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Class of cell surface receptors
Sigma receptors (σ-receptors) are protein receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine
Sigma_receptor
Chaperone protein
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling
Sigma-1_receptor
Protein-coding gene in the species Homo sapiens
The sigma-2 receptor (σ2R) is a sigma receptor subtype that has attracted attention due to its involvement in diseases such as neurological diseases, neurodegenerative
Sigma-2_receptor
Eighteenth letter of the Greek alphabet
as the absolute mean value. In biology, the sigma receptor (σ–receptors) is a type of cell surface receptor. In biochemistry, the σ factor (or specificity
Sigma
Chemical compound
is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 9 ± 1 nM for the sigma-1 receptor and more than 49 times selectivity
BD1063
Class of antidepressant medication
gradual changes in brain signaling and receptor regulation, with some also interacting with sigma-1 receptors, particularly fluvoxamine, which may contribute
Selective serotonin reuptake inhibitor
Selective_serotonin_reuptake_inhibitor
Topics referred to by the same term
quantum physics Sigma baryon in particle physics Sigma receptor, a neural receptor Surface charge density in classical electromagnetism Sigma, a Greek letter
Sigma_(disambiguation)
Chemical compound
selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor
BD1008
Pharmaceutical compound
the sigma receptors and shows high affinity for 3-PPP-labeled sigma receptors (Ki = 5.3 nM). Its selectivity for the sigma σ1 versus σ2 receptor is unknown
SR-31742A
Chemical compound
PRE-084 is a sigma receptor agonist, selective for the σ1 subtype. It has nootropic and antidepressant actions in animal studies, as well as antitussive
PRE-084
Sigma σ2 receptor ligand
Lu 29-252 is a selective sigma σ2 receptor ligand which was under development for the treatment of anxiety disorders but was never marketed. It reached
Lu_29-252
Synthetic opioid analgesic
activity, the drug is a sigma receptor agonist, and has been used widely in scientific research in studies of this receptor. Alazocine is described as
Alazocine
Sigma-1 receptor antagonist
selective antagonist of the sigma-1 receptor. It possesses anti-psychotic properties. MS-377 acts selectively at the sigma-1 receptor as an antagonist. It does
MS-377
Chemical compound
is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 3 ± 0.1 nM for the sigma-1 receptor and greater than 50 times
BD1060
Chemical compound
2-a]pyrazine is a selective sigma receptor ligand, with a reported binding affinity of Ki = 5 ± 0.7 nM for the sigma-1 receptor and approximately 10 times
BD1018
Chemical compound
selective sigma receptor agonist, with a reported binding affinity of Ki = 2 ± 0.5 nM for the sigma-1 receptor and 30 times selectivity over the sigma-2 receptor
BD1052
Central nervous system stimulant
Methamphetamine binds to and activates both sigma receptor subtypes, σ1 and σ2, with micromolar affinity. Sigma receptor activation may promote methamphetamine-induced
Methamphetamine
Chemical compound
selective sigma receptor antagonist, with reported binding affinity of Ki = 30 ± 2 nM for the sigma-1 receptor and Ki = 138 ± 18 nM for the sigma-2 receptor, and
AC927
Chemical compound
International Nonproprietary Name; developmental code name EMD-57455) is a sigma receptor antagonist that was under development by Merck as a potential antipsychotic
Panamesine
Piperazine based chemical compound
piperazine based chemical compound with nanomolar affinity for both sigma receptor subtypes that has been shown to counteract the deleterious effects of
CM156
Chemical compound
Cutamesine (SA 4503) is a synthetic sigma receptor agonist which is selective for the σ1 receptor, a chaperone protein mainly found in the endoplasmic
Cutamesine
Experimental drug
Ditolylguanidine (DTG) is a sigma receptor agonist. It is somewhat selective for sigma receptors, but non-selective between the two sigma receptor subtypes, binding
Ditolylguanidine
Investigational antipsychotics
Roluperidone (CYR-101; MIN-101; MT-210) – serotonin 5-HT2A receptor antagonist, sigma σ2 receptor antagonist, and other actions – schizophrenia [2] Brilaroxazine
List of investigational antipsychotics
List_of_investigational_antipsychotics
Chemical compound
fenpropimorph is also a very high affinity ligand of the mammalian sigma receptor. Amorolfine - same core structure but with a tert-amyl group in place
