (10.8 +/- 0.3), human alphaCGRP (10.8 +/- 0.4), rat alphaCGRP (10.4 +/- 0.3). Rat amylin and the CGRP2 receptor selective agonist [Cys(ACM2,7]-human alphaCGRP were 100 fold less potent (estimates were 8.5 +/- 0.4 and 8.2 +/- 0.3 respectively). 3. The GCRP1 receptor antagonist, CGRP8-37 (300 nmol kg(-1); i.v.) reversibly inhibited the increase in diameter evoked by human alphaCGRP (0.3 nM) from 178 +/- 22% to 59 +/- 12% (n = 8; P < 0.05) and by rat amylin (100 nM) from 138 +/- 23% to 68 +/- 24% (n = 6; P < 0.05). CGRP8-37 did not inhibit vasodilation evoked by substance P (10 nM; n = 4: P > 0.05). 4. The amylin receptor antagonist, amylin8-37 (300 nmol kg(-1); i.v.) did not significantly inhibit the increase in diameter evoked by human alphaCGRP (0.3 nM) which was 112 +/- 26% in the absence, and 90 +/- 29% in the presence of antagonist (n = 4; P < 0.05); nor that evoked by rat amylin (100 nM) which was 146 +/- 23% in the absence and 144 +/- 32% in the presence of antagonist (n = 4; P > 0.05). 5. The agonist profile for vasodilatation and the inhibition of this dilatation by CGRP8-37, although not the amylin8-37 indicates that amylin causes vasodilatation through interaction with CGRP1 receptors in the hamster cheek pouch.  (+info)

Conformational restraints revealing bioactive beta-bend structures for halpha CGRP8-37 at the CGRP2 receptor of the rat prostatic vas deferens. (2/248)

1. The main aim of this study was to identify putative beta-bends and the role of the N- and C-terminus in the CGRP receptor antagonist halpha CGRP8-37, which was measured against halpha CGRP inhibition of twitch responses in the rat prostatic vas deferens. 2. With a bend-biasing residue (proline) at position 16 in halpha CGRP8-37 (10(-5) M) an inactive compound was produced, while alanine at the same position retained antagonist activity (apparent pKB 5.6+/-0.1 at 10(-5) M). Proline at position 19 within halpha CGRP8-37 (10(-5) M) was an antagonist (apparent pKB 5.8+/-0.1). 3. Incorporation of a bend-forcing structure (beta-turn dipeptide or BTD) at either positions 19,20 or 33,34 in halpha CGRP8-37 (10(-5) M) antagonized halpha CGRP responses (apparent pKB 6.0+/-0.1 and 6.1+/-0.1, respectively). Replacement by BTD at both positions 19,20 and 33,34 within halpha CGRP8-37 competitively antagonized responses to halpha CGRP (pA2 6.2; Schild plot slope 1.0+/-0.1). 4. Halpha CGRP8-37 analogues (10(-5) M), substituted at the N-terminus by either glycine8, or des-NH2 valine8 or proline8 were all antagonists against halpha CGRP (apparent pKB 6.1+/-0.1, 6.5+/-0.1 and 6.1+/-0.1, respectively), while halpha CGRP8-37 (10(-5) M) substituted in three places by proline8 and glutamic acid10,14 was inactive. 5. Replacement of the C-terminus by alanine amide37 in halpha CGRP8-37 (10(-5) M) failed to antagonize halpha CGRP responses. 6. Peptidase inhibitors did not alter either the agonist potency of halpha CGRP or the antagonist affinities of halpha CGRP8-37 BTD19,20 and 33,34 and halpha CGRP8-37 Gly8 (against halpha CGRP responses). 7. In conclusion, two beta-bends at positions 18-21 and 32-35 are compatible with high affinity by BTD and is the first approach of modelling the bioactive structure of halpha CGRP8-37. Further, the N-terminus of halpha CGRP8-37 is not essential for antagonism, while the C-terminus interacts directly with CGRP receptor binding sites of the rat vas deferens.  (+info)

Characterization of receptors for calcitonin gene-related peptide and adrenomedullin on the guinea-pig vas deferens. (3/248)

1. The receptors which mediate the effects of calcitonin gene-related peptide (CGRP), amylin and adrenomedullin on the guinea-pig vas deferens have been investigated. 2. All three peptides cause concentration dependant inhibitions of the electrically stimulated twitch response (pD2s for CGRP, amylin and adrenomedullin of 7.90+/-0.11, 7.70+/-0.19 and 7.25+/-0.10 respectively). 3. CGRP8-37 (1 microM) and AC187 (10 microM) showed little antagonist activity against adrenomedullin. 4. Adrenomedullin22-52 by itself inhibited the electrically stimulated contractions of the vas deferens and also antagonized the responses to CGRP, amylin and adrenomedullin. 5. [125I]-adrenomedullin labelled a single population of binding sites in vas deferens membranes with a pIC50 of 8.91 and a capacity of 643 fmol mg(-1). Its selectivity profile was adrenomedullin> AC187>CGRP=amylin. It was clearly distinct from a site labelled by [125I]-CGRP (pIC50=8.73, capacity=114 fmol mg(-1), selectivity CGRP>amylin=AC187>adrenomedullin). [125I]-amylin bound to two sites with a total capacity of 882 fmol mg(-1). 6. Although CGRP has been shown to act at a CGRP2 receptor on the vas deferens with low sensitivity to CGRP8-37, this antagonist displaced [125I]-CGRP with high affinity from vas deferens membranes. This affinity was unaltered by increasing the temperature from 4 degrees C to 25 degrees C, suggesting the anomalous behaviour of CGRP8-37 is not due to temperature differences between binding and functional assays.  (+info)

Co-expression of prepro-adrenomedullin with a putative adrenomedullin receptor gene in vascular smooth muscle. (4/248)

The prepro-adrenomedullin (prepro-AM) gene encodes several biologically active peptides, including the potent vasodilator AM. At least part of the vasodilator action of AM appears to be mediated via interactions with receptors on vascular smooth muscle cells (VSMC); however, the specific receptors involved are not known. The aim of the present study was to identify putative AM receptor genes that are co-expressed with AM in cultured rat aortic VSMC that may mediate the actions of AM. AM mRNA was shown to be expressed in rat aortic VSMC cultures. In acute (4 h) secretion studies, only 20% of the total immunoreactive AM was intracellular, with the majority (80%) found in the medium, indicating active release of AM peptide from VSMC. Using highly specific ribonuclease protection analysis, mRNAs encoding three putative AM receptors [L1, calcitonin-receptor-like receptor (CRLR) and RDC1] were shown to be present at high concentrations in RNA extracts from lung. In cultured VSMC, however, whereas RDC1 mRNA was expressed at relatively high concentrations, transcripts encoding CRLR and L1 were not detected. The co-expression of prepro-AM mRNA with the RDC1 receptor implies that AM may act in a localized manner via this receptor to modulate VSMC function.  (+info)

Limitations in using peptide drugs to characterize calcitonin gene-related peptide receptors. (5/248)

Calcitonin gene-related peptide (CGRP) is an endogenous vasodilator peptide that produces its effects by activation of CGRP1 and CGRP2 receptor subtypes. These receptor subtypes are characterized in functional studies using the agonist Cys(Acm)2, 7-human-alpha-calcitonin gene-related peptide (Cys(ACM)2, 7-h-alpha-CGRP), which activates CGRP2 receptors, and the antagonist h-alphaCGRP(8-37) which has a high affinity for CGRP1 receptors and a low affinity for CGRP2 receptors. Our aim was to identify factors that may limit the use of these drugs to characterize CGRP receptor subtypes. We studied CGRP receptors using isolated ring segments of pig coronary and basilar arteries studied in vitro. The affinity of the antagonist h-alphaCGRP(8-37) for inhibiting h-alphaCGRP-induced relaxation of coronary arteries (log10 of the antagonist equilibrium dissociation constant = -5.33) was determined from Schild plots that had steep slopes. Therefore, we used capsaicin to investigate the role of endogenous CGRP in confounding affinity measurements for h-alphaCGRP(8-37). After capsaicin treatment, the slopes of the Schild plots were not different from one, and a higher affinity of h-CGRP(8-37) in blocking relaxation was obtained (log10 of the antagonist equilibrium dissociation constant = -6.01). We also investigated the agonist activity of the putative CGRP2 receptor selective agonist Cys(Acm)2,7-h-alphaCGRP. We found that maximal relaxation of coronary arteries caused by Cys(Acm)2,7-h-alphaCGRP was dependent upon the level of contractile tone induced by KCl. We also determined the KA for Cys(Acm)2,7-h-alphaCGRP and found that the KA (817 nM) was not significantly different from the EC50 (503 nM) for this drug in causing relaxation, indicating that Cys(Acm)2, 7-h-alphaCGRP is a partial agonist. Because experimental conditions affect the actions of h-CGRP(8-37) and Cys(Acm)2,7-h-alphaCGRP, the conditions must be carefully controlled to reliably identify CGRP receptor subtypes.  (+info)

Capsaicin-insensitive sensory-efferent meningeal vasodilatation evoked by electrical stimulation of trigeminal nerve fibres in the rat. (6/248)

