Pharmacologic effects and detection methods of methylated analogs of fentanyl in horses.
Abstract: Pharmacologic effects of alpha-methylfentanyl and 3-methylfentanyl, analogs of fentanyl, were investigated in mares. The ability of an 125I-labeled fentanyl radioimmunoassay (125I-RIA) to detect these methylated fentanyl analogs in individual and pooled urine samples from horses was evaluated. Also, the ability of 7 fentanyl antibodies to react with fentanyl and fentanyl derivatives (sufentanil, alfentanil, and carfentanil) was investigated. Mares were studied in a locomotor test to determine the amount of stimulation methylated fentanyl analogs might induce. Two mares each were given alpha-methylfentanyl at 1, 2, 4, 8, or 13 micrograms/kg of body weight, IV, or 3-methylfentanyl at 0.4, 0.7, or 1 microgram/kg IV. The cross-reactivity of sufentanil, alfentanil, carfentanil, alpha-methylfentanyl, and 3-methylfentanyl with 7 fentanyl antibodies was studied, using the 125I-RIA. All fentanyl analogs, with the exception of alfentanil, cross-reacted well with a C1 antibody raised to fentanyl. Less satisfactory cross-reactivity was determined with 6 other antibodies raised to fentanyl derivatives. When the C1 antibody was combined with an iodinated analog to fentanyl, good detectability of alpha-methylfentanyl and 3-methylfentanyl, in terms of fentanyl equivalents, was obtained from urine samples of dosed mares. The ability of the 125I-RIA to detect methylated fentanyl analogs in forensic urine samples pooled in groups of up to 20 samples was evaluated. When these methylated analogs were administered to mares in doses that induced measurable locomotor stimulation, the analog's presence was readily detected in individual or pooled samples.
Publication Date: 1989-04-01 PubMed ID: 2523679
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- Journal Article
- Research Support
- Non-U.S. Gov't
Summary
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The research investigates the pharmacological effects of two fentanyl analogs, alpha-methylfentanyl and 3-methylfentanyl, in horses and the performance of different antibodies in detecting these analogs in horse urine samples with an iodine-labeled fentanyl radioimmunoassay.
Pharmacological Effects of Methylated Fentanyl Analogs
- The team examined the impact of two methylated fentanyl analogs, alpha-methylfentanyl and 3-methylfentanyl, in mares.
- The potency of these analgesics was determined in a locomotor test, which measured the amount of stimulation they could induce.
- Different doses of these analogs, ranging from 1 to 13 micrograms per kg for alpha-methylfentanyl and from 0.4 to 1 microgram per kg for 3-methylfentanyl, were administered intravenously to two mares each to assess their effects.
Ability of Fentanyl Antibodies to Detect Methylated Fentanyl Analogs
- The effectiveness of different fentanyl antibodies in detecting the two analgesics was examined.
- The study tested seven fentanyl antibodies, determined their compatibility with fentanyl, and its derivatives, including sufentanil, alfentanil, and carfentanil.
- All fentanyl analogs, except alfentanil, demonstrated good cross-reactivity with a certain fentanyl antibody, known as C1 antibody. However, the cross-reactivity of the analogs with the other six antibodies tested, all raised to detect fentanyl derivatives, was considered less satisfactory.
Detection of Methylated Fentanyl Analogs in Urine Samples
- Employing a fentanyl radioimmunoassay marked with iodine-125 (125I-RIA), the researchers then assessed the drug’s detectability in horse urine samples, both individual and pooled.
- When the C1 antibody was combined with an iodine-labeled analog to fentanyl, the scientists were able to detect alpha-methylfentanyl and 3-methylfentanyl in urine samples from dosed mares accurately.
- The effectiveness of this detection method was further evaluated on forensic urine samples pooled from different subjects (up to 20 samples in a group).
- The results showed that if the mares were given doses of the methylated analogs that triggered noticeable stimulation, the presence of these substances was easily detected in individual or pooled samples.
Cite This Article
APA
Weckman TJ, Tai CL, Woods WE, Tai HH, Blake JW, Tobin T.
(1989).
Pharmacologic effects and detection methods of methylated analogs of fentanyl in horses.
Am J Vet Res, 50(4), 502-507.
Publication
Researcher Affiliations
- Department of Veterinary Science, School of Pharmacy, University of Kentucky, Lexington 40546-0076.
MeSH Terms
- Alfentanil
- Analgesics / administration & dosage
- Analgesics / pharmacology
- Analgesics / urine
- Animals
- Female
- Fentanyl / administration & dosage
- Fentanyl / analogs & derivatives
- Fentanyl / pharmacology
- Fentanyl / urine
- Horses / urine
- Motor Activity / drug effects
- Radioimmunoassay
- Sufentanil
- Time Factors
Citations
This article has been cited 2 times.- Smith LC, Bremer PT, Hwang CS, Zhou B, Ellis B, Hixon MS, Janda KD. Monoclonal Antibodies for Combating Synthetic Opioid Intoxication.. J Am Chem Soc 2019 Jul 3;141(26):10489-10503.
- Misailidi N, Papoutsis I, Nikolaou P, Dona A, Spiliopoulou C, Athanaselis S. Fentanyls continue to replace heroin in the drug arena: the cases of ocfentanil and carfentanil.. Forensic Toxicol 2018;36(1):12-32.
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