Dogs receiving cyclooxygenase-2-sparing nonsteroidal anti-inflammatory drugs and/or nonphysiologic steroids are at risk of severe gastrointestinal ulceration.

Article

Author: Hillier, Townes N ; Heinz, Justin A ; Grimes, Janet A ; Berg, Alexia N ; Dickerson, Vanna M ; Watt, Meghan M

OBJECTIVETo report the incidence and characteristics of gastrointestinal ulceration lesions in dogs receiving an NSAID and/or corticosteroid.ANIMALS33 dogs.CLINICAL PRESENTATIONMedical records of dogs with gastrointestinal ulceration receiving NSAIDs and/or corticosteroids within 30 days of diagnosis between January 2012 and July 2022 at multiple referral institutions were reviewed. Diagnosis was confirmed via endoscopy, surgery, or necropsy. Clinical data were collected from the medical record, including the dose and reason for administration of NSAIDs or steroids.RESULTSDogs received a single NSAID (n = 22, most commonly carprofen [9], meloxicam [4], and deracoxib [3]), 2 NSAIDs (5), a single steroid (5: prednisolone [2], prednisone [2], or dexamethasone SP [1]), or an NSAID and steroid (1). Eleven dogs receiving a single cyclooxygenase (COX)-2-sparing NSAID at an appropriate dose had ulcerations. All dogs receiving 2 NSAIDs concurrently experienced full-thickness perforation (5 of 5). The most common ulcer locations were duodenum (n = 18) and pylorus (11). Abdominal ultrasound correctly identified the site of ulceration in 5 of 24 dogs.CLINICAL RELEVANCEDogs receiving COX-2 sparing NSAIDs at recommended doses are at risk of severe GI ulceration. Carprofen was the most common NSAID resulting in ulceration; however, it is one of the most prescribed NSAIDs. Adding another NSAID and steroid could increase this risk. Careful monitoring is crucial for dogs on NSAIDs, regardless of duration.

01 Sep 2024·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Time-dependent and clustering-induced phosphorescence, mechanochromism, structural-function relationships, and advanced information encryption based on isomeric effects and host–guest doping

Article

Author: Liu, Jiaqi ; Wang, Yongtao ; Ma, Lei ; Zhao, Yupeng ; Guo, Jianmei ; Jiang, Jianfeng

To explore the intrinsic mechanism of pure organic room temperature and clustering-induced phosphorescence and investigate mechanochromism and structural-function relationships, here, 4-(2-(9H-carbazol-9-yl)phenyl)-2-amino-6-methoxypyridine-3,5-dicarbonitrile (Lo-CzAD), 4-(3-(9H-carbazol-9-yl)phenyl)-2-amino-6-methoxypyridine-3,5-dicarbonitrile (Lm-CzAD), and 4-(4-(9H-carbazol-9-yl)phenyl)-2-amino-6-methoxypyridine-3,5-dicarbonitrile (Lp-CzAD) were designed and synthesized by choosing self-made carbazole and 3, 5-dicyanopyridine (DCP) unit as electron acceptor and electron donor in sequence. Compared with crystals Lm-CzAD and Lp-CzAD, crystal Lo-CzAD shows better room temperature phosphorescence (RTP) performance, with RTP lifetimes of 187.16 ms, as well as afterglows 1s, which are attributed to twisted carbazole unit and donor-acceptor (D-A) molecular conformation, big crystal density and spin orbit coupling constant ξ (S₁ → T₁ and S₁ → T₂), as well as intermolecular H type stacking and small ξ (S₀ → T₁). By choosing urea and PPh₃ as host materials and tuning doping ratio, four doping systems were successfully constructed, significantly improving RTP performance of Lo-CzAD and Lp-CzAD, as well as showing different fluorescence and RTP. The lifetimes and afterglows of pure organic Urea/Lo-CzAD and Urea/Lp-CzAD systems are up to 478.42 ms, 5 s, 261.66 ms and 4.5 s in turn. Moreover, Lo-CzAD and Lp-CzAD show time-dependent RTP in doping systems due to monomer and aggregate dispersion, as well as clustering-induced phosphorescence. Based on the different luminescent properties, multiple information encryptions were successfully constructed.

