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Status:
US Approved OTC
Source:
21 CFR 341.14(b)(2) cough/cold:antitussive menthol
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Menthyl lactate is derived from menthol, a compound that comes from peppermint oil, or is made synthetically. Menthol has a natural cooling effect, which makes it useful as a topical analgesic to treat skin irritation, pain, itching or sunburn. Despite its cooling benefits, menthol can be a skin irritant. Like menthol, menthyl lactate is cooling, but it causes less skin irritation than menthol. Menthyl lactate also has a refreshing, minty taste. For this reason, some manufacturers use it as a flavoring ingredient. The compound is recommended for use as a flavor in concentrations of 0.005% to 0.2% and in cosmetic and other external products in concentrations ranging from 0.2% to 2.0%. Menthyl lactate is a known compound available e.g. from Haarmann & Reimer GmbH (Germany) under the name FRESCOLAT, Type ML.
Status:
Investigational
Source:
NCT00839631: Phase 1 Interventional Completed Solid Tumors
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04498182: Phase 2 Interventional Completed Dry Eye Disease
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
WS-12 is a cooling agent and potent TRPM8 agonist. It activates TRPM8 but not related TRP channels like TRPM3 and TRPV6. WS-12 seems to activate TRPM8 mediated cation currents by shifting the voltage dependence of the activation curves to the left toward more physiological membrane potentials. Highly selective TRPM8 activators may be useful for prostate cancer imaging and/or therapy and for therapy in chronic neuropathic pain states.
Status:
Investigational
Source:
NCT01393652: Phase 1 Interventional Completed Healthy Volunteers
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
BCTC is an orally effective mixed TRPV1/TRPM8 antagonist. Inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). BCTC is shown to have robust antihyperalgesic properties
in rat models of inflammatory and neuropathic pain. TRPM8 specific antagonist BCTC demonstrated excellent anti-tumor activity in PCa DU145 cells, and therefore has the potential to become a targeted therapeutic strategy against PCa.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
AG-3-5 (also known as icilin) was first identified as a super-cooling agent in the early 1980s and bears little resemblance to menthol structurally. Icilin is able to activate both TRPM8 and TRPA1 channel activity. Icilin alleviates pain sensation in animal models.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Catharanthine is a terpene indole alkaloid produced by the medicinal plant Catharanthus roseus. Catharanthine is derived from strictosidine, but the exact mechanism by which this happens is currently unknown. Catharanthine is one of the two precursors that form vinblastine, the other being vindoline.
Status:
Possibly Marketed Outside US
First approved in 2000
Source:
21 CFR 348
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Borneol, a monoterpenoid alcohol, is a component of many essential oils. Barneol occurs in nature as a single enantiomer (d- or l-, depending on the oil type) or, less frequently, as the racemate. Several studies have proved the effectiveness of borneol. In Chinese medicines borneol has been used in relieving symptoms of anxiety, fatigue and insomnia; inducing anesthesia and analgesia to alleviate abdominal pain, wounds and burns; relieving rheumatic pain, hemorrhoids, skin diseases and ulcerations of the mouth, ears, eyes or nose; to treat sore throats and skin infections, and is mainly used to treat cardiovascular and cerebrovascular diseases. Borneol has a significant therapeutic effect on neuralgia. This compound is considered a GRAS approved by the FDA as food flavor. Additionally, borneol is a fragrance ingredient. GABAA, TRPV3, TRPM8 and TRPA1 have been identified as the molecular targets of borneol.
Status:
Possibly Marketed Outside US
Source:
ESIKA EXPRESSION ANTIPERSPIRANT ROLL-ON DEODORANT by Winthrop
Source URL:
First approved in 1982
Source:
21 CFR 350
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Hydroxycitronellal is a perfume ingredient with a medium strength floral scent, reminiscent of lily and sweet tropical melon. It is produced synthetically from naturally occurring scent chemical citronellal. It is on the CFR - Code of Federal Regulations Title 21 list of synthetic flavoring substances and adjuvants. Hydroxycitronellal is banned in the European Union because of its toxic properties. Hydroxycitronellal is an allergen. Hydroxycitronellal has being shown to consistently modulate CCR5, CCL27, CCL2 and CCR7 in immature dendritic cells. Hydroxycitronellal is a TRPM8 agonist.
Status:
US Approved OTC
Source:
21 CFR 341.14(b)(2) cough/cold:antitussive menthol
Source URL:
First marketed in 1921
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Menthyl lactate is derived from menthol, a compound that comes from peppermint oil, or is made synthetically. Menthol has a natural cooling effect, which makes it useful as a topical analgesic to treat skin irritation, pain, itching or sunburn. Despite its cooling benefits, menthol can be a skin irritant. Like menthol, menthyl lactate is cooling, but it causes less skin irritation than menthol. Menthyl lactate also has a refreshing, minty taste. For this reason, some manufacturers use it as a flavoring ingredient. The compound is recommended for use as a flavor in concentrations of 0.005% to 0.2% and in cosmetic and other external products in concentrations ranging from 0.2% to 2.0%. Menthyl lactate is a known compound available e.g. from Haarmann & Reimer GmbH (Germany) under the name FRESCOLAT, Type ML.