1. Antidromic vasodilatation and plasma extravasation to stimulation of the trigeminal ganglion or its perivascular meningeal fibres was investigated by laser-Doppler flowmetry and 125I-labelled bovin serum albumin in the dura mater and in exteroceptive areas (nasal mucosa, upper eyelid) of anaesthetized rats pretreated with guanethidine and pipecuronium. 2 Trigeminal stimulation at 5 Hz for 20 s elicited unilateral phasic vasodilatation in the dura and lasting response in the nasal mucosa. Resiniferatoxin (1-3 microg kg(-1) i.v.), topical (1%) or systemic capsaicin pretreatment (300 mg kg(-1) s.c. plus 1 mg kg(-1) i.v.) did not inhibit the meningeal responses but abolished or strongly inhibited the nasal responses. Administration of vinpocetine (3 mg kg(-1) i.v.) increased both basal blood flow and the dural vasodilatation to perivascular nerve stimulation. 3. Dural vasodilatation to trigeminal stimulation was not inhibited by the calcitonin gene-related peptide-1 receptor (CGRP-1) antagonist hCGRP8-37 (15 or 50 microg kg(-1) i.v), or the neurokinin-1 receptor antagonist RP 67580 (0.1 mg kg(-1) i.v.) although both antagonists inhibited the nasal response. Neither mucosal nor meningeal responses were inhibited by atropine (5 mg kg(-1) i.v.), hexamethonium (10 mg kg(-1) i.v.) or the vasoactive intestinal polypeptide (VIP) antagonist (p-chloro-D-Phe6-Leul7)VIP (20 microg kg(-1) i.v.). 4. Plasma extravasation in the dura and upper eyelid elicited by electrical stimulation of the trigeminal ganglion was almost completely abolished in rats pretreated with resiniferatoxin (3 microg kg(-1) i.v.). 5. It is concluded that in the rat meningeal vasodilatation evoked by stimulation of trigeminal fibres is mediated by capsaicin-insensitive primary afferents, while plasma extravasation in the dura and upper eyelid and the vasodilatation in the nasal mucosa are mediated by capsaicin-sensitive trigeminal fibres.  (+info)

Influence of CGRP (8-37), but not adrenomedullin (22-52), on the haemodynamic responses to lipopolysaccharide in conscious rats. (7/248)

1. The functional involvement of the vasodilator peptides, adrenomedullin (ADM) and calcitonin gene-related peptide (CGRP), in the haemodynamic sequelae of continuous infusion of lipopolysaccharide (LPS) was assessed in conscious, male, Long Evans rats, by the use of peptide antagonists. 2. It was demonstrated that ADM (22-52) at a dose of 500 nmol kg-1 h-1 caused significant inhibition of the effects of ADM (1 nmol kg-1), without affecting responses to CGRP (0.1 or 1 nmol kg-1). 3. Even when the regional vasodilator responses to LPS infusion were enhanced (by pre-treatment with dexamethasone and the endothelin antagonist, SB 209670, or by pretreatment with SB 209670 and the AT1-receptor antagonist, losartan), ADM (22-52) had no significant cardiovascular effects. In contrast, the CGRP1-receptor antagonist, CGRP (8-37), caused small, but significant, inhibitions of the hypotensive and renal and mesenteric vasodilator effects of LPS, but only 6 h after onset of infusion in the presence of dexamethasone and SB 209670. 4. The results indicate that, in this model of endotoxaemia, the marked regional vasodilatations seen in the presence of dexamethasone and SB 209670 do not involve ADM, but do involve CGRP, albeit only to a small extent.  (+info)

Regulation of calcitonin gene-related peptide receptors in the rat uterus during pregnancy and labor and by progesterone. (8/248)

Calcitonin gene-related peptide (CGRP) is a potent smooth muscle relaxant in a variety of tissues. We recently demonstrated that CGRP relaxes uterine tissue during pregnancy but not during labor. In the present study we examined whether uterine (125)I-CGRP binding and immunoreactive CGRP receptors are regulated by pregnancy and labor and by sex steroid hormones. We found that (125)I-CGRP binding to membrane preparations from uteri was elevated during pregnancy and decreased during labor and postpartum. Changes in immunoreactive CGRP receptors were similar to the changes in (125)I-CGRP binding in these tissues, suggesting pregnancy-dependent regulation of CGRP receptor protein. CGRP receptors were elevated by Day 7 of gestation, and a precipitous decrease in these receptors occurred on Day 22 of gestation prior to the onset of labor. Both (125)I-CGRP-binding and immunofluorescence studies indicated that CGRP receptors were localized to myometrial cells. Hormonal control of uterine CGRP receptors was assessed by the use of antiprogesterone RU-486, progesterone, and estradiol-17beta. RU-486 induced a decrease in uterine CGRP receptors during pregnancy (Day 19). On the other hand, progesterone prevented the fall in uterine CGRP receptors at term (Day 22). In addition, progesterone also increased uterine CGRP receptors in nonpregnant, ovariectomized rats, while estradiol had no effects. These hormone-induced changes in uterine CGRP receptors were demonstrated by (125)I-CGRP-binding, Western immunoblotting, and immunolocalization methods. These results indicate that CGRP receptors and CGRP binding in the rat uterus are increased with pregnancy and decreased at term. These receptors are localized to the myometrial cells, and progesterone is required for maintaining CGRP receptors in the rat uterus. Thus, the inhibitory effects of CGRP on uterine contractility are mediated through the changes in CGRP receptors and may play a role in uterine quiescence during pregnancy.  (+info)

Calcitonin gene-related peptide (CGRP) is a neurotransmitter and vasodilator peptide that is widely distributed in the nervous system. It is encoded by the calcitonin gene, which also encodes calcitonin and catestatin. CGRP is produced and released by sensory nerves and plays important roles in pain transmission, modulation of inflammation, and regulation of blood flow.

CGRP exists as two forms, α-CGRP and β-CGRP, which differ slightly in their amino acid sequences but have similar biological activities. α-CGRP is found primarily in the central and peripheral nervous systems, while β-CGRP is expressed mainly in the gastrointestinal tract.

CGRP exerts its effects by binding to specific G protein-coupled receptors, which are widely distributed in various tissues, including blood vessels, smooth muscles, and sensory neurons. Activation of CGRP receptors leads to increased intracellular cyclic AMP levels, activation of protein kinase A, and subsequent relaxation of vascular smooth muscle, resulting in vasodilation.

CGRP has been implicated in several clinical conditions, including migraine, cluster headache, and inflammatory pain. Inhibition of CGRP signaling has emerged as a promising therapeutic strategy for the treatment of these disorders.

Calcitonin is a hormone that is produced and released by the parafollicular cells (also known as C cells) of the thyroid gland. It plays a crucial role in regulating calcium homeostasis in the body. Specifically, it helps to lower elevated levels of calcium in the blood by inhibiting the activity of osteoclasts, which are bone cells that break down bone tissue and release calcium into the bloodstream. Calcitonin also promotes the uptake of calcium in the bones and increases the excretion of calcium in the urine.

Calcitonin is typically released in response to high levels of calcium in the blood, and its effects help to bring calcium levels back into balance. In addition to its role in calcium regulation, calcitonin may also have other functions in the body, such as modulating immune function and reducing inflammation.

Clinically, synthetic forms of calcitonin are sometimes used as a medication to treat conditions related to abnormal calcium levels, such as hypercalcemia (high blood calcium) or osteoporosis. Calcitonin can be administered as an injection, nasal spray, or oral tablet, depending on the specific formulation and intended use.

Bethanechol compounds are a type of cholinergic agent used in medical treatment. They are parasympathomimetic drugs, which means they mimic the actions of the neurotransmitter acetylcholine at muscarinic receptors. Specifically, bethanechol compounds stimulate the muscarinic receptors in the smooth muscle of the bladder and gastrointestinal tract, increasing tone and promoting contractions.

Bethanechol is primarily used to treat urinary retention and associated symptoms, such as those that can occur after certain types of surgery or with conditions like spinal cord injury or multiple sclerosis. It works by helping the bladder muscle contract, which can promote urination.

It's important to note that bethanechol should be used with caution, as it can have various side effects, including sweating, increased salivation, flushed skin, and gastrointestinal symptoms like nausea, vomiting, or diarrhea. It may also interact with other medications, so it's crucial to discuss any potential risks with a healthcare provider before starting this treatment.

Bethanechol is a parasympathomimetic drug, which means it stimulates the parasympathetic nervous system. This system is responsible for regulating many automatic functions in the body, including digestion and urination. Bethanechol works by causing the smooth muscles of the bladder to contract, which can help to promote urination in people who have difficulty emptying their bladder completely due to certain medical conditions such as surgery, spinal cord injury, or multiple sclerosis.

The medical definition of 'Bethanechol' is:

A parasympathomimetic agent that stimulates the muscarinic receptors of the autonomic nervous system, causing contraction of smooth muscle and increased secretion of exocrine glands. It is used to treat urinary retention and associated symptoms, such as those caused by bladder-neck obstruction due to prostatic hypertrophy or neurogenic bladder dysfunction. Bethanechol may also be used to diagnose urinary tract obstruction and to test the integrity of the bladder's innervation.

Substance P is an undecapeptide neurotransmitter and neuromodulator, belonging to the tachykinin family of peptides. It is widely distributed in the central and peripheral nervous systems and is primarily found in sensory neurons. Substance P plays a crucial role in pain transmission, inflammation, and various autonomic functions. It exerts its effects by binding to neurokinin 1 (NK-1) receptors, which are expressed on the surface of target cells. Apart from nociception and inflammation, Substance P is also involved in regulating emotional behaviors, smooth muscle contraction, and fluid balance.

Neuropeptide Y (NPY) is a neurotransmitter and neuropeptide that is widely distributed in the central and peripheral nervous systems. It is a member of the pancreatic polypeptide family, which includes peptide YY and pancreatic polypeptide. NPY plays important roles in various physiological functions such as energy balance, feeding behavior, stress response, anxiety, memory, and cardiovascular regulation. It is involved in the modulation of neurotransmitter release, synaptic plasticity, and neural development. NPY is synthesized from a larger precursor protein called prepro-NPY, which is post-translationally processed to generate the mature NPY peptide. The NPY system has been implicated in various pathological conditions such as obesity, depression, anxiety disorders, hypertension, and drug addiction.

Neuropeptides are small protein-like molecules that are used by neurons to communicate with each other and with other cells in the body. They are produced in the cell body of a neuron, processed from larger precursor proteins, and then transported to the nerve terminal where they are stored in secretory vesicles. When the neuron is stimulated, the vesicles fuse with the cell membrane and release their contents into the extracellular space.

Neuropeptides can act as neurotransmitters or neuromodulators, depending on their target receptors and the duration of their effects. They play important roles in a variety of physiological processes, including pain perception, appetite regulation, stress response, and social behavior. Some neuropeptides also have hormonal functions, such as oxytocin and vasopressin, which are produced in the hypothalamus and released into the bloodstream to regulate reproductive and cardiovascular function, respectively.