Fenpropimorph
Chemical compound
mixed sigma σ1 and σ2 receptor agonist (with similar affinity for both subtypes, though slightly higher affinity for the latter) and D2 receptor partial
3-PPP
Chemical compound
serotonin, dopamine and noradrenaline. It also acts as a high affinity sigma receptor ligand, selective for the σ2 subtype. It produces both stimulant and
3-Methyl-PCPy
Chemical compound
is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 0.5 nM for the sigma-1 receptor and greater than 19 times
BD1067
Dissociative hallucinogenic drug, mostly used recreationally
member of the arylcyclohexylamine class. PCP works primarily as an NMDA receptor antagonist. PCP is most commonly used in the US. While usage peaked in
Phencyclidine
Pharmaceutical compound
receptors, glutamate receptors, GABA receptors, opioid receptors, and sigma receptors. There were five hits (>50% binding inhibition), which included the
Compound 22 (TAAR1 antagonist)
Compound_22_(TAAR1_antagonist)
Group of protein families
hormone receptors are found in the nucleus, cytosol, and also on the plasma membrane of target cells. They are generally intracellular receptors (typically
Steroid_hormone_receptor
Psychoactive substance found in plants in the family Apocynaceae
sigma, NMDA, and nicotinic acetylcholine receptors; its metabolite noribogaine primarily acts as a serotonin reuptake inhibitor and κ-opioid receptor
Ibogaine
Experimental antiparkinsonian agent and adamantane derivative
sigma receptor agonist. Analogues of hemantane, such as memantine and amantadine, share some of these actions, like NMDA receptor antagonism, sigma receptor
Hemantane
Chemical compound
selective sigma receptor agonist, with a reported binding affinity of Ki = 1 ± 0.2 nM for the sigma-1 receptor and 80 times selectivity over the sigma-2 receptor
BD1031
Antihistamine and calcium channel blocker medication
movement. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether
Cinnarizine
Pharmaceutical drug
"Structure-activity relationships and evolution of sigma receptor ligands (1976-present)". In Itzhak Y (ed.). Sigma Receptors. Neuroscience Perspectives. Elsevier Science
Deprenyl
Drug class
opposed to these effects being mediated by concomitant sigma receptor agonism. κ-Opioid receptor § Agonists List of hallucinogens Dalefield ML, Scouller
Κ-Opioid_receptor_agonist
Chemical compound
affinity for the sigma receptor, where it acts as an agonist, whereas esketamine binds negligibly to this receptor, and so the sigma receptor activity of racemic
Arketamine
Cough suppressant and dissociative drug
reuptake inhibitor and a sigma-1 receptor agonist. Dextromethorphan and its major metabolite dextrorphan also block the NMDA receptor at high doses, producing
Dextromethorphan
Pharmaceutical compound
as AF710B, is a muscarinic acetylcholine M1 receptor positive allosteric modulator and sigma σ1 receptor agonist which is under development for the treatment
ANAVEX_3-71
Index of chemical compounds with the same molecular formula
299.24 g/mol) may refer to: BD1018, a selective sigma receptor ligand BD1031, a selective sigma receptor agonist This set index page lists chemical structure
C15H20Cl2N2
Medication mainly used for depression and smoking cessation
Bupropion has been claimed to be a sigma σ1 receptor agonist. Its antidepressant-like effects in rodents depend on σ1 receptor activation. They are enhanced
Bupropion
Stimulant drug
to explain certain differences in pharmacology. It is possible that sigma receptor activity might also account for some of the differences between cocaine
(+)-CPCA
Tricyclic antidepressant
"1,3-Di(2-[5-3H]tolyl)guanidine: a selective ligand that labels sigma-type receptors for psychotomimetic opiates and antipsychotic drugs". Proceedings
Amitriptyline
Anticonvulsant medication
channel-blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side effects with other
Lamotrigine
Antihistamine used to treat allergies
first-generation antihistamine and works by blocking the histamine H1 receptor. Common side effects include sleepiness, restlessness, and weakness. Other
Chlorphenamine
Chemical compound
the serotonin 5-HT2A receptor and also interacts with other serotonin receptors. The drug activates the serotonin 5-HT2A receptor with sufficiently high
Zalsupindole
Chemical compound
sigma-1 receptor antagonist, with a reported binding affinity of Ki = 1.03 ± 0.01 nM, and more than 205 times selectivity over the sigma-2 receptor.
