Analgesic, Heart Rate, and Temperature Effects of &amp;Delta;&lt;sup&gt;8&lt;/sup&gt;-THC during Acute and Chronic Administration to Conscious Rats

Hine, Bromfield; Torrelio, Marina; Gershon, Samuel

doi:10.1159/000136664

Cited by 18 publications

(19 citation statements)

References 14 publications

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“…Beyond the CBD and THC values represented it is important to note that due to the extensive nature of our testing we can confirm that there were no other forms of THC represented in any of the products (Δ8-THC or exo-THC) that can still impart psychotropic properties. 21 Other cannabinoids of interest that may have implications in neurology and inflammation are CBC, CBG and CBN which could not be found in over 50% of products. In products that did contain some of these cannabinoids the concentrations were less than 1 mg/ mL or gram on average with concentrations at high as 1.6 mg/mL in an occasional product.…”

Section: Discussionmentioning

confidence: 99%

Cannabinoid, Terpene, and Heavy Metal Analysis of 29 Over-the-Counter Commercial Veterinary Hemp Supplements

Wakshlag¹,

Cital²,

Eaton³

et al. 2020

VMRR

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Purpose: The use of veterinary low tetrahydrocannabinol (THC) Cannabis sativa (ie, hemp) products has increased in popularity for a variety of pet ailments. Low-THC Cannabis sativa is federally legal for sale and distribution in the USA, and the rise in internet commerce has provided access to interested consumers, with minimal quality control. Materials and Methods: We performed an internet word search of "hemp extract and dog" or "CBD product and dog" and analyzed 29 products that were using low-THC Cannabis sativa extracts in their production of supplements. All products were tested for major cannabinoids including cannabidiol (CBD), Δ9-tetrahydrocannabinol (THC), cannabigerol (CBG), and other minor cannabinoids, as well as their carboxylic acid derivatives (CBDA, THCA, CBGA) using an ISO/IEC 17025 certified laboratory. Products were also tested for major terpenes and heavy metals to understand constituents in the hemp plants being extracted and distributed. Results: All products were below the federal limit of 0.3% THC with variable amounts of CBD (0-88 mg/mL or g). Only two products did not supply a CBD or total cannabinoid concentration on their packaging or website, while 22/29 could supply a certificate of analysis (COA) from a third-party laboratory. Ten of the 27 products were within 10% of the total cannabinoid concentrations of their label claim with a median concentration of 93% of claims (0-154%). Heavy metal contamination was found in 4/29 products, with lead being the most prevalent contaminant (3/29). Conclusion: The products analyzed had highly variable concentrations of CBD or total cannabinoids with only 18 of 29 being appropriately labeled according to current FDA nonmedication, non-dietary supplement or non-food guidelines. Owners and veterinarians wanting to utilize CBD-rich Cannabis sativa products should be aware of low-concentration products and should obtain a COA enabling them to fully discuss the implications of use and calculated dosing before administering to pets.

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Section: Discussionmentioning

confidence: 99%

Cannabinoid, Terpene, and Heavy Metal Analysis of 29 Over-the-Counter Commercial Veterinary Hemp Supplements

Wakshlag¹,

Cital²,

Eaton³

et al. 2020

VMRR

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“…These investigators used brain levels of 5-H1AA as an indicator of changes in serotonin release. On the other hand, Mine et al (8) reported doserelated hypothermia, analgesia and negative chronotropic effects which were unidirectional following i.p. administration of THC at 0 .1 -10.0 mg/kg.…”

Section: Discussionmentioning

confidence: 99%

Comparative Effects of Δ9-Tetrahydrocannabinol, Tetrabenazine and Chlorpromazine on Rectal Temperature in the Rat

Diamantis¹,

Melton²,

Sofia³

1979

Pharmacology

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Tetrabenazine evoked a biphasic response in rectal temperature of the rat following intraperitoneal administration of 4.4–70.0 mg/kg. The initial hyperthermia was inversely related to the dose while the subsequent hypothermia was dose-dependent. This biphasic effect on temperature was similar to that seen with THC at 0.5 mg/kg, thus adding further evidence of a similarity in the mode of action of the two drugs. In contrast, only hypothermia was evident following chlorpromazine administration.