There are hundreds of different neuropeptides that have been identified in the nervous system, and many of them have multiple functions and interact with other signaling molecules to modulate neural activity. Dysregulation of neuropeptide systems has been implicated in various neurological and psychiatric disorders, such as chronic pain, addiction, depression, and anxiety.

Capsaicin is defined in medical terms as the active component of chili peppers (genus Capsicum) that produces a burning sensation when it comes into contact with mucous membranes or skin. It is a potent irritant and is used topically as a counterirritant in some creams and patches to relieve pain. Capsaicin works by depleting substance P, a neurotransmitter that relays pain signals to the brain, from nerve endings.

Here is the medical definition of capsaicin from the Merriam-Webster's Medical Dictionary:

caпсаісіn : an alkaloid (C18H27NO3) that is the active principle of red peppers and is used in topical preparations as a counterirritant and analgesic.

Nerve fibers are specialized structures that constitute the long, slender processes (axons) of neurons (nerve cells). They are responsible for conducting electrical impulses, known as action potentials, away from the cell body and transmitting them to other neurons or effector organs such as muscles and glands. Nerve fibers are often surrounded by supportive cells called glial cells and are grouped together to form nerve bundles or nerves. These fibers can be myelinated (covered with a fatty insulating sheath called myelin) or unmyelinated, which influences the speed of impulse transmission.

Vasoactive Intestinal Peptide (VIP) is a 28-amino acid polypeptide hormone that has potent vasodilatory, secretory, and neurotransmitter effects. It is widely distributed throughout the body, including in the gastrointestinal tract, where it is synthesized and released by nerve cells (neurons) in the intestinal mucosa. VIP plays a crucial role in regulating various physiological functions such as intestinal secretion, motility, and blood flow. It also has immunomodulatory effects and may play a role in neuroprotection. High levels of VIP are found in the brain, where it acts as a neurotransmitter or neuromodulator and is involved in various cognitive functions such as learning, memory, and social behavior.

Peptides are short chains of amino acid residues linked by covalent bonds, known as peptide bonds. They are formed when two or more amino acids are joined together through a condensation reaction, which results in the elimination of a water molecule and the formation of an amide bond between the carboxyl group of one amino acid and the amino group of another.

Peptides can vary in length from two to about fifty amino acids, and they are often classified based on their size. For example, dipeptides contain two amino acids, tripeptides contain three, and so on. Oligopeptides typically contain up to ten amino acids, while polypeptides can contain dozens or even hundreds of amino acids.

Peptides play many important roles in the body, including serving as hormones, neurotransmitters, enzymes, and antibiotics. They are also used in medical research and therapeutic applications, such as drug delivery and tissue engineering.

Calcitonin receptors (CTRs) are a type of G protein-coupled receptor (GPCR) that bind and respond to the hormone calcitonin. Calcitonin is a peptide hormone secreted by the parafollicular cells (C cells) of the thyroid gland, and plays a crucial role in regulating calcium homeostasis in the body.

CTRs are widely expressed in various tissues and organs, including bone, kidney, intestine, and brain. In bone, CTR activation inhibits osteoclast-mediated bone resorption, thereby increasing bone density and reducing the risk of fractures. In the kidney, CTR activation promotes calcium reabsorption and phosphate excretion, helping to maintain normal serum calcium and phosphate levels.

CTRs are also involved in various physiological processes, such as nociception (pain perception), neuroprotection, and cell proliferation and differentiation. Dysregulation of CTR signaling has been implicated in several diseases, including osteoporosis, hypercalcemia, and cancer.

The medical definition of "Receptors, Calcitonin" refers to the specific proteins that bind calcitonin hormone and mediate its effects on target cells and tissues.

Calcitonin gene-related peptide (CGRP) receptors are a type of cell surface receptor found in various tissues and cells, including the nervous system and blood vessels. CGRP is a neuropeptide that plays a role in regulating vasodilation, inflammation, and nociception (the sensation of pain).

The CGRP receptor is a complex of two proteins: calcitonin receptor-like receptor (CLR) and receptor activity-modifying protein 1 (RAMP1). When CGRP binds to the CLR-RAMP1 complex, it activates a signaling pathway that leads to vasodilation and increased pain sensitivity.

CGRP receptors have been identified as important targets for the treatment of migraine headaches, as CGRP levels are known to increase during migraine attacks. Several drugs that target CGRP receptors have been developed and approved for the prevention and acute treatment of migraines.

Thyroid neoplasms refer to abnormal growths or tumors in the thyroid gland, which can be benign (non-cancerous) or malignant (cancerous). These growths can vary in size and may cause a noticeable lump or nodule in the neck. Thyroid neoplasms can also affect the function of the thyroid gland, leading to hormonal imbalances and related symptoms. The exact causes of thyroid neoplasms are not fully understood, but risk factors include radiation exposure, family history, and certain genetic conditions. It is important to note that most thyroid nodules are benign, but a proper medical evaluation is necessary to determine the nature of the growth and develop an appropriate treatment plan.

A peptide fragment is a short chain of amino acids that is derived from a larger peptide or protein through various biological or chemical processes. These fragments can result from the natural breakdown of proteins in the body during regular physiological processes, such as digestion, or they can be produced experimentally in a laboratory setting for research or therapeutic purposes.

Peptide fragments are often used in research to map the structure and function of larger peptides and proteins, as well as to study their interactions with other molecules. In some cases, peptide fragments may also have biological activity of their own and can be developed into drugs or diagnostic tools. For example, certain peptide fragments derived from hormones or neurotransmitters may bind to receptors in the body and mimic or block the effects of the full-length molecule.

Messenger RNA (mRNA) is a type of RNA (ribonucleic acid) that carries genetic information copied from DNA in the form of a series of three-base code "words," each of which specifies a particular amino acid. This information is used by the cell's machinery to construct proteins, a process known as translation. After being transcribed from DNA, mRNA travels out of the nucleus to the ribosomes in the cytoplasm where protein synthesis occurs. Once the protein has been synthesized, the mRNA may be degraded and recycled. Post-transcriptional modifications can also occur to mRNA, such as alternative splicing and addition of a 5' cap and a poly(A) tail, which can affect its stability, localization, and translation efficiency.

Calcitonin receptor-like protein (CRLR) is a gene that encodes for a protein involved in the regulation of various physiological functions, including cell proliferation, differentiation, and apoptosis. CRLR itself does not bind to calcitonin or any other ligands, but it serves as a necessary component for the formation of functional receptors for certain peptide hormones, such as calcitonin gene-related peptide (CGRP) and adrenomedullin.

These hormones play important roles in regulating blood pressure, inflammation, and nociception (the perception of pain). CRLR forms a complex with receptor activity-modifying proteins (RAMPs) to create functional receptors for CGRP and adrenomedullin. The specific combination of CRLR and RAMPs determines the type of receptor formed, which in turn dictates the ligand specificity and downstream signaling pathways activated.

Mutations in the CRLR gene have been associated with various diseases, including familial hypocalciuric hypercalcemia (FHH) type 3, a rare inherited disorder characterized by elevated serum calcium levels and decreased urinary calcium excretion. Additionally, dysregulation of CRLR-mediated signaling pathways has been implicated in the development and progression of several types of cancer, neurodegenerative disorders, and cardiovascular diseases.

FMRFamide is not a medical term per se, but it is a neuropeptide that was first identified in the clam, Mytilus edulis. FMRFamide stands for Phe-Met-Arg-Phe-NH2, which are its five amino acid residues. It functions as a neurotransmitter or neuromodulator in various organisms, including humans. In mammals, related peptides are involved in the regulation of several physiological processes such as cardiovascular function, feeding behavior, and nociception (pain perception).

A base sequence in the context of molecular biology refers to the specific order of nucleotides in a DNA or RNA molecule. In DNA, these nucleotides are adenine (A), guanine (G), cytosine (C), and thymine (T). In RNA, uracil (U) takes the place of thymine. The base sequence contains genetic information that is transcribed into RNA and ultimately translated into proteins. It is the exact order of these bases that determines the genetic code and thus the function of the DNA or RNA molecule.

An amino acid sequence is the specific order of amino acids in a protein or peptide molecule, formed by the linking of the amino group (-NH2) of one amino acid to the carboxyl group (-COOH) of another amino acid through a peptide bond. The sequence is determined by the genetic code and is unique to each type of protein or peptide. It plays a crucial role in determining the three-dimensional structure and function of proteins.

A gene is a specific sequence of nucleotides in DNA that carries genetic information. Genes are the fundamental units of heredity and are responsible for the development and function of all living organisms. They code for proteins or RNA molecules, which carry out various functions within cells and are essential for the structure, function, and regulation of the body's tissues and organs.

Each gene has a specific location on a chromosome, and each person inherits two copies of every gene, one from each parent. Variations in the sequence of nucleotides in a gene can lead to differences in traits between individuals, including physical characteristics, susceptibility to disease, and responses to environmental factors.

Medical genetics is the study of genes and their role in health and disease. It involves understanding how genes contribute to the development and progression of various medical conditions, as well as identifying genetic risk factors and developing strategies for prevention, diagnosis, and treatment.

Southern blotting is a type of membrane-based blotting technique that is used in molecular biology to detect and locate specific DNA sequences within a DNA sample. This technique is named after its inventor, Edward M. Southern.

In Southern blotting, the DNA sample is first digested with one or more restriction enzymes, which cut the DNA at specific recognition sites. The resulting DNA fragments are then separated based on their size by gel electrophoresis. After separation, the DNA fragments are denatured to convert them into single-stranded DNA and transferred onto a nitrocellulose or nylon membrane.

Once the DNA has been transferred to the membrane, it is hybridized with a labeled probe that is complementary to the sequence of interest. The probe can be labeled with radioactive isotopes, fluorescent dyes, or chemiluminescent compounds. After hybridization, the membrane is washed to remove any unbound probe and then exposed to X-ray film (in the case of radioactive probes) or scanned (in the case of non-radioactive probes) to detect the location of the labeled probe on the membrane.

The position of the labeled probe on the membrane corresponds to the location of the specific DNA sequence within the original DNA sample. Southern blotting is a powerful tool for identifying and characterizing specific DNA sequences, such as those associated with genetic diseases or gene regulation.