NE-100
Pharmaceutical compound
shows substantial interaction with the serotonin 5-HT3 receptor and the sigma σ1 and σ2 receptor (92.5–95.1% binding inhibition, relative to 94.9% at the
UCD0168
Chemical compound
Rimcazole is an antagonist of the sigma receptor as well as a dopamine reuptake inhibitor. Sigma receptors are thought to be involved in the drug psychosis
Rimcazole
Chemical compound
L-687,384 is a sigma receptor agonist, selective for the σ1 subtype, as well as an NMDA antagonist. Bergeron R, Debonnel G (February 1997). "Effects of
L-687,384
Typical antipsychotic medication
octopamine receptor β, high for Drosophila tyramine receptor 1, intermediate for migratory locust (Locusta migratoria) tyramine receptor 1, and high
Chlorpromazine
Drug used to treat depressive and anxiety disorders
most other tricyclic antidepressants, and instead acts primarily as a sigma-1 receptor agonist. It was developed by Schindler and Blattner in 1961. Opipramol
Opipramol
Chemical compound
of the sigma σ1 receptor (Ki = 870 nM) and has some affinity for certain serotonin receptors including the serotonin 5-HT1A and 5-HT2A receptors. In animals
Mesdopetam
Sedating antihistamine
primarily as a strong antagonist of the H1 receptor (antihistamine, Ki = 1.4 nM) and a moderate mACh receptor antagonist (anticholinergic), and also has
Promethazine
Pharmaceutical compound
also act on sigma receptors. In addition to the KOR, it has affinity for the μ-opioid receptor (MOR), but does not activate this receptor. The drug produces
MR-2034
Investigational other psychiatric disorder drugs
d-DM; deuterated-DM; deuDXM; deu-DXM; deuterated DXM) – NMDA receptor antagonist, sigma receptor agonist, other actions – impulse–control disorders [10] Fasedienol
List of investigational other psychiatric disorder drugs
List_of_investigational_other_psychiatric_disorder_drugs
Chemical compound
selective serotonin 5-HT2A, 5-HT1A, or 5-HT1B receptor antagonists nor by a selective sigma σ1 receptor antagonist in vivo. The drug's beneficial effects
Dipropyltryptamine
Anti-seizure medication
also: Receptor/signaling modulators • Transient receptor potential channel modulators v t e Sigma receptor modulators σ1 Agonists: 3-PPP 4-PPBP 5-MeO-DMT
Phenytoin
Class of medications used to alleviate anxiety
GABAergic, NGF and BDNF release promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma receptor agonism thought to have some involvement. Bromantane
Anxiolytic
Pharmaceutical compound
States Adopted Name; developmental code name CT-1812 or CT1812) is a sigma σ2 receptor antagonist which is under development for the treatment of Alzheimer's
Zervimesine
SSRI antidepressant
Hashimoto K (2017). "Sigma-1 Receptor Agonists and Their Clinical Implications in Neuropsychiatric Disorders". Sigma Receptors: Their Role in Disease
Sertraline
Dissociative anesthetic and anti-depressant
Ketamine is a cyclohexanone-derived general anesthetic and NMDA receptor antagonist with analgesic and hallucinogenic properties, used medically for anesthesia
Ketamine
Typical antipsychotic medication
dopaminergic D2 and D1 receptors in the basal ganglia, cortical and limbic system. It also blocks α1 adrenergic receptors, muscarinic M1 receptors, and histaminergic
Fluphenazine
Experimental drug for stimulant use disorder
profile of modafinil. However, RDS03-94 also has high affinity for the sigma σ1 receptor (Ki = 2.19 nM). RDS03-94 shows some reversal of tetrabenazine-induced
RDS03-94
Opioid analgesic
whereas it has relatively low affinity for the δ-opioid receptor (DOR) and sigma receptors. Nalbuphine was patented in 1968 and was introduced for medical
Nalbuphine
Chemical compound
