Trends in Pharmacological Sciences
Use of in vivo apparent pA2 analysis in assessment of opioid abuse liability
References (38)
- et al.
Life Sci.
(1982) - et al.
Drug Alcohol Depend.
(1985) - et al.
Eur. J. Pharmacol.
(1989) - et al.
Life Sci.
(1978) - et al.
Drug Alcohol Depend.
(1988) - et al.
Drug Alcohol Depend.
(1987) - et al.
Pharmacol. Biochem. Behav.
(1983) Drug Alcohol Depend.
(1985)- et al.
J. Pharmacol. Meth.
(1986) J. Am. Med. Assoc.
(1988)
J. Pharmacol. Exp. Ther.
J. Pharmacol. Exp. Ther.
J. Pharmacol. Exp. Ther.
J. Pharmacol. Exp. Ther.
J. Pharmacol. Exp. Ther.
J. Pharmacol. Exp. Ther.
J. Pharmacol. Exp. Ther.
Cited by (28)
Antagonism of triazolam self-administration in rhesus monkeys responding under a progressive-ratio schedule: In vivo apparent pA<inf>2</inf> analysis
2016, Drug and Alcohol DependenceCitation Excerpt :We evaluated the antagonists (see Table 1) βCCT (α1GABAA-preferring, Huang et al., 2000); 3-PBC (α1GABAA-preferring; Harvey et al., 2002); and XLi-093 (α5GABAA-selective; Li et al., 2003). When rightward shifts in the triazolam self-administration dose–effect functions were evident, these results were analyzed using in vivo apparent pA2 analysis (Rowlett et al., 2005; Tallarida, 2000; Woods et al., 1992). This analysis enabled us to quantitatively analyze the potency of the antagonists and to draw conclusions or hypotheses about a role for particular receptor subtypes in the reinforcing effects of benzodiazepines.
Using the self-administration of apomorphine and cocaine to measure the pharmacodynamic potencies and pharmacokinetics of competitive dopamine receptor antagonists
2011, Journal of Neuroscience MethodsCitation Excerpt :This is a measure of the absolute potency of the antagonist, which is also the apparent antagonist pA2 (negative logarithm of the antagonist concentration (or dose) required to produce a 2-fold increase in the agonist concentration (or dose) required to induce a defined magnitude of response). Occasional reports have provided pA2 values that have been used to identify the receptor subtypes mediating the discriminative stimulus effects of opiates (Bertalmio and Woods, 1987; Woods et al., 1992), and the self-administration of alfentanil (Bertalmio and Woods, 1989), heroin (Rowlett et al., 1998) and benzodiazepines (Paronis and Bergman, 1999), all of which are direct receptor agonists. The theory of competitive antagonism assumes that the competitive antagonist and the agonist bind reversibly to the same site.
In Vitro and In Vivo Assessment of Mu opioid receptor constitutive activity
2010, Methods in EnzymologyCitation Excerpt :Of the naloxone and naltrexone related compounds we have tested, the majority of them reduce the morphine effect by ~ 50% within 3–5 min and produce near maximal blockade within 10 min. More involved methods are available to estimate antagonist potency including in vivo apparent pA2 analysis (Walker et al., 1994; Woods et al., 1992). An example of this approach using naltrexone analogs is depicted in Fig. 21.9.
Chronic pain, substance abuse and addiction
2003, Nursing Clinics of North AmericaGuidelines and methodological reviews concerning drug abuse liability assessment
2003, Drug and Alcohol DependencePain responses in methadone-maintained opioid abusers
2000, Journal of Pain and Symptom Management