Oligopeptides are defined in medicine and biochemistry as short chains of amino acids, typically containing fewer than 20 amino acid residues. These small peptides are important components in various biological processes, such as serving as signaling molecules, enzyme inhibitors, or structural elements in some proteins. They can be found naturally in foods and may also be synthesized for use in medical research and therapeutic applications.

Molecular sequence data refers to the specific arrangement of molecules, most commonly nucleotides in DNA or RNA, or amino acids in proteins, that make up a biological macromolecule. This data is generated through laboratory techniques such as sequencing, and provides information about the exact order of the constituent molecules. This data is crucial in various fields of biology, including genetics, evolution, and molecular biology, allowing for comparisons between different organisms, identification of genetic variations, and studies of gene function and regulation.

Carnosine is a dipeptide molecule composed of the amino acids histidine and alanine, which is naturally found in high concentrations in certain tissues of the body, particularly in muscle and brain tissue. It acts as an antioxidant, helping to protect cells from damage caused by free radicals and other oxidative stressors. Carnosine also has anti-glycation properties, meaning it helps prevent the formation of advanced glycation end products (AGEs) that can contribute to aging and age-related diseases. Additionally, carnosine has been shown to have potential benefits in neuroprotection, cardioprotection, and anti-inflammation. It is being studied for its potential therapeutic uses in various health conditions, including diabetes, cataracts, Alzheimer's disease, and other neurological disorders.

A peptide library is a collection of a large number of peptides, which are short chains of amino acids. Each peptide in the library is typically composed of a defined length and sequence, and may contain a variety of different amino acids. Peptide libraries can be synthesized using automated techniques and are often used in scientific research to identify potential ligands (molecules that bind to specific targets) or to study the interactions between peptides and other molecules.

In a peptide library, each peptide is usually attached to a solid support, such as a resin bead, and the entire library can be created using split-and-pool synthesis techniques. This allows for the rapid and efficient synthesis of a large number of unique peptides, which can then be screened for specific activities or properties.

Peptide libraries are used in various fields such as drug discovery, proteomics, and molecular biology to identify potential therapeutic targets, understand protein-protein interactions, and develop new diagnostic tools.

Parathyroid Hormone-Related Protein (PTHrP) is a protein that is encoded by the PTHLH gene in humans. It is structurally similar to parathyroid hormone (PTH) and was initially identified due to its role in humoral hypercalcemia of malignancy, a condition characterized by high levels of calcium in the blood caused by certain types of cancer.

PTHrP has a variety of functions in the body, including regulation of calcium and phosphate homeostasis, cell growth and differentiation, and bone metabolism. It acts through a specific G protein-coupled receptor called the PTH/PTHrP receptor, which is found in many tissues throughout the body, including bone, kidney, and cartilage.

In contrast to PTH, which is primarily produced by the parathyroid glands and regulates calcium levels in the blood, PTHrP is produced by many different types of cells throughout the body. Its expression is regulated in a tissue-specific manner, and its functions can vary depending on the context in which it is produced.

Overall, PTHrP plays important roles in normal physiology as well as in various disease states, including cancer, bone disorders, and developmental abnormalities.

I'm sorry for the confusion, but "Peptide PHI" is not a widely recognized or established medical term. It seems that there might be some misunderstanding or miscommunication related to this term.

If you are referring to a specific type of peptide or a research study, could you please provide more context or clarify the source of the term? I would be happy to help you with accurate and reliable information once I have a better understanding of what you are asking about.

Genetic transcription is the process by which the information in a strand of DNA is used to create a complementary RNA molecule. This process is the first step in gene expression, where the genetic code in DNA is converted into a form that can be used to produce proteins or functional RNAs.

During transcription, an enzyme called RNA polymerase binds to the DNA template strand and reads the sequence of nucleotide bases. As it moves along the template, it adds complementary RNA nucleotides to the growing RNA chain, creating a single-stranded RNA molecule that is complementary to the DNA template strand. Once transcription is complete, the RNA molecule may undergo further processing before it can be translated into protein or perform its functional role in the cell.

Transcription can be either "constitutive" or "regulated." Constitutive transcription occurs at a relatively constant rate and produces essential proteins that are required for basic cellular functions. Regulated transcription, on the other hand, is subject to control by various intracellular and extracellular signals, allowing cells to respond to changing environmental conditions or developmental cues.

Bombesin is a type of peptide that occurs naturally in the body. It is a small protein-like molecule made up of amino acids, and it is involved in various physiological processes, including regulating appetite and digestion. Bombesin was first discovered in the skin of a frog species called Bombina bombina, hence its name. In the human body, bombesin-like peptides are produced by various tissues, including the stomach and brain. They bind to specific receptors in the body, triggering a range of responses, such as stimulating the release of hormones and increasing gut motility. Bombesin has been studied for its potential role in treating certain medical conditions, including cancer, although more research is needed to establish its safety and efficacy.

Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene ... v t e (CS1 German-language sources (de), Antimigraine drugs, Receptor antagonists, Calcitonin gene-related peptide receptor ... an Oral Calcitonin Gene Related Peptide Receptor Antagonist". British Journal of Clinical Pharmacology. 79 (5): 831-7. doi: ... related peptide receptor (CGRPR). Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved ...
Fenethylline Theodrenaline Morton IK, Hall JM (1999). "Calcitonin gene-related peptide receptor antagonist". Concise Dictionary ... Adenosine receptor antagonists, Substituted amphetamines, Cardiac stimulants, Norepinephrine releasing agents, ...
... is a calcitonin gene-related peptide receptor antagonist. It is sprayed into the nose. It is sold by Pfizer. The ... Calcitonin gene-related peptide receptor antagonists, Pfizer brands, Piperazines, Piperidines, Indazoles, Quinolines, Ureas, ...
"Regulation of signal transduction by calcitonin gene-related peptide receptors." Trends in Pharmacological Sciences 31, no. 10 ... Investigation of the calcitonin receptor-like receptor and receptor activity modifying proteins' at Imperial College London. ... "Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes." Molecular Pharmacology ... "Agonist-dependent consequences of proline to alanine substitution in the transmembrane helices of the calcitonin receptor." Br ...
The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors". Pharmacological Reviews. 54 ... Calcitonin gene-related peptide (CGRP) is a member of the calcitonin family of peptides consisting of calcitonin, amylin, ... Regulation of the calcitonin gene-related peptide (CGRP) gene is in part controlled by the expression of the mitogen-activated ... of the calcitonin gene-related peptide (CGRP) receptor using a comprehensive mutagenesis approach" (PDF). Molecular and ...
... is a small-molecule calcitonin gene-related peptide receptor antagonist. It is the first drug in this class approved ... A Potent and Selective Antagonist of the Human Calcitonin GeneRelated Peptide Receptor". The Journal of Pharmacology and ... Calcitonin gene-related peptide receptor antagonists, Carboxamides, Trifluoromethyl compounds, Spiro compounds, Piperidinones, ...
"A cDNA encoding the calcitonin gene-related peptide type 1 receptor". J Biol Chem. 271 (19): 11325-9. doi:10.1074/jbc.271.19. ... Lesche R, Peetz A, van der Hoeven F, Rüther U (1998). "Ft1, a novel gene related to ubiquitin-conjugating enzymes, is deleted ... Fluhmann B, Muff R, Hunziker W, Fischer JA, Born W (Feb 1995). "A human orphan calcitonin receptor-like structure". Biochem ... AKT-interacting protein is a protein that in humans is encoded by the AKTIP gene. The mouse homolog of this gene produces fused ...
They are calcitonin gene-related peptide (CGRP) receptor antagonists. Gepants have been suggested to have less pain relief at 2 ... and Calcitonin-Gene-Related Peptide (CGRP) Receptor Monoclonal Antibodies". Pharmaceutics. 12 (12): 1180. doi:10.3390/ ... It is theorized that by antagonizing the CGRP receptor of the trigeminal ganglia, lowered CGRP is released and less migraine ... These medications are selective 5-HT1B/1D receptor agonists with some activity at 5-HT1F. They produce an antimigraine effect ...
... calcitonin receptor-like receptor/receptor activity modifying protein complexes define calcitonin gene-related peptide and ... it is a receptor for calcitonin gene-related peptide. The protein encoded by the CALCRL gene is a G protein-coupled receptor ... Calcitonin gene-related peptide receptor antagonists are approved for the treatment of migraine. GRCh38: Ensembl release 89: ... 2003). "Calcitonin gene-related peptide in pregnancy and its emerging receptor heterogeneity". Trends Endocrinol. Metab. 13 (6 ...
"Entrez Gene: RCP9 calcitonin gene-related peptide-receptor component protein". Yallampalli C, Chauhan M, Thota CS, et al. (2003 ... 2002). "Characterization of calcitonin gene-related peptide (CGRP) receptors and their receptor-activity-modifying proteins ( ... "Calcitonin gene-related peptide in pregnancy and its emerging receptor heterogeneity". Trends Endocrinol. Metab. 13 (6): 263-9 ... a novel protein required for signal transduction at calcitonin gene-related peptide and adrenomedullin receptors". J. Biol. ...
Durham PL, Vause CV (July 2010). "Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine". ... The calcitonin gene-related peptide (CGRP) is a therapeutic target in migraine because of its hypothesized role in mediating ... In turn, histamine evokes the release of substance P and calcitonin gene-related peptide; thus, a bidirectional link between ... Calcitonin Gene-Related Peptide (CGRP), neurokinin A (NKA), and endothelin-3 (ET-3). In such neurons, release of these pro- ...
... is a small molecule calcitonin gene-related peptide (CGRP) receptor antagonist. Rimegepant was developed by Biohaven ... Calcitonin gene-related peptide receptor antagonists, Carbamates, Fluoroarenes, Heterocyclic compounds with 2 rings, Nitrogen ... It works by blocking CGRP receptors. In the United States, rimegepant was approved for treating acute migraine in February 2020 ...
It is a gepant, an orally active calcitonin gene-related peptide receptor antagonist. The most common side effects include ... Moreno-Ajona D, Pérez-Rodríguez A, Goadsby PJ (June 2020). "Gepants, calcitonin-gene-related peptide receptor antagonists: what ... Calcitonin gene-related peptide receptor antagonists, Carboxamides, Organofluorides, Piperidines, Pyridines, Pyrroles, Spiro ... "FDA Approves Qulipta (atogepant), the First and Only Oral CGRP Receptor Antagonist Specifically Developed for the Preventive ...
... , sold under the brand name Aimovig, is a medication which targets the calcitonin gene-related peptide receptor (CGRPR ... Erenumab is a fully human monoclonal antibody blocking the calcitonin gene-related peptide receptor (CGRPR). After subcutaneous ... Calcitonin gene-related peptide receptor antagonists, Monoclonal antibodies, Amgen, Novartis brands). ... Like other proteins, the substance is degraded by proteolysis to small peptides and amino acids. It has an elimination half- ...
... modifying protein-directed G protein signaling specificity for the calcitonin gene-related peptide family of receptors receptor ... In humans, the glucagon receptor is encoded by the GCGR gene. Glucagon receptors are mainly expressed in liver and in kidney ... "Tissue-specific and glucose-dependent expression of receptor genes for glucagon and glucagon-like peptide-1 (GLP-1)". Hormone ... Shiota D, Kasamatsu T, Dib SA, Chacra AR, Moisés RS (May 2002). "Role of the Gly40Ser mutation in the glucagon receptor gene in ...
In her early career she discovered the Calcitonin gene-related peptide receptor antagonist (CGRP) as a potent microvascular ... Brain, S. D.; Williams, T. J.; Tippins, J. R.; Morris, H. R.; MacIntyre, I. (1985). "Calcitonin gene-related peptide is a ... More recently her research found that the gene TRPC5 can help protect against pain in arthritis and that the gene TRPA1 is ... "Transient receptor potential canonical 5 (TRPC5) protects against pain and vascular inflammation in arthritis and joint ...
... is a calcitonin/calcitonin gene-related peptide family peptide acting through the calcitonin receptor-like receptor/receptor ... CRLR, a receptor with seven transmembrane domains, can function as either a calcitonin gene-related peptide (CGRP) receptor or ... 2004). "Characterization of the human calcitonin gene-related peptide receptor subtypes associated with receptor activity- ... 2008). "Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide ...
CRLR, a receptor with seven transmembrane domains, can function as either a calcitonin gene-related peptide (CGRP) receptor or ... 2004). "Characterization of the human calcitonin gene-related peptide receptor subtypes associated with receptor activity- ... 2008). "Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide ... of the human receptor activity-modifying protein components of calcitonin gene-related peptide and adrenomedullin receptors". J ...
... (INN, code name BIBN-4096BS) is a calcitonin gene-related peptide receptor antagonist being studied as a potential ... Calcitonin gene-related peptide receptor antagonists, All stub articles, Nervous system drug stubs). ...
This lack of swelling indicates that WaTx fails to promote the release of calcitonin gene-related peptide (CGRP)-a hallmark of ... WaTx targets TRPA1, also known as the wasabi receptor or irritant receptor. WaTx is a cell-penetrating toxin that stabilizes ... Andersson, D. A.; Gentry, C.; Moss, S.; Bevan, S. (2008-03-05). "Transient Receptor Potential A1 Is a Sensory Receptor for ... Peptides. 32 (7): 1509-1517. doi:10.1016/j.peptides.2011.05.017. PMID 21624408. Quintero-Hernández, V.; Jiménez-Vargas, J.M.; ...
"Functional expression of receptors for calcitonin gene-related peptide, calcitonin, and vasoactive intestinal peptide in the ... "Entrez Gene: VIPR1 vasoactive intestinal peptide receptor 1". Ishihara T, Shigemoto R, Mori K, Takahashi K, Nagata S (Apr 1992 ... Dorsam G, Goetzl EJ (Apr 2002). "Vasoactive intestinal peptide receptor-1 (VPAC-1) is a novel gene target of the ... VPAC1 is a receptor for vasoactive intestinal peptide (VIP), a small neuropeptide. Vasoactive intestinal peptide is involved in ...
Calcitonin gene-related peptide, a peptide present in spinal cord motoneurons, increases the number of acetylcholine receptors ... Calcitonin-gene related peptide and muscle activity regulate acetylcholine receptor alpha-subunit mRNA levels by distinct ... and a stimulation of gene transcription at the synapse by the calcitonin gene-related peptide (CGRP) activating PKA and the ... Laufer R., and Changeux J.-P. (1987). Calcitonin gene-related peptide elevates cyclic AMP levels in chick skeletal muscle : ...
Imidazo[4,5-b]pyridines: Telcagepant-a calcitonin gene-related peptide receptor antagonist which was in clinical trials as a ... TP-003-a subtype-selective partial agonist at GABAA receptors, binding to GABAA receptor complexes bearing either α2, α3 or α5 ... Media related to Imidazopyridines at Wikimedia Commons (Articles with short description, Short description matches Wikidata, ... DS-1-a GABAA receptor positive allosteric modulator selective for the α4β3δ subtype, which is not targeted by other GABAergics ...
Calcitonin gene-related peptide receptor antagonists (CGRP) target calcitonin gene-related peptide or its receptor to prevent ... Calcitonin gene-related peptides (CGRPs) have been found to play a role in the pathogenesis of the pain associated with ... Medications in the anti-calcitonin gene-related peptide, including eptinezumab, erenumab, fremanezumab, and galcanezumab, ... Four genes have been shown to be involved in familial hemiplegic migraine. Three of these genes are involved in ion transport. ...
... is a calcitonin/calcitonin gene-related peptide family peptide acting through the calcitonin receptor-like receptor/receptor ... ADM2 is a protein that in humans is encoded by the ADM2 gene. ADM2 belongs to a family of calcitonin (MIM 114130)-related ... "Entrez Gene: ADM2 adrenomedullin 2". Human ADM2 genome location and ADM2 gene details page in the UCSC Genome Browser. Kawai M ... Peptides. 27 (6): 1383-9. doi:10.1016/j.peptides.2005.11.004. PMID 16359754. S2CID 27665694. Kindt F, Wiegand S, Löser C, et al ...
... the receptors contribute to nociception through the modulation of the extracellular concentration of calcitonin gene related ... peptide (CGRP). These conflicting roles are being researched further so that they may serve as potential targets for the ... P2Y receptors are also found on both neurons and glial cells. Their role is less clear than that of the P2X receptors, but it ... The receptor has been implicated in the release of interleukin IL-1β from macrophages or microglia and astrocytes. The receptor ...
