Other Experimental Options for Evaluating Drug Abuse PotentialEx Vivo Binding and Microdialysis


RenaSci offers a battery of other in vitro, ex vivo and in vivo techniques that can be used to investigate the pharmacological mode of action of a drug as this can give an indication of its relative risk of being abused :-

     •     Ex vivo binding to determine compound occupancy of abuse-related receptors,
           binding sites and transporters  
     •     Intracerebral microdialysis in freely-moving rats to assess the abuse potential
           of compounds by their effects on extracellular levels of key neurotransmitters
           eg dopamine or 5-HT and their metabolites
     •     Correlation of drug levels with neurochemistry and behaviour using the
           Culex Bambino/Raturn system (plus drug levels in microdialysates if required)
     •     Neurochemical Fingerprinting - neurochemical phenotyping of substances of abuse
     •     Three Component Test – sequential determination of the effects of drugs on limbic 
           and striatal dopaminergic function (locomotor activity and stereotyped
           behaviour) and brain neurochemistry (dopamine and metabolites) in mice 
     •     Behavioural phenotyping – all types of substances of abuse
     •     Measurement of locomotor activity - stimulants and sedatives
     •     Repeated drug administration to assess the development of drug-induced
           sensitisation (eg hyperactivity or stereotyped behaviour)
     •     Head twitches -  a 5-HT2A  receptor-mediated behaviour in mice that can be used to
           detect potential hallucinogens

Ex Vivo Binding to Determine Compound Occupancy of Abuse-related Transporters
For further information about any of these supplementary tests to evaluate the abuse liability of novel compounds  please get in touch.




Cheetham et al. 2018. Validation of ex vivo receptor occupancy at mu and kappa opioid receptors in rat brain using morphine, buprenorphine and (-)-pentazocine. P105. Presented at Pharmacology 2018, Annual Meeting of the British Pharmacological Society, London, UK, 18th-20th December 2018.

Heal et al. 2018. Use of in vivo intracerebral microdialysis in rats to identify stimulant drugs of abuse. P0009. Presented at the 18th Annual Meeting of the Safety Pharmacology Society, Washington, DC, USA, 30th September-3rd October 2018.