Igmesine (JO-1,784) is a sigma receptor agonist (IC50 = 39 nM (rat brain)). It has neuroprotective and antidepressant-like effects in animal studies, as
Igmesine
Opioid used to treat pain and opioid use disorder
buprenorphine binds only weakly to and possesses little if any activity at the sigma receptor. Buprenorphine also blocks voltage-gated sodium channels via the local
Buprenorphine
Beta blocker drug
is a non-selective beta blocker which works by blocking β-adrenergic receptors. Propranolol was patented in 1962 and approved for medical use in 1964
Propranolol
Chemical compound
dimethyltryptamine (DMT) but are longer-lasting, with durations of up to 3 hours. The receptor interactions of DALT have been studied. The drug produces the head-twitch
DALT
Cocaine-like dopamine reuptake inhibitor derived from modafinil
290-fold less than for the DAT). It also binds with high affinity to the sigma σ1 receptor (Ki = 41.6 nM). The drug has high affinity for the hERG antitarget
JJC8-088
Chemical compound
the σ1 receptor (Ki = 20 nM) (likely an agonist), GIRK channel blocker (described as "potent"), antihistamine (Ki = 3.8 nM for the H1 receptor), and anticholinergic
Cloperastine
Principal psychoactive metabolite of the oneirogen ibogaine
bind to the sigma σ2 receptor. Similarly to ibogaine, noribogaine acts as a weak NMDA receptor antagonist and binds to opioid receptors. It has greater
Noribogaine
Chemical compound
derivative of piracetam and a positive allosteric modulator of the sigma-1 receptor. It differs from phenylpiracetam by having a methyl group. E1R is the
Methylphenylpiracetam
SSRI antidepressant
nausea. Nausea is often caused when the 5-HT3 receptors actively absorb free serotonin, as this receptor is present within the digestive tract. Citalopram
Citalopram
Chemical substance that alters brain function
their primary neurotransmitter, receptor or method of action. Many drugs act on more than one transmitter or receptor in the brain. Psychoactive drugs
Psychoactive_drug
Chemical compound
Siramesine (or Lu 28-179) is a sigma receptor agonist, selective for the σ2 subtype. In animal studies, siramesine has been shown to produce anxiolytic
Siramesine
Chemical compound
is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 2 ± 0.1 nM for the sigma-1 receptor and more than 350 times
LR132
Cough suppressant drug susceptible to misuse
CNS and peripheral nervous system. Dextromethorphan is primarily a sigma receptor agonist and an SNRI, and dextromethorphan's effects as a dissociative
Recreational use of dextromethorphan
Recreational_use_of_dextromethorphan
SNRI antidepressant
and migraine prevention. It may work on pain via effects on the opioid receptor. It has also been found to reduce the severity of 'hot flashes' in menopausal
Venlafaxine
Pharmaceutical compound
pridopidine was found to act as a sigma receptor ligand with much higher affinity than for the dopamine D2 receptor, with this balance of activities potentially
Ordopidine
Compound which binds to the sigma-2 receptor, a cell-membrane protein
protein, the sigma-2 receptor, found in cell membranes. It is highly selective for this over the related sigma-1 receptor. The sigma-2 receptor is significant
SAS-1121
SSRI antidepressant
astemizole, mizolastine), macrolide and fluoroquinolone antibiotics, some 5-HT3 receptor antagonists (except palonosetron), and some antiretrovirals (e.g., ritonavir
Escitalopram
Chemical compound
α2-adrenergic receptor. However, this occurs at concentrations well above its MAE actions. The drug is also a weak agonist of the sigma receptor likewise at
Benzofuranylpropylaminopentane
Benzofuranylpropylaminopentane
Medication used for dementia