... rizatriptan induces vasoconstriction-possibly by inhibiting the release of calcitonin gene-related peptide from sensory neurons ... Rizatriptan is in the triptan class and is believed to work by activating the 5-HT1 receptor. Rizatriptan was patented in 1991 ... Propranolol Rizatriptan acts as an agonist at serotonin 5-HT1B and 5-HT1D receptors. Like the other triptans sumatriptan and ...
... and angiotensin II type 2 receptors (AT2R). AngII co-localized in neurons that express substance P and calcitonin gene-related ... Alterman M. (2010). "Development of selective non-peptide angiotensin II type 2 receptor agonists". J Renin Angiotensin ... angiotensin II type 1 receptors (AT1R) and angiotensin II type 2 receptors (AT2R). AT1R is the receptor subtype that was found ... Receptor agonists and antagonist of angiotensin II receptors that target various parts of the complicated renin-angiotensin ...
... involved the calcitonin gene-related peptide, CGRP, a peptide involved in neuronal communication. This provided a new target ... for drugs, namely those that could interfere with the interaction of CGRP and its receptor. As a result, the gepants such as ... P. Goadsby, L Edvinsson and Ekman (1990) Vasoactive peptide release in the extracerebral circulation of humans during migraine ...
... calcitonin gene-related peptide receptors are formed by the asymmetric assembly of a calcitonin receptor-like receptor homo- ... CALCRL, a receptor with seven transmembrane domains, can function as either a calcitonin gene-related peptide (CGRP) receptor ... 2004). "Characterization of the human calcitonin gene-related peptide receptor subtypes associated with receptor activity- ... 2008). "Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide ...
Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene ... v t e (CS1 German-language sources (de), Antimigraine drugs, Receptor antagonists, Calcitonin gene-related peptide receptor ... an Oral Calcitonin Gene Related Peptide Receptor Antagonist". British Journal of Clinical Pharmacology. 79 (5): 831-7. doi: ... related peptide receptor (CGRPR). Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved ...
title = "Calcium: Calcitonin gene-related peptide and adrenomedullin receptors",. abstract = "Calcitonin gene-related peptide ( ... Calcitonin gene-related peptide (CGRP), adrenomedullin (AM) and adrenomedullin 2 (AM2) are related peptides, which are potent ... N2 - Calcitonin gene-related peptide (CGRP), adrenomedullin (AM) and adrenomedullin 2 (AM2) are related peptides, which are ... AB - Calcitonin gene-related peptide (CGRP), adrenomedullin (AM) and adrenomedullin 2 (AM2) are related peptides, which are ...
The development and optimisation of an HPLC-based in vitro serum stability assay for a calcitonin gene-related peptide receptor ... The development and optimisation of an HPLC-based in vitro serum stability assay for a calcitonin gene-related peptide receptor ... and validation of a method for the evaluation of the stability of a lead calcitonin gene-related peptide antagonist peptide ( ... Evaluation of the stability of peptide drug candidates in biological fluids, such as blood serum, is of high importance during ...
Dual action of the cannabinoid receptor 1 ligand arachidonyl-2′-chloroethylamide on calcitonin gene-related peptide release. * ... Dual action of the cannabinoid receptor 1 ligand arachidonyl-2′-chloroethylamide on calcitonin gene-related peptide release}}, ... on calcitonin gene-related peptide (CGRP) release in the dura and trigeminal ganglion (TG), as cannabinoids are known to ... on calcitonin gene-related peptide (CGRP) release in the dura and trigeminal ganglion (TG), as cannabinoids are known to ...
Dual action of the cannabinoid receptor 1 ligand arachidonyl-2′-chloroethylamide on calcitonin gene-related peptide release. ... on calcitonin gene-related peptide (CGRP) release in the dura and trigeminal ganglion (TG), as cannabinoids are known to ... CGRP and receptor activity modifying protein 1 (RAMP1), a subunit of the functional CGRP receptor, in the TG. Results: CB1 was ... for transient receptor potential vanilloid 1 (TRPV1) -induced stimulation) and measured using an enzyme-linked immunosorbent ...
Endosomal signaling of the receptor for calcitonin gene-related peptide mediates pain transmission. ...
... ganglion neurons which were immunoreactive to CGRP and the CGRP receptor components calcitonin receptor-like receptor (CLR) and ... CGRP release; calcitonin gene-related peptide; fremanezumab; migraine pain; monoclonal antibody; rat; trigeminal ganglion ... The Anti-Calcitonin Gene-Related Peptide (Anti-CGRP) Antibody Fremanezumab Reduces Trigeminal Neurons Immunoreactive to CGRP ... In preclinical rat experiments, fremanezumab has been shown to reduce calcitonin gene-related peptide (CGRP) release from ...
... receptor antagonist, procalcitonin and C-reactive protein offer a better sensitivity and specificity in predicting serious bact ... Calcitonin Gene-Related Peptide ... Procalcitonin, IL-6, IL-8, IL-1 receptor antagonist and C- ... receptor antagonist, procalcitonin and C-reactive protein offer a better sensitivity and specificity in predicting serious ... IL-8 and interleukin-1 receptor antagonist (IL- Ra) was superior to these commonly used markers for the prediction of a serious ...
Evidence for decreased calcitonin gene-related peptide (CGRP) receptors and compromised responsiveness to CGRP of fetoplacental ... Dive into the research topics of Evidence for decreased calcitonin gene-related peptide (CGRP) receptors and compromised ... Calcitonin Gene-Related Peptide Receptors 100% * Calcitonin Gene-Related Peptide 78% * Receptor Activity-Modifying Protein 1 67 ...
Calcitonin gene-related peptide (CGRP) or adrenomedullin (AM) receptors are heteromers of the calcitonin receptor-like receptor ... Adrenomedullin; Calcitonin gene-related peptide; GPCR; Receptor activity-modifying protein; Molecular modeling; Molecular ... Receptor activity-modifying protein dependent and independent activation mechanisms in the coupling of calcitonin gene-related ... dependent and independent activation mechanisms in the coupling of calcitonin gene-related peptide and adrenomedullin receptors ...
... calcitonin gene-related peptide (CGRP). Some anti-CGRPs target the protein itself, while others target the receptor (blocking ... 2021). Calcitonin gene-related peptide receptor.. https://www.ncbi.nlm.nih.gov/books/NBK560648/. ... Drinking plain water regularly can help prevent dehydration headaches, both flu-related and otherwise. Guidelines for how much ...
Ubrogepant is in a class of medications called calcitonin gene-related peptide receptor antagonists. It works by blocking the ...
Visual Hypersensitivity in Patients Treated With Anti-calcitonin Gene-related Peptide (Receptor) Monoclonal Antibodies Might ... Treatment of Hemiplegic Migraine With Anti-calcitonin Gene-related Peptide Monoclonal Antibodies Hemiplegic migraine is a ... head Observational Cohort Study on the Efficacy and Safety of Monoclonal Antibodies Against Calcitonin Gene-related Peptide for ... Mitochondrial metabolism related markers GDF-15, FGF-21, and HIF-1α are elevated in pediatric migraine attacks. August 19, 2023 ...
... and related medications including drug comparison and health resources. ... Ubrogepant is a calcitonin gene-related peptide receptor antagonist.. Pharmacodynamics. Cardiac Electrophysiology. At a dose 2 ... Ubrelvy (ubrogepant) is a calcitonin gene-related peptide receptor antagonist used for the acute treatment of migraine with or ... The active ingredient of UBRELVY is ubrogepant, a calcitonin gene-related peptide (CGRP) receptor antagonist. The chemical name ...
Viral vectors are commonly used in the manufacture of cell and gene therapies, but come with high manufacturing costs and ... Calcitonin Gene Related Peptide Type 1 Receptor drugs in development, 2023 Sign up for our daily news round-up!. Give your ... Could gene therapy capacity crunch be solved by non-viral transfection?. Cell and gene therapies have drawn huge interest from ... Cell and gene therapies have drawn huge interest from manufacturers, investors and developers alike, but their developers still ...
Rimegepant, an Oral Calcitonin Gene-Related Peptide Receptor Antagonist, for Migraine. N Engl J Med. 2019 Jul 11;381(2):142-149 ... Ferini-Strambi L, Galbiati A, Combi R. Sleep disorder-related headaches. Neurol Sci. 2019 May;40(Suppl 1):107-113. [PubMed: ... In addition, specific questions relating to any possible life-threatening causes of secondary headache should be asked, as the ...
... interacts with receptor activity-modifying protein-1 (RAMP1) to generate a calcitonin gene-related pept... ... Biochemical and functional evidence suggest that the calcitonin receptor-like receptor (CRLR) ... Calcitonin receptor‐like receptor (CLR), receptor activity‐modifying protein 1 (RAMP1), and calcitonin generelated peptide ( ... Functional Calcitonin Gene-related Peptide Receptors Are Formed by the Asymmetric Assembly of a Calcitonin Receptor-like ...
Selective serotonin 1F receptor agonist *Lasmiditan (Reyvow). *Calcitonin-gene related peptide (CGRP) antagonists *Rimegepant ( ...
... receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. Ubrogepant is ... Ubrogepant is a small molecule inhibitor of the calcitonin gene-related peptide (CGRP) ... Ubrogepant (ue broe je pant) is a small molecule inhibitor of the receptor for the calcitonin gene- related peptide (CGRP), ... Ubrogepant is a small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP ...
Calcitonin gene-related peptide (CGRP) receptor antagonist; binds to CGRP receptor, which is thought to be causally involved in ...
Advanced ChemTech VIP Receptor-Binding Inhibitor L-8-K $252.00 SKU-5306 Peptides ... Calcitonin Gene Related Peptide (8-37), human SKU: SKU-4470 Category: Calcitonin, Peptides ...
11] Calcitonin gene-related peptide, nitric oxide, vasoactive intestinal peptide, and substance P function as inhibitory ... Vasoactive intestinal peptide and substance P receptor antagonists improve postoperative ileus. J Surg Res. 1995 Jun. 58(6):719 ... Nitric oxide and vasoactive intestinal peptide inhibitors and substance P receptor antagonists have been demonstrated to ... Farro et al indicate that C-C motif chemokine receptor 2 (CCR2) monocyte-derived macrophages are crucial for resolution of ...
... angiotensin receptor blockers (candesartan); and newer agents such as calcitonin gene-related peptide(CGRP) antagonists ( ... δ-opioid receptors, potassium channels, transient receptor potential ion channels, and acid-sensing ion channels. ... CGRP Receptor Antagonists. CGRP is produced in both the central and peripheral nervous systems and is thought to trigger ... Reduce headache-related distress and psychological symptoms.. Treatment options include both pharmacological and non- ...
1996) Coexpression of preprotachykinin-A, alpha-calcitonin gene-related peptide, somatostatin, and neurotrophin receptor family ... calcitonin gene-related peptide (CGRP), and TMP staining.. Electrophysiological analysis was performed on five different groups ... GDNF receptor component expression within sensory neurons. The signal transducing domain of the GDNF receptor RET was found to ... 1997) Neurturin responsiveness requires a GPI-linked receptor and Ret receptor tyrosine kinase. Nature 387:721-724. ...
Modulation of nocioceptive transmission with calcitonin gene-related peptide receptor antagonists in the thalamus. Brain 133, ... An exploratory study of salivary calcitonin gene-related peptide levels relative to acute interventions and preventative ... Lack of association between oxidative stress-related gene polymorphisms and chronic migraine in an Italian population. Expert ... The impact of topiramate on health-related quality of life indicators in chronic migraine. Headache 47, 1398-1408 (2007). ...
