Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ (lot no. RIS2001-003, specific radioactivity: 6.19 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study, (5/7/02) 99.2%, (5/17/02) 99.1%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin/ lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 75% of the total administered dose was excreted in the urine and 22% in the feces. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups on the benzyl moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione and sulfate adducts. /Z-isomer/
Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Carbonyl-(14)C) S-1264RTZ (/metofluthrin/ lot no. RIS2000-019, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study;(5/8/02) 98.6%, (5/16/02) 99.7%),. Dosing preparations were supplemented with unlabeled S-1264RTZ (lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 57% of the total administered dose was excreted in the urine and 38% in the feces. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione, sulfate and glucuronide adducts. /Z-isomer/
Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ (/metofluthrin z-isomer/ lot no. RIS2001-003, specific radioactivity: 6.19 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 4 times during study, (10/22/01) 99.1%, (10/31/01) 98.6%, (11/19/01) 99.1%, (11/26/01) 99.5%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin z-isomer/ lot no. 010621G, purity: 99.3%). In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 60 to 71% of the administered dose was excreted in the urine and 25 to 36% in the feces with little difference demonstrated between the two dosing levels. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione, sulfate and glucuronide adducts. /Z-isomer/
Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Carbonyl-(14)C) S-1264RTE (/metofluthrin e-isomer/ lot no. RIS2000-020, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.2%; repurified 4 times during study, (3/18/02) 99.0%, (3/26/02) 98.1%, (4/15/02) 99.4%, (4/22/02) 99.2%;). Dosing preparations were supplemented with unlabeled S-1264RTE (/metofluthrin e-isomer/ lot no. 010831G, purity: 96.9%) . In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Biliary Excretion Study, four male rats, whose bile ducts had been cannulated, were dosed with 1 mg/kg of the test material. Bile, urine and fecal samples were collected through 72 hours post-dose. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 29 to 45% of the administered dose was excreted in the urine and 50 to 66% in the feces with little difference demonstrated between the two dosing levels. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of a sulfate adduct. /E-isomer/
Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Carbonyl-(14)C) S-1264RTZ (/metofluthrin z-isomer/ lot no. RIS2000-019, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 4 times during study, (12/3/01) 99.6%, (12/19/1) 98.2%, (2/18/02) 98.6%, (2/25/02) 98.9%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin z-isomer/ lot no. 010621G, purity: 99.3%). In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Biliary Excretion Study, four male rats, whose bile ducts had been cannulated, were dosed with 1 mg/kg of the test material. Bile, urine and fecal samples were collected through 72 hours post-dose. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 44 to 57% of the administered dose was excreted in the urine and 38 to 52% in the feces with little difference demonstrated between the two dosing levels. Air sampling recovered from 0.7 to 1.4% of the administered dose. Seventy four to 83% of the administered dose was recovered in the 1st 24 hours post-dose. In the Bile Excretion Study, 30 to 40% of the dose was recovered in the bile, 25 to 26% in the urine and 30 to 39% in the feces. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione, sulfate and glucuronide adducts. /Z-isomer/
/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand-valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Pyrethrins, pyrethroids, and related compounds/
/SRP:/ Basic treatment: . Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Anticipate seizures and treat if necessary... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool. Administer activated charcoal ... . /Pyrethrins, pyrethroids, and related compounds/
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for air way control in the patient who is unconscious or is in severe respiratory distress. Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias if necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Pyrethrins, pyrethroids, and related compounds/