S2CID 8460305. Maurice T, Su TP (November 2009). "The pharmacology of sigma-1 receptors". Pharmacology & Therapeutics. 124 (2): 195–206. doi:10.1016/j.pharmthera
Donepezil
Abandoned drug
dopamine D2 receptor (Ki = 228 nM), the dopamine D3 receptor (Ki = 65.9 nM), the dopamine D4 receptor (Ki = 28.1 nM), and the sigma σ1 receptor (Ki = 159 nM)
JJC8-016
Chemical compound
ligand-gated ion channels, pregnenolone sulfate is an agonist of the sigma receptor, as well as an activator of the TRPM1 and TRPM3 channels. It may also
Pregnenolone_sulfate
Spice made from crocus flowers
also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators v t e Sigma receptor modulators
Saffron
Chemical compound
molecule investigational drug. Pridopidine is a selective and potent sigma-1 receptor agonist. It is being developed by Prilenia Therapeutics and is currently
Pridopidine
Typical antipsychotic medication
decline in gray matter volume. Haloperidol irreversibly blocks the sigma σ1 receptor. It may exert deleterious effects on the dorsolateral prefrontal cortex
Haloperidol
Antipsychotic medication
Remoxipride acts as a selective D2 and D3 receptor antagonist and also has high affinity for the sigma receptor, possibly playing a role in its atypical
Remoxipride
First generation antihistamine
known as pyrilamine, is a first-generation antihistamine, targeting the H1 receptor as an inverse agonist. Mepyramine rapidly permeates the brain, often causing
Mepyramine
Medication
disorders is uncommon, controversial, and less frequent than with dopamine receptor agonists like pramipexole. Impulse control disorders with dopaminergic
Selegiline
Chemical compound
that was briefly marketed as a cough suppressant. It binds to the sigma-1 receptor with an IC50 value of 190 nM. It also has local anesthetic action,
Pipazetate
Combination medication
PMID 31124380. Sałaciak K, Pytka K (January 2022). "Revisiting the sigma-1 receptor as a biological target to treat affective and cognitive disorders"
Dextromethorphan/bupropion
Chemical compound
80–. ISBN 978-94-011-4439-1. Stone TW (January 1993). Acetylcholine, Sigma Receptors, CCK and Eicosanoids, Neurotoxins. Taylor & Francis. pp. 124–. ISBN 978-0-7484-0063-8
Clorgiline
Chemical compound
inhibits GIRK channels and interacts with α1-adrenergic, serotonin, and sigma receptors. Chemically, ifenprodil is a substituted phenethylamine and β-hydroxyamphetamine
Ifenprodil
Pharmaceutical compound
2T-2CTFM-3PIP, and Z3517967757 (Z7757), the antipsychotic OSU-6162, and the sigma receptor agonist 3-PPP. Chemical structures of selected 3-phenylpiperidines 3-Phenylpiperidine
3-Phenylpiperidine
Medication used to treat Alzheimer's disease
relevance of Memantine's D2 receptor action, suggesting a low Ki value. Memantine acts as a weak agonist of the sigma σ1 receptor with low affinity (Ki =
Memantine
Substance having effect(s) on the body of an individual
acetylcholine receptor modulators Others: Imidazoline receptor modulators Purine receptor modulators Sigma receptor modulators Thyroid hormone receptor modulators
Drug
American pharmacologist and biologist
leader in research on sigma receptors and is generally credited with the discovery and initial characterization of the sigma-2 receptor. "Bowen, Wayne". vivo
Wayne_Bowen
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SIGMA RECEPTOR
SIGMA RECEPTOR
Girl/Female
Hindu
Boundary, Border
Girl/Female
Latin
Sign.
Surname or Lastname
English
English : patronymic from Sim.Jewish (Ashkenazic) : metronymic from the Yiddish female personal name Sime (see Sima).
Boy/Male
Hindu, Indian, Muslim
Powerful; Mighty; Strong; Rich; Successful
Female
Hindi/Indian
(सीमा) Hindi name SIMA means "boundary, limit." Compare with another form of Sima.