Gepants stop head pain by blocking the receptor for calcitonin gene-related peptide (CGRP), a small protein that the body ... What are serotonin receptor agonists?. Serotonin receptor agonists help to activate serotonin receptors in the central nervous ... Triptans work by activating serotonin receptors, an effect that lowers inflammation and tightens blood vessels. As they ...
Zavzpret is the first calcitonin gene-related peptide (CGRP) receptor antagonist nasal spray. Zavzpret was approved based on ... See separate articles for pipeline information on specialty drugs, biosimilars and gene/cell therapy. ...
Localization of the calcitonin gene-related peptide receptor complex at the vertebrate neuromuscular junction and its role in ... Calcitonin gene-related peptide and muscle activity regulate acetylcholine receptor alpha-subunit mRNA levels by distinct ... Calcitonin gene-related peptide. (CGRP). This peptide is distributed throughout the central and peripheral nervous systems and ... Effect of calcitonin gene-related peptide on contraction of striated muscle in the mouse. Neurosci Lett. 60. 227. 230. ...
... calcitonin gene-related peptide [CGRP] antagonists [gepants], and lasmiditan [a 5-HT1F receptor agonist]) were associated with ... New evidence identified for the updates supported effectiveness of the calcitonin gene-related peptide eptinezumab (one new RCT ... Results for postoperative pain were based on a small number of trials and pain related to a limited set of surgical procedures ... Jayadevappa R, Cook R, Chhatre S. Minimal important difference to infer changes in health-related quality of life-a systematic ...
Calcitonin gene-related peptide (CGRP) inhibitors. CGRP is a type of protein thats released in the brain and can affect ... Gepants (CGRP receptor antagonists). Gepants are small molecules that block CGRP receptors from the peptides. ... 2020). Calcitonin gene-related peptide antagonists for the prevention of migraine: Highlights from pivotal studies and the ... 2021). Role of monoclonal antibodies against calcitonin gene-related peptide (CGRP) in episodic migraine prevention: Where do ...
  • Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drugs that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR). (wikipedia.org)
  • Ubrogepant is in a class of medications called calcitonin gene-related peptide receptor antagonists. (medlineplus.gov)
  • Studies suggest that blocking CGRP is therefore a potential treatment for episodic migraine and in fact, oral CGRP receptor antagonists (known as gepants) such as atogepant, represents a promising new therapy for migraine. (hospitalhealthcare.com)
  • Aim 2 determines whether endosomally-targeted antagonists inhibit channel activity, gene expression and hyperexcitability of neurons. (dtic.mil)
  • Small molecule CGRP receptor antagonists work by blocking the activity of a molecule called calcitonin gene-related peptide (CGRP), which is believed to play a key role in the development of migraines. (psychiatrist.com)
  • The development and optimisation of an HPLC-based in vitro serum stability assay for a calcitonin gene-related peptide receptor antagonist peptide. (iasp-pain.org)
  • Here, we describe the optimisation and validation of a method for the evaluation of the stability of a lead calcitonin gene-related peptide antagonist peptide (P006) in blood serum. (iasp-pain.org)
  • In this study we asked the question whether the determination of procalcitonin (PCT), interleukin (IL)-6, IL-8 and interleukin-1 receptor antagonist (IL- Ra) was superior to these commonly used markers for the prediction of a serious bacterial infection (SBI). (nih.gov)
  • Compared to commonly used screening methods such as the McCarthy score, leucocyte count and other inflammatory markers such as interleukin-6, interleukin-8 and interleukin- receptor antagonist, procalcitonin and C-reactive protein offer a better sensitivity and specificity in predicting serious bacterial infection in children with fever without localising signs. (nih.gov)
  • Ubrelvy (ubrogepant) is a calcitonin gene-related peptide receptor antagonist used for the acute treatment of migraine with or without aura in adults. (rxlist.com)
  • The active ingredient of UBRELVY is ubrogepant, a calcitonin gene-related peptide (CGRP) receptor antagonist . (rxlist.com)
  • In contrast, telcagepant, the initial oral CGRP receptor antagonist evaluated as therapy for migraine headaches, was abandoned during development because of several instances of clinically apparent liver injury in recipients that was characterized by marked elevations in serum aminotransferase levels and symptoms of fatigue, nausea and abdominal discomfort arising within 2 to 4 weeks of starting therapy which rapidly resolved with prompt stopping of therapy. (nih.gov)
  • Zavzpret is the first calcitonin gene-related peptide (CGRP) receptor antagonist nasal spray. (primetherapeutics.com)
  • NEW YORK--(BUSINESS WIRE)-- Pfizer Inc. (NYSE: PFE) today announced the U.S. Food and Drug Administration (FDA) has approved ZAVZPRET™ (zavegepant), the first and only calcitonin gene-related peptide (CGRP) receptor antagonist nasal spray for the acute treatment of migraine with or without aura in adults. (pfizer.com)
  • It is the first nonsteroidal mineralocorticoid receptor (MR) antagonist to be approved for this purpose. (medscape.com)
  • Several monoclonal antibodies that bind to the CGRP receptor or peptide have been approved for prevention of migraine. (wikipedia.org)
  • Several monoclonal antibodies that block CGRP or its receptor are approved for use in prevention of migraines and two small molecule inhibitors of the CGRP receptor (the "gepants": ubrogepant and rimegepant) are available for treatment of acute migraine. (nih.gov)
  • Ubrogepant can be safely given in patients receiving preventive therapy with monoclonal antibodies to CGRP or its receptor. (nih.gov)
  • Migraine prophylactic therapy has changed over recent years with the development and approval of monoclonal antibodies (mAbs) targeting the calcitonin gene-related peptide (CGRP) pathway. (biomedcentral.com)
  • in fact, a new class of drugs to prevent migraines use injections of monoclonal antibodies to target CGRP or its receptor. (futurity.org)
  • The receptors for these peptides are unusual, comprising a G-protein-coupled receptor (GPCR) with receptor activity-modifying proteins (RAMPs). (coventry.ac.uk)
  • The GPCR, the calcitonin receptor-like receptor (CLR), forms a CGRP receptor with RAMP1, (the CGRPR), whereas CLR with RAMP2 or RAMP3 forms two subtypes of adrenomedullin receptor (AM1 and AM2 receptors). (coventry.ac.uk)
  • Neuropeptides substance P, calcitonin gene-related peptide and proteases trypsin stimulated GPCR endocytosis and evoked sustained signals and hyperexcitability in pain-sensing neurons. (dtic.mil)
  • CGRP release was induced by either 60 mM K + (for depolarization-induced stimulation) or 100 nM capsaicin (for transient receptor potential vanilloid 1 (TRPV1) -induced stimulation) and measured using an enzyme-linked immunosorbent assay. (lu.se)
  • MCs can secrete nociceptor sensitizing and activating agents, such as serotonin, prostaglandins, histamine, and proteolytic enzymes that can also activate the pain-mediating transient receptor potential vanilloid channels. (frontiersin.org)
  • CGRP is also a potent agonist at the AMY1(a) receptor, a heterodimer between the calcitonin receptor (CTR) and RAMP1. (coventry.ac.uk)
  • Naratriptan tablets are a serotonin (5-HT 1B/1D ) receptor agonist (triptan) indicated for the acute treatment of migraine with or without aura in adults. (nih.gov)
  • Ubrogepant is a small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. (nih.gov)
  • Ubrogepant (ue broe' je pant) is a small molecule inhibitor of the receptor for the calcitonin gene- related peptide (CGRP), which is believed to play a role in the pathogenesis of migraine headaches. (nih.gov)
  • Calcitonin gene-related peptide (CGRP) or adrenomedullin (AM) receptors are heteromers of the calcitonin receptor-like receptor (CLR), a class B G protein-coupled receptor, and one of three receptor activity-modifying proteins (RAMPs). (essex.ac.uk)
  • The receptor activity-modifying proteins (RAMPs) are a family of three single transmembrane proteins that have been identified as accessory proteins to some G-protein-coupled receptors (GPCRs). (nih.gov)
  • To keep CGRP receptors out of endosomes, the researchers inhibited clathrin and dynamin, two proteins that are important for substances entering cells. (futurity.org)
  • The analysis of CGRP release data was combined with immunohistochemistry in order to study the cellular localization of CB1, cannabinoid receptor type 2 (CB2), CGRP and receptor activity modifying protein 1 (RAMP1), a subunit of the functional CGRP receptor, in the TG. (lu.se)
  • After fremanezumab treatment , the fraction of trigeminal ganglion neurons which were immunoreactive to CGRP and the CGRP receptor components calcitonin receptor-like receptor (CLR) and receptor activity modifying protein 1 (RAMP1) was significantly lowered compared to the control. (bvsalud.org)
  • Biochemical and functional evidence suggest that the calcitonin receptor-like receptor (CRLR) interacts with receptor activity-modifying protein-1 (RAMP1) to generate a calcitonin gene-related peptide (CGRP) receptor. (acs.org)
  • The homodimerization of the coreceptor was further confirmed by the ability of RAMP1 to prevent cell surface targeting of a truncated RAMP1 that normally exhibits receptor-independent plasma membrane delivery. (acs.org)
  • In addition to shed new light on the CRLR−RAMP1 signaling complex, the BRET assays developed herein offer new biosensors for probing CGRP receptor activity. (acs.org)
  • The association of RAMP1 with the calcitonin receptor-like receptor (CL) constitutes the calcitonin gene-related peptide receptor, whereas RAMP2 or 3 with CL generates adrenomedullin receptors. (nih.gov)
  • The researchers studied mice in which the CGRP receptor, called CLR/RAMP1, was disabled in Schwann cells. (futurity.org)
  • They modified the CGRP receptor by deleting RAMP1, one of two important components of the receptor, from Schwann cells in the facial area of mice. (futurity.org)
  • Calcitonin gene-related peptide (CGRP), adrenomedullin (AM) and adrenomedullin 2 (AM2) are related peptides, which are potent vasodilators. (coventry.ac.uk)
  • The data suggest that hydrophobic interactions are more important for CLR activation than other class B GPCRs, providing new insights into the mechanisms of activation of this class of receptor. (essex.ac.uk)
  • The best characterized receptor complexes formed by RAMPs and GPCRs are the calcitonin peptide family receptors. (nih.gov)
  • The grant seeks to determine whether G protein-coupled receptors GPCRs in endosomes, rather than at the plasma membrane, are mediators and therapeutic targets for chronic pain. (dtic.mil)
  • Aim 1 examines whether GPCRs in endosomes control activity of ion channels and expression of genes that induce sustained neuronal excitation. (dtic.mil)
  • Mitochondrial metabolism related markers GDF-15, FGF-21, and HIF-1α are elevated in pediatric migraine attacks. (medscape.com)
  • Gepants stop head pain by blocking the receptor for calcitonin gene-related peptide (CGRP), a small protein that the body releases during migraine episodes. (medicalnewstoday.com)
  • However, a third of sensory neurons do not express receptors for the neurotrophins. (jneurosci.org)
  • MCs express receptors for both estrogen and progesterone that induce degranulation upon binding. (frontiersin.org)