01 Aug 2024·European Journal of Medicinal Chemistry

Identification of 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids as promising DNMT1 inhibitors

Review

Author: Zhang, Qian ; Liu, Yueqin ; Ruan, Minli ; Liu, Jingyi ; Hong, Xiaoqian ; Zhang, Lijun

DNA methyltransferase 1 (DNMT1) is the primary enzyme responsible for maintaining DNA methylation patterns during cellular division, crucial for cancer development by suppressing tumor suppressor genes. In this study, we retained the phthalimide structure of N-phthaloyl-l-tryptophan (RG108) and substituted its indole ring with nitrogen-containing aromatic rings of varying sizes. We synthesized 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids and confirmed them as DNMT1 inhibitors through protein affinity testing, radiometric method using tritium labeled SAM, and MTT assay. Preliminary structure-activity relationship analysis revealed that introducing substituents on the carbazole ring could enhance inhibitory activity, with S-configuration isomers showing greater activity than R-configuration ones. Notably, S-3-(3,6-di-tert-butyl-9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acid (7r-S) and S-3-(1,3,6-trichloro-9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acid (7t-S) exhibited significant DNMT1 enzyme inhibition activity, with IC₅₀ values of 8.147 μM and 0.777 μM, respectively (compared to RG108 with an IC₅₀ above 250 μM). Moreover, they demonstrated potential anti-proliferative activity on various tumor cell lines including A2780, HeLa, K562, and SiHa. Transcriptome analysis and KEGG pathway enrichment of K562 cells treated with 7r-S and 7t-S identified differentially expressed genes (DEGs) related to apoptosis and cell cycle pathways. Flow cytometry assays further indicated that 7r-S and 7t-S induce apoptosis in K562 cells and arrest them in the G0/G1 phase in a concentration-dependent manner. Molecular docking revealed that 7t-S may bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1 with an orientation opposite to RG108, suggesting potential for deeper penetration into the DNMT1 pocket and laying the groundwork for further modifications.