Boy/Male
Arabic, Muslim
Gold Stigma of a Flower; Derived from Zarparan
Girl/Female
British, Danish, English, German, Swedish
Powerful Silence; Peaceful Victory
Surname or Lastname
English (Midlands)
English (Midlands) : from the Middle English personal name, a pet form of Sim.Jewish (from Belarus) : metronymic from Simke, a pet form of the Yiddish female personal name Sime (see Sima) with the eastern Slavic possessive suffix -in.
Girl/Female
Danish, German, Latin, Scandinavian, Swedish
Sign; Signal; Victory
Girl/Female
Tamil
Boundary, Border
Boy/Male
Norse
Victorious defender.
Girl/Female
Arabic, Muslim
Peace
Surname or Lastname
English
English : patronymic from a short form of the personal name Simon.Jewish (from Ukraine; Symes, Symis) : metronymic from the Yiddish female personal name Sime (see Sima).Benjamin Syms was a planter and philanthropist, probably the earliest inhabitant of any North American colony to bequeath property for the establishment of a free school. His name was spelled variously as Sims, Simes, Sym, Symms, Syms, and Symes. He was probably born in England, but was reported in the VA census of 1624/25 as age 33 and living at Basse’s Choice in what was later known as Isle of Wight County.
Girl/Female
Scottish
Listener.
Male
Hebrew
(ש×Öµ×) Hebrew name SHEM means "conspicuous position, name, renown, sigma." In the bible, this is the name of a son of Noah.
Girl/Female
Afghan, Arabic, Armenian, Australian, Farsi, French, Gujarati, Hebrew, Hindu, Indian, Malayalam, Muslim, Sanskrit, Tamil
Limit; Border; Listener; Precious Thing; Treasure; Boundary; Bank; Shore
Female
Hindi/Indian
(सीमा) Variant spelling of Hindi Sima, SEEMA means "boundary, limit." Compare with another form of Seema.
SIGMA RECEPTOR
SIGMA RECEPTOR
SIGMA RECEPTOR
SIGMA RECEPTOR
SIGMA RECEPTOR
SIGMA RECEPTOR
SIGMA RECEPTOR
v. t.
That part of a pistil which has no epidermis, and is fitted to receive the pollen. It is usually the terminal portion, and is commonly somewhat glutinous or viscid. See Illust. of Stamen and of Flower.
v. t.
A red speck upon the skin, produced either by the extravasation of blood, as in the bloody sweat characteristic of certain varieties of religious ecstasy, or by capillary congestion, as in the case of drunkards.
n. pl.
The signs, abbreviations, letters, or characters standing for words, shorthand, etc., in ancient manuscripts, or on coins, medals, etc.
pl.
of Stigma
v. t.
To apply pollen to (a stigma).
n.
The Greek letter /, /, or / (English S, or s). It originally had the form of the English C.
pl.
of Stigma
v. t.
A point so connected by any law whatever with another point, called an index, that as the index moves in any manner in a plane the first point or stigma moves in a determinate way in the same plane.
a.
Of or pertaining to a stigma or stigmata.
n.
Stigma; brand; reproach.
pl.
of Sigma
n.
pl. of Stigma.
v. t.
One of the apertures of the gill of an ascidian, and of Amphioxus.
v. t.
One of the external openings of the tracheae of insects, myriapods, and other arthropods; a spiracle.
v. t.
One of the apertures of the pulmonary sacs of arachnids. See Illust. of Scorpion.
v. t.
A small spot, mark, scar, or a minute hole; -- applied especially to a spot on the outer surface of a Graafian follicle, and to spots of intercellular substance in scaly epithelium, or to minute holes in such spots.
v. t.
Any mark of infamy or disgrace; sign of moral blemish; stain or reproach caused by dishonorable conduct; reproachful characterization.
v. t.
Marks believed to have been supernaturally impressed upon the bodies of certain persons in imitation of the wounds on the crucified body of Christ. See def. 5, above.
n.
A stigma. See Stigma, n., 6 (a) & (b).
v. t.
A mark made with a burning iron; a brand.
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