  • Although the RAMPs themselves are not responsive to calcitonin peptide family ligands, there is clear evidence that they participate in ligand binding, although it is still unclear whether this is by directly participating in binding or through allosteric modulation of CL or CTR. (nih.gov)
  • The data reveal key regions in RAMPs that are important for ligand binding and receptor interactions. (nih.gov)
  • A long-lasting reduction in CGRP receptors expressed in trigeminal afferents may contribute to the attenuation of CGRP signalling and antinociceptive effects of monoclonal anti-CGRP antibodies in rats . (bvsalud.org)
  • Might treatment with anti-CGRP receptor antibodies reduce visual hypersensitivity in patients with migraine? (medscape.com)
  • iii) stopping rules of antibodies targeting the CGRP (receptor). (biomedcentral.com)
  • In the field of cephalalgias, migraine has a prominent role (35,311 publications retrieved for search terms "migraine" in PubMed, accessed on August 15, 2018), with the recent breakthrough in therapeutics, represented by the successful clinical development of calcitonin gene-related peptide (CGRP) antibodies [ 1 ]. (biomedcentral.com)
  • In the field of headache, we have an entirely new class of drugs for the prevention of migraine: antibodies against calcitonin gene-related peptide (CGRP) or the CGRP receptor. (medscape.com)
  • Triptans work by activating serotonin receptors, an effect that lowers inflammation and tightens blood vessels. (medicalnewstoday.com)
  • Acute treatment involves the use of 5HT 1 -receptor agonists ('or triptans') of which there are several e.g., sumatriptan. (hospitalhealthcare.com)
  • The development of the anti-migraine therapeutics, triptans-5-HT 1B/1D receptor agonists, had originally targeted the craniovasculature to exert therapeutic effects, and this locus of action seemed to predict efficacy in the clinic. (medscape.com)
  • Although clinically distinguishable, migraine and cluster headache share prominent features such as unilateral pain, common pharmacological triggers such glyceryl trinitrate, histamine, calcitonin gene-related peptide (CGRP) and response to triptans and neuromodulation. (biomedcentral.com)
  • Amylin receptor subtypes are formed from calcitonin receptor (CTR) interactions with RAMPs. (nih.gov)
  • Calcitonin gene-related peptide (CGRP) is a mediator of nociceptive processing and may serve as a target for therapy. (aspetjournals.org)
  • We have defined how CGRP and AM induce Gs-coupling in CLR-RAMP heteromers by measuring the effect of targeted mutagenesis in the CLR transmembrane domain on cAMP production, modeling the active state conformations of CGRP and AM receptors in complex with the Gs C-terminus and conducting molecular dynamics simulations in an explicitly hydrated lipidic bilayer. (essex.ac.uk)
  • Levels of CGRP are elevated during episodes of migraine headache, and administration of the peptide can induce migraines in susceptible patients. (nih.gov)
  • The aim of the present study was to examine the effect of the synthetic endocannabinoid (eCB) analogue, arachidonyl-2′-chloroethylamide (ACEA), on calcitonin gene-related peptide (CGRP) release in the dura and trigeminal ganglion (TG), as cannabinoids are known to activate G i/o -coupled cannabinoid receptors type 1 (CB1), resulting in neuronal inhibition. (lu.se)
  • coupled cannabinoid receptors type 1 (CB1), resulting in neuronal inhibition. (lu.se)
  • Inhibition of influenza A virus matrix and nonstructural gene expression using RNA interference. (cdc.gov)
  • Interleukin-11 receptor subunit alpha-1 is required for maximal airway responsiveness to methacholine following acute exposure to ozone. (cdc.gov)
  • The Anti-Calcitonin Gene-Related Peptide (Anti-CGRP) Antibody Fremanezumab Reduces Trigeminal Neurons Immunoreactive to CGRP and CGRP Receptor Components in Rats. (bvsalud.org)
  • Here we show that these neurons express the receptor components for glial-derived neurotrophic factor (GDNF) signaling (RET, GFRα-1, and GFRα-2). (jneurosci.org)
  • The trk receptors in general are expressed in a nonoverlapping manner by sensory neurons in combination with the low-affinity neurotrophin receptor p75 ( Wright and Snider, 1995 ). (jneurosci.org)
  • In preclinical rat experiments, fremanezumab has been shown to reduce calcitonin gene-related peptide (CGRP) release from trigeminal tissues and aversive behaviour to noxious facial stimuli, which are characteristic pathophysiological changes accompanying severe primary headaches . (bvsalud.org)
  • Migraine involves incapacitating head pain and physical impairment, frequently accompanied by nausea, vomiting, and aura-related sound or other sensory disturbances. (amgen.com)
  • The rest are sensory in nature, although the largest sensory receptors, the neuromuscular spindles, have a motor supply of their own. (medscape.com)
  • These genes are not involved in common migraine [ 17 ] or in CH [ 8 ], in which numerous genes and environmental factors contribute to susceptibility in a manner still unclear. (biomedcentral.com)
  • Development of asthma is multifactorial and depends on the interactions among multiple susceptibility genes and environmental factors. (msdmanuals.com)
  • Again, capsaicin did not cause migraine-like pain in mice lacking the CGRP receptor in Schwann cells, providing further support for the idea that the CGRP receptor in Schwann cells plays a critical role in migraine pain. (futurity.org)
  • The current suggestion to discontinue CGRP(-receptor) targeted mAbs after 6 to 12 months is based on expert opinion, as opposed to robust scientific evidence. (biomedcentral.com)
  • In addition, observational studies and, eventually, clinical trials focusing on the effect of discontinuation of migraine prophylactic therapies, are essential to substantiate evidence-based recommendations on stopping rules for both oral preventives and CGRP(-receptor) targeted therapies in migraine. (biomedcentral.com)
  • This article covers the pharmacology of these receptors, their structure, distribution, and potential involvement in disease. (coventry.ac.uk)
  • Ergotamine and its derivatives work by activating the 5-HT1D receptors, causing vasoconstriction of intracranial blood vessels and inhibiting the release of inflammatory neuropeptides. (pharmacytimes.com)
  • Cell and gene therapies have drawn huge interest from manufacturers, investors and developers, but still face manufacturing bottlenecks. (pharmaceutical-technology.com)
  • Cell and gene therapies have drawn huge interest from manufacturers, investors and developers alike. (pharmaceutical-technology.com)
  • Viral vectors are commonly used in the manufacture of cell and gene therapies, but come with high manufacturing costs and capacity constraints. (pharmaceutical-technology.com)
  • Cell and gene therapies have drawn huge interest from manufacturers, investors and developers alike, but their developers still face manufacturing bottlenecks due to a lack of manufacturing facilities with the relevant equipment, know-how or raw materials. (pharmaceutical-technology.com)
  • They could therefore make cell and gene therapies cheaper and improve their uptake with healthcare providers and patients. (pharmaceutical-technology.com)
  • Within endosomes, the CGRP receptor continues to signal for prolonged periods of time. (futurity.org)
  • This new understanding of how pain originates inside Schwann cells gave the researchers two ideas for treating migraine pain: stopping the CGRP receptor from entering endosomes in the first place, or using nanoparticles to send drugs targeting the CGRP receptor in endosomes. (futurity.org)
  • In Schwann cells, the nanoparticles carried the drug into endosomes and blocked the CGRP receptor, which strongly inhibited migraine pain. (futurity.org)
  • Parental occupational exposure to solvents and autism spectrum disorder: An exploratory look at gene-environment interactions. (cdc.gov)
  • Its mechanism of action is by blocking CGRP receptor of nerve cells, which trigger intense pain and activate CGRP cascade, which prevents the immune system attacks to control the pathogen. (wikipedia.org)
  • The molecular underpinnings common to and connecting these disorders are not known, but may include shared genetic risk factors ( 1 , 8 ), regulation of brain cations ( 9 , 10 ), or common receptor signaling events that activate pain ( 11 ), inflammation ( 12 ), or oxidative ( 13 ) pathways. (frontiersin.org)
  • Aryl hydrocarbon receptors improve migraine-like pain behaviors in rats through the regulation of regulatory T cell/T-helper 17 cell-related homeostasis. (medscape.com)
  • Erenumab specifically targets the Calcitonin-Gene-Related-Peptide (CGRP) receptor, which is believed to transmit signals that can cause incapacitating pain. (amgen.com)
  • However, in mice lacking the CGRP receptor in Schwann cells, CGRP did not cause pain. (futurity.org)
  • The researchers also successfully blocked CGRP-evoked pain using nanoparticles in which they encapsulated a small molecule drug that binds to and blocks the CGRP receptor. (futurity.org)
  • Pedro stated: "One of the main disadvantages of viral vectors is related to their difficulty in manufacturing dose at scale. (pharmaceutical-technology.com)
  • A second approach was also studied, [ 6 ] with a single-dose gene replacement therapy for SMA in which the SMA gene is applied with a viral vector. (medscape.com)
  • Zavegepant, which will be sold under the brand name Zavzpret, is the first and only calcitonin gene-related peptide (CGRP) receptor to be approved by the agency for migraine treatment. (psychiatrist.com)
  • Could gene therapy capacity crunch be solved by non-viral transfection? (pharmaceutical-technology.com)
  • See separate articles for pipeline information on specialty drugs, biosimilars and gene/cell therapy. (primetherapeutics.com)
  • it showed an improvement in achieving motor milestones in these children after gene therapy. (medscape.com)
  • The largest effects on receptor signaling were seen with H295A5.40b, I298A5.43b, L302A5.47b, N305A5.50b, L345A6.49b and E348A6.52b, F349A6.53b and H374A7.47b (class B numbering in superscript). (essex.ac.uk)
  • Genetic variants in the major histocompatibility complex class I and class II genes are associated with diisocyanate-induced Asthma. (cdc.gov)
  • SIGNIFICANCE STATEMENT A monoclonal antibody against calcitonin gene-related peptide (CGRP) was found to reduce concomitant colonic and bladder hypersensitivity and hyperpermeability. (aspetjournals.org)
  • In mouse embryos, cells seem prepatterned to become certain cell lineage because the first cleavage plane has been related with further embryonic-abembryonic axis at the blastocyst stage. (bioone.org)
  • This increases low-density lipoprotein (LDL-C) receptor recycling and expression on the hepatocyte cell surface, which increases LDL-C uptake and lowers LDL-C levels in the circulation. (medscape.com)
  • They found that when CGRP binds to its receptor on a Schwann cell, the receptor moves into a compartment inside the cell called an endosome. (futurity.org)
  • It is essential for cell homeostasis and survival and has been related to various diseases and pathophysiology. (helsinki.fi)
  • After initially determining appropriate peptide and human serum concentrations and selection of the quenching reagent, the HPLC method optimisation used two experimental designs, Plackett-Burman design and Taguchi design. (iasp-pain.org)
  • Aimovig is a fully human monoclonal antibody, designed to selectively block the calcitonin gene-related peptide (CGRP) receptor. (empr.com)
  • Aimovig, a fully human monoclonal antibody, works by selectively blocking the calcitonin gene-related peptide (CGRP) receptor, which is involved in migraine activation. (empr.com)