Absorption, Distribution and Excretion
Absorption of camphor in the mucous membranes and the gastrointestinal tract is rapid, and peak concentration following oral ingestion occurs within 5 to 90 minutes.
Camphor undergoes renal excretion.
Volume of distribution of camphor is 2 to 4 L/kg. Camphor and its metabolites are relatively fat-soluble thus may accumulate in adipose and other tissues. Camphor ingested by mothers was present in amnionic fluid, cord and fetal blood and fetal brain, liver and kidneys.
No pharmacokinetic data available.

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Metabolism / Metabolites
(S)-camphor undergoes rapid oxidation to 5-exo-hydroxyfenchone, which is predominantly mediated by human liver microsomal cytochrome (P450). CYP2A6 is the major enzyme involved in the hydroxylation of (-)-camphor by human liver microsomes.

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Biological Half-Life
Following oral ingestion of 200 mg camphor, the half life was 167 minutes.

Protein Binding
No pharmacokinetic data available.

[1]. Manjarrez A, Medina F. The analysis of the volatile oils of the leaves of Artemisia mexicana and Artemisia klotzchiana. Canadian Journal of Chemistry, 1964, 42(9): 2085-2088.

L-camphor appears as colorless or white crystals. Fragrant and penetrating odor. Slightly bitter and cooling taste. Odor index at 68 °F: 40. Flash point 149 °F. Burns with a bright, smoky flame. Sublimes appreciably at room temperature and pressure; 14% sublimes within 60 minutes at 176 °F and 12 mmHg. (NTP, 1992)
(S)-camphor is the S-enantiomer of camphor. It is an enantiomer of a (R)-camphor.
(S)-camphor, or L(-)-Camphor, is a stereoisomer of [DB01744], a bicyclic monoterpene known to potentiate both heat and cold sensations. (S)-camphor is not the naturally-occurring stereoisomer but displays similar TRPV channel affinity and current inhibition. [DB01744] is isolated from the wood of the camphor laurel tree, Cinnamomum camphora, and had a long history of medicinal use. It has been used as a nasal decongestant and cough suppressant, and has been topically applied due to its antipruritic, analgesic, and counterirritant properties. Camphor is a major active ingredient in over-the-counter balms and liniments supplied as topical analgesics by causing sensitization to heat and coolness to relieve minor muscle and joint pain.
(-)-Camphor has been reported in Salvia officinalis, Thymus camphoratus, and other organisms with data available.

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Drug Indication
Indicated for the temporary symptomatic relief of minor aches and pains of muscles and joints in topical analgesics.

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Mechanism of Action
TRPV3 cation channels are molecular sensors that play a role in nociception and thermosensation by inducing thermal sensation and heat-induced hyperalgesia. Camphor interacts with TRPV3 channels via pore-region cysteine residues, leading to channel activation and a rise in intracellular calcium levels. Camphor also activates TRPV1 and a TRPV1-like current in dorsal root ganglion (DRG) neurons but inhibits the ankyrin-repeat TRP 1 (TRPA1) channel expressed in most nociceptive DRG neurons, which is responsible for the detection of temperature. The precise role of TRPA1 current inhibition on the analgesic properties of camphor is unclear. Repeated stimulation by camphor leads to sensitization of the TRPV1 and TRPV3 channels, resulting in desensitization, or reduced channel response that likely leads to the analgesic effects of camphor. Camphor also activates cold-sensitive transient receptor potential melastatin 8 (TRPM8) and sensitizes cold-induced calcium transients, which explains the cooling effect of camphor following dermal application. Additionally, camphor was shown to inhibit the TRPM8 receptor response to menthol.

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Pharmacodynamics
Camphor exerts an analgesic action when applied topically by producing a warm sensation. It excites and desensitizes sensory nerves by activating heat-sensitive TRP vanilloid subtype 1 (TRPV1) and TRPV3 receptors. (S)-camphor is reported to exert a weaker action on TRPV1 channels, which is thought to be a result of tachyphylaxis, which is the reduction of the response to multiple stimulations.

C10H16O

152.24

152.12

464-48-2

444294

Typically exists as solid at room temperature

1.0±0.1 g/cm3

207.4±0.0 °C at 760 mmHg

178-180ºC

64.4±0.0 °C

0.2±0.4 mmHg at 25°C

1.485

2.13

0

1

0

11

217

2

O=C1C([H])([H])C2([H])C([H])([H])C([H])([H])C1(C([H])([H])[H])C2(C([H])([H])[H])C([H])([H])[H]

DSSYKIVIOFKYAU-OIBJUYFYSA-N

InChI=1S/C10H16O/c1-9(2)7-4-5-10(9,3)8(11)6-7/h7H,4-6H2,1-3H3/t7-,10+/m0/s1

(1S,4S)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-one

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)