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“…Excess sodium hydride was added to indole (33), which was subsequently alkylated with the appropriate bromoalkane, and then treated with trifluoroacetic anhydride to give the corresponding N-alkyl-3-(trifluoroacetyl)indole (34)(35)(36) in a one-pot process. Alkaline hydrolysis induced fluoroform elimination, 29 Indole SCs derived from L-valinamide (13,15,17) were recrystallized from isopropanol to analytical purity, while those comprising L-tert-leucinamide (14,16,18) were purified by flash chromatography owing to their superior solubility in a range of alcoholic solvents.…”

mentioning

confidence: 99%

“…[30][31][32] Cannabinoids are known to induce hypothermia and bradycardia in rats, effects that are common to phytocannabinoids like ∆ 9 -THC and heteroaromatic SCs such as JWH-018. [33][34][35] We have previously evaluated the hypothermic and bradycardic potencies of ∆ 9 -THC and numerous structurally diverse SCs including JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135. 14,36 The cannabimimetic activities AB-FUBINACA and AB-PINACA were evaluated using radiotelemetry in male Wistar rats, and the effects of these SCs on body temperature ( Fig.…”

mentioning

confidence: 99%

Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA, ADB-PINACA, 5F-AB-PINACA, 5F-ADB-PINACA, ADBICA, and 5F-ADBICA

Banister

Moir

Stuart

et al. 2015

ACS Chem. Neurosci.

212

165

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Synthetic cannabinoid (SC) designer drugs based on indole and indazole scaffolds and featuring l-valinamide or l-tert-leucinamide side chains are encountered with increasing frequency by forensic researchers and law enforcement agencies and are associated with serious adverse health effects. However, many of these novel SCs are unprecedented in the scientific literature at the time of their discovery, and little is known of their pharmacology. Here, we report the synthesis and pharmacological characterization of AB-FUBINACA, ADB-FUBINACA, AB-PINACA, ADB-PINACA, 5F-AB-PINACA, 5F-ADB-PINACA, ADBICA, 5F-ADBICA, and several analogues. All synthesized SCs acted as high potency agonists of CB1 (EC50 = 0.24-21 nM) and CB2 (EC50 = 0.88-15 nM) receptors in a fluorometric assay of membrane potential, with 5F-ADB-PINACA showing the greatest potency at CB1 receptors. The cannabimimetic activities of AB-FUBINACA and AB-PINACA in vivo were evaluated in rats using biotelemetry. AB-FUBINACA and AB-PINACA dose-dependently induced hypothermia and bradycardia at doses of 0.3-3 mg/kg, and hypothermia was reversed by pretreatment with a CB1 (but not CB2) antagonist, indicating that these SCs are cannabimimetic in vivo, consistent with anecdotal reports of psychoactivity in humans.

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Analgesic, Heart Rate, and Temperature Effects of Δ<sup>8</sup>-THC during Acute and Chronic Administration to Conscious Rats

Cited by 18 publications

References 14 publications

<p>Cannabinoid, Terpene, and Heavy Metal Analysis of 29 Over-the-Counter Commercial Veterinary Hemp Supplements</p>

<p>Cannabinoid, Terpene, and Heavy Metal Analysis of 29 Over-the-Counter Commercial Veterinary Hemp Supplements</p>

Comparative Effects of Δ<sup>9</sup>-Tetrahydrocannabinol, Tetrabenazine and Chlorpromazine on Rectal Temperature in the Rat

Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA, ADB-PINACA, 5F-AB-PINACA, 5F-ADB-PINACA, ADBICA, and 5F-ADBICA

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Analgesic, Heart Rate, and Temperature Effects of &Delta;<sup>8</sup>-THC during Acute and Chronic Administration to Conscious Rats

Cited by 18 publications

References 14 publications

<p>Cannabinoid, Terpene, and Heavy Metal Analysis of 29 Over-the-Counter Commercial Veterinary Hemp Supplements</p>

<p>Cannabinoid, Terpene, and Heavy Metal Analysis of 29 Over-the-Counter Commercial Veterinary Hemp Supplements</p>

Comparative Effects of &Delta;<sup>9</sup>-Tetrahydrocannabinol, Tetrabenazine and Chlorpromazine on Rectal Temperature in the Rat

Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA, ADB-PINACA, 5F-AB-PINACA, 5F-ADB-PINACA, ADBICA, and 5F-ADBICA

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Analgesic, Heart Rate, and Temperature Effects of Δ<sup>8</sup>-THC during Acute and Chronic Administration to Conscious Rats

Comparative Effects of Δ<sup>9</sup>-Tetrahydrocannabinol, Tetrabenazine and Chlorpromazine on Rectal Temperature in the Rat