News (Medical) associated with Carprofen

13 Dec 2023

·www.prnewswire.com

Forget Cool Cats -- Dogs are the Real Potheads

Pet Toxicology Experts Release Top 10 Pet Poisons List for 2023, Announce Toxin Tails Voting MINNEAPOLIS, Dec. 13, 2023 /PRNewswire/ -- According to case data released by Pet Poison Helpline, marijuana is on this year's Top 10 Pet Poisons list for dogs, while cats don't seem to be too interested in sampling the jazz cabbage. Chocolate, however, is a toxin that has cross-over appeal to both species. Continue Reading "As more states legalize medical and recreational cannabis, the more marijuana-related calls we are receiving." Post this Toxicology experts at Pet Poison Helpline have released the Top 10 pet toxins of 2023 based on actual medical cases. Pet Poison Helpline provides toxicology advice for all species of animals, including dogs, cats, birds, small mammals, large animals and exotic species. Dog-related incidents account for 88% of calls, 11% are cat-related and the remainder are other species. Here is a list of Pet Poison Helpline's Top 10 Pet Poisons for all species in 2023: Chocolate Grapes/Raisons Ibuprofen Xylitol Bromethalin (Rat Poison) Marijuana Onions/Chives/Leeks/Shallots (Allium species) Anticoagulant Rat Poison Vitamin D3 (supplement) Carprofen (pain medication) "Chocolate is once again our top toxin for all species," explained Dr. Renee Schmid, a senior veterinary toxicologist at Pet Poison Helpline. "Even though it is widely known that pets shouldn't consume chocolate-containing products, they constantly find a way. While chocolate consumption is the number one toxin for dogs, it is the number two poison on the feline list." Common chocolate poisoning signs include hyperactivity, restlessness, vomiting, diarrhea, increased thirst, elevated heart rate, hypertension, abnormal heart rhythms, tremors and hyperthermia. "When we broke down the overall Top 10 Pet Poisons list by cats and dogs, we found some toxins that are specific to each," Schmid explained. " Following is the Top 10 Pet Poisons list for dogs in 2023: Chocolate Grapes/Raisons Xylitol Ibuprofen Bromethalin (Rat Poison) Marijuana Anticoagulant Rat Poison Onions/Chives/Leeks/Shallots (Allium species) Vitamin D3 (supplement) Carprofen (pain medication) "Both marijuana and carprofen made their first appearance on our canine Top 10 list last year, and they appear again on our 2023 list," Dr. Schmid said. "As more states legalize medical and recreational cannabis, the more marijuana-related calls we are receiving. Interestingly, dogs seem to be much more attracted to marijuana, as cannabis didn't make the feline Top 10 list." Carprofen is a prescription pain-relief product approved by the FDA specifically for dogs. While it is an NSAID (non-steroidal anti-inflammatory drug) similar to ibuprofen for humans, it is a safer product for dogs when used at therapeutic dosing levels to treat short and long-term pain. Following is the Top 10 Pet Poisons list for cats in 2023: Lilies Chocolate Onions/Chives/Leeks/Shallots (Allium species) Garlic Ibuprofen Vitamin D3 (supplement) Alstroemeria, Peruvian lily (Alstroemeria species) Amphetamine combos (ADHD medication) Tulips (Tulipa species) Daylily (Hemerocallis species) "Cats are incredibly attracted to plants and flowers, particularly lilies," Dr. Schmid added. "Three different varieties of lilies appear in our feline Top 10 list, which also includes tulips. Surprisingly, marijuana was not on our Top 10 feline list." Many kinds of plants are found or sold with "lily" as part of their name. If you live with cats, it is critical to know which lilies are toxic to your feline friend. The most dangerous and potentially fatal lilies for cats are "true lilies" or those in the genus Lilium. Common examples include Oriental hybrid lilies, roselily, Star Gazer and Casa Blanca lilies—these beautiful, fragrant and affordable flowers are often found in cut-flower bouquets. Other examples include potted Easter lilies or garden plants such as Asiatic and tiger lilies. Additionally, daylilies (Hemerocallis), although not a true lily, may also cause kidney failure in cats. Exposure to any part of the plant, including leaves, flowers, pollen, or even the water from the vase may result in acute kidney failure in cats. These ingestions are medical emergencies requiring immediate veterinary care. Early decontamination, aggressive intravenous fluid therapy, renal function tests, and supportive care greatly improve the cat's prognosis. Dogs may experience minor gastrointestinal upset after ingestion of these lilies but do not appear to develop kidney damage. "While our Top 10 list provides pet lovers with the most common poisons, there are hundreds of toxins that can be dangerous to your pet," Dr. Schmid explained. "We offer a free poison list on our website that helps pet lovers identify potential toxins and provides common symptoms. If you are concerned about something your pet has come in contact with, or has ingested, contact your veterinarian or call us." "If you do need to take your pet to the emergency hospital, we can develop treatment options on your way in," Dr. Schmid added. "In many poisoning cases, time is critical, and most veterinarians value the additional toxicology expertise. In fact, 96% of veterinarians surveyed said they were likely to recommend Pet Poison Helpline to pet owners." In addition to releasing its annual Top 10 toxins list, Pet Poison Helpline created an educational campaign called Toxin Tails to educate the veterinary community and pet lovers on the many types of poisoning dangers facing pets, both in and out of the home. All the pets highlighted in Toxin Tails have been successfully treated for the poisoning and fully recovered. Starting Dec. 15, pet lovers can vote for their favorite Toxin Tails stories of 2023 by visiting petpoisonhelpline.com/vote. About Pet Poison Helpline Pet Poison Helpline®, your trusted source for toxicology and pet health advice in times of potential emergency, is available 24 hours, seven days a week for pet owners and veterinary professionals who require assistance treating a potentially poisoned pet. We are an independent, nationally recognized animal poison control center triple licensed by the Boards of Veterinary Medicine, Medicine and Pharmacy providing unmatched professional leadership and expertise. Our veterinarians and board-certified toxicologists provide treatment advice for poisoning cases of all species, including dogs, cats, birds, small mammals, large animals and exotic species. As the most cost-effective option for animal poison control care, Pet Poison Helpline's fee of $85 per incident includes follow-up consultations for the duration of the case. Based in Minneapolis, Pet Poison Helpline is available in North America by calling 800-213-6680. Additional information can be found online at . For Immediate Release Contact: Dr. Renee Schmid Pet Poison Helpline (952) 806-3803 RSchmid@petpoisonhelpline.com SOURCE Pet Poison Helpline

Drug Approval

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KEGG	Wiki	ATC	Drug Bank
D03410	Carprofen	-	DB00821

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Preclinical	IT	Istituto Italiano di Tecnologia	08 Oct 2012

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2010	Not Applicable	Ophthalmologic surgical procedures	-	Dexamethasone	ncstfyzhqm(ayrsbepbks) = wiymiajvmm tumcqsfxoq (spllcuyexh )	Positive	01 Apr 2010
				Melatonin	ncstfyzhqm(ayrsbepbks) = qvavuhmigb tumcqsfxoq (spllcuyexh )

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