Skin decontamination. Wash skin promptly with soap and water ... . If irritant or paresthetic effects occur, obtain treatment by a physician. Because volatilization of pyrethroids apparently accounts for paresthesia affecting the face, strenuous measures should be taken (ventilation, protective face mask and hood) to avoid vapor contact with the face and eyes. Vitamin E oil preparations (dL-alpha tocopheryl acetate) are uniquely effective in preventing and stopping the paresthetic reaction. They are safe for application to the skin under field conditions. Corn oil is somewhat effective, but possible side effects with continuing use make it less suitable. Vaseline is less effective than corn oil. Zinc oxide actually worsens the reaction. /Pyrethroids/
Eye contamination. Some pyrethroid compounds can be very corrosive to the eyes. Extraordinary measures should be taken to avoid eye contamination. the eye should be treated immediately by prolonged flushing of the eye with copious amounts of clean water or saline. If irritation persists, obtain professional ophthalmologic care. /Pyrethroids/
Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ (lot no. RIS2001-003, specific radioactivity: 6.19 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study, (5/7/02) 99.2%, (5/17/02) 99.1%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin/ lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 75% of the total administered dose was excreted in the urine and 22% in the feces. The liver and kidneys were the primary sites of radiolabel recovery over the course of the dosing period with the level of radioactivity stabilizing over the dosing period. At 14 days post-final dose, the liver, red blood cell and hair were the primary locations where the radiolabel was recovered. The level of radioactivity recovered from the stomach, small intestine, cecum and large intestine was stabilized or slightly increased over the course of the dosing period. Radiolabel recovered in the hair peaked at the time of the 16th dose. The radiolabel was not sequestered in the fat nor did a significant fraction of the administered dose pass across the blood:brain barrier. ... /Z-isomer/
Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Carbonyl-(14)C) S-1264RTZ (lot no. RIS2000-019, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study;(5/8/02) 98.6%, (5/16/02) 99.7%),. Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin/ lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 57% of the total administered dose was excreted in the urine and 38% in the feces. The liver and kidneys were the primary sites of radiolabel recovery over the course of the dosing period with the level of radioactivity stabilizing over the dosing period. However, at 14 days post-final dose, the red blood cell and hair were the primary locations where the radiolabel was recovered. The level of radioactivity recovered from the stomach, small intestine, cecum and large intestine was stabilized over the course of the dosing period. Radiolabel recovered in the hair peaked at the time of the 21st dose. The radiolabel was not sequestered in the fat nor did a significant fraction of the administered dose pass across the blood:brain barrier. ... /Z-isomer/
Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ (/metofluthrin z-isomer/ lot no. RIS2001-003, specific radioactivity: 6.19 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 4 times during study, (10/22/01) 99.1%, (10/31/01) 98.6%, (11/19/01) 99.1%, (11/26/01) 99.5%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin z-isomer/ lot no. 010621G, purity: 99.3%). In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 60 to 71% of the administered dose was excreted in the urine and 25 to 36% in the feces with little difference demonstrated between the two dosing levels. No radiolabel was recovered in the air sampling. Sixty eight to 84% of the administered dose was recovered in the 1st 24 hours post-dose. The time to maximal blood concentrations ranged from 4.0 to 8.0 hours post-dose. The liver and kidneys were the primary sites of radiolabel recovery over the course of the 7 day collection period. Radioassay of the stomach, small intestine, cecum and large intestine demonstrated a time-course of passage for the radiolabeled compound through the gastrointestinal tract. Radiolabel recovery in the hair peaked later than that observed in the systemic circulation. The radiolabel was not sequestered in the fat nor did a significant fraction of the administered dose pass across the blood:brain barrier. ... /Z-isomer/
Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Carbonyl-(14)C) S-1264RTE (/metofluthrin e-isomer/ lot no. RIS2000-020, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.2%; repurified 4 times during study, (3/18/02) 99.0%, (3/26/02) 98.1%, (4/15/02) 99.4%, (4/22/02) 99.2%;). Dosing preparations were supplemented with unlabeled S-1264RTE (/metofluthrin e-isomer/ lot no. 010831G, purity: 96.9%) . In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Biliary Excretion Study, four male rats, whose bile ducts had been cannulated, were dosed with 1 mg/kg of the test material. Bile, urine and fecal samples were collected through 72 hours post-dose. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 29 to 45% of the administered dose was excreted in the urine and 50 to 66% in the feces with little difference demonstrated between the two dosing levels. Air sampling recovered 0.4 to 0.6% of the administered dose. Sixty five to 78% of the administered dose was recovered in the 1st 24 hours post-dose. In the Bile Excretion Study, 27 and 55% of the dose was recovered in the bile of the males and females, respectively. The greater recovery of the radiolabel in the bile of the females resulted in a decrease of radioactivity recovered from the urine and the feces (urine: 45.1 to 20.4%, feces: 50.2 to 19.6%), For the males, only the urinary recovery of the radiolabel was decreased (37.1 to 9.6%). The males absorbed only 40% of the administered dose in contrast to the 77% demonstrated by the females. The time to maximal blood concentrations ranged from 4.7 to 6.7 hours post-dose, irrespective of the dosing level. The liver was the primary site of radiolabel recovery over the course of the 7 day collection period. Radioassay of the stomach, small intestine, cecum and large intestine demonstrated a time-course of passage for the radiolabeled compound through the gastrointestinal tract. Radiolabel recovery in the hair peaked later than that observed in the systemic circulation. The radiolabel was not sequestered in the fat nor did a significant fraction of the administered dose pass across the blood:brain barrier. ... /E-isomer/
Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Carbonyl-(14)C) S-1264RTZ (/metofluthrin z-isomer/ lot no. RIS2000-019, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 4 times during study, (12/3/01) 99.6%, (12/19/1) 98.2%, (2/18/02) 98.6%, (2/25/02) 98.9%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin z-isomer/ lot no. 010621G, purity: 99.3%). In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Biliary Excretion Study, four male rats, whose bile ducts had been cannulated, were dosed with 1 mg/kg of the test material. Bile, urine and fecal samples were collected through 72 hours post-dose. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 44 to 57% of the administered dose was excreted in the urine and 38 to 52% in the feces with little difference demonstrated between the two dosing levels. Air sampling recovered from 0.7 to 1.4% of the administered dose. Seventy four to 83% of the administered dose was recovered in the 1st 24 hours post-dose. In the Bile Excretion Study, 30 to 40% of the dose was recovered in the bile, 25 to 26% in the urine and 30 to 39% in the feces. The males and females demonstrated 58 and 68% absorption of the administered dose. The time to maximal blood concentrations ranged from 3.3 to 6.7 hours post-dose. The liver and kidneys were the primary sites of radiolabel recovery over the course of the 7 day collection period. Radioassay of the stomach, small intestine, cecum and large intestine demonstrated a time-course of passage for the radiolabeled compound through the gastrointestinal tract. Radiolabel recovery in the hair peaked later than that observed in the systemic circulation. The radiolabel was not sequestered in the fat nor did a significant fraction of the administered dose pass across the blood:brain barrier. ... /Z-isomer/
outstanding insecticidal activity against mosquitoes. In particular, the 2,3,5,6-tetrafluoro-4-methoxymethylbenzyl analog (metofluthrin) exhibits the highest potency, being approximately forty times as potent as d-allethrin in a mosquito coil formulation when tested against southern house mosquitoes (Culex quinquefasciatus). Metofluthrin also exhibits a significant vapor action at room temperature.
A wide temperature water borne sealant that can be applied at low temperatures. The sealant can be a latex sealant composition including at least one latex polymer, at least one freeze thaw stabilizer, and at least one peptone or at least one additive derived from a peptone. The latex polymer can be an acrylic latex polymer with a Glass Transition Temperature (Tg) of 0° C. or less. The peptone can be enzymatic hydrolysate. The sealant can remain pliable at low temperatures making it ideal for applications that require flexibility at low temperatures its' rheology and viscosity are such that it can be applied at temperatures below 0° C. The low Tg latex assures that the sealant will remain permanently flexible and non-tacky when cured, and the peptone provides the sealant with the means to prevent the water from freezing down to approximately −20° C.
