![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
Vol. 286, Issue 3, 1301-1308, September 1998
Department of Pharmacology and Toxicology, Medical College of
Virginia/Virginia Commonwealth University, Richmond, Virginia
We evaluated delta-9 tetrahydrocannabinol
(
9-THC), delta-8 tetrahydrocannabinol
(8-THC), CP55,940 (CP55),
1-deoxy-11-hydroxy-8-THC-dimethylheptyl (deoxy-HU210, a
CB2-selective cannabinoid that also binds the CB1 receptor) and the
endogenous cannabinoid anandamide (ANA) via i.c.v. and/or
intrathecal (i.t.) routes of administration, alone and in combination
with SR141716A (SR), a CB1 antagonist, using the tail-flick test. Our
studies were performed in order better to characterize potential
diversity in interactions of the cannabinoids with the cannabinoid
(CB1) receptor. When SR was administered i.c.v. or i.p. before
9-THC, 8-THC or CP55 (i.c.v. or i.t.), SR
was a potent antagonist and the blockade was complete (AD50 
8.1 µg/mouse i.c.v. or AD50 1.4 mg/kg i.p.). The
AD50 values (dose of antagonist that produced a 50%
antagonism of agonist effects) for blockade of 9-THC,
8-THC, CP55,940 (i.c.v. or i.t.) by SR (i.c.v. or i.p.)
differed significantly for only two combinations
[8-THC/SR, both i.c.v. and CP55 (i.t.)/SR (i.p.)].
Conversely, SR (i.t.) produced an incomplete block of the
antinociceptive effects of i.t. 9-THC,
8-THC and CP55 (AD50 = 28.6, 50.2 and 20.9 µg/mouse, respectively). Blockade of the deoxy-HU210 (i.c.v.) by SR
(either i.c.v. or i.p.) was incomplete and AD50 values
could not be calculated. Although the maximal blockade of deoxy-HU210
(i.t.) by SR (i.t.) was only 50%, SR administered i.p. before
deoxy-HU210 (i.t.) produced a potent and complete blockade
(AD50 = 0.4 mg/kg). The effects of SR on ANA-induced
antinociception were mixed. The maximal attenuation of the ANA (i.t.)
by SR (i.t.) was 38%. SR (i.p.) blockade of ANA was complete, but the
AD50 was 15.4 mg/kg, greater than 15-fold higher than that
required to block 9-THC, 8-THC, CP55 or
deoxy-HU210. In addition, SR (i.p. or i.t.) failed to block the
hypothermic effects of ANA (i.t.), while completely reversing the
hypothermic effects of 9-THC (i.t.). These data indicate
that SR has a much greater efficacy at supraspinal than at spinal
sites. Alternatively, such data suggest either a differential
interaction of the cannabinoids at the CB1 receptor or the existence of
subtypes of the CB1 receptor.
This article has been cited by other articles:
|
|
 |
|
  K. Benamar, E. B. Geller, and M. W. Adler First in Vivo Evidence for a Functional Interaction between Chemokine and Cannabinoid Systems in the Brain J. Pharmacol. Exp. Ther., May 1, 2008; 325(2): 641 - 645. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 C. Liu and J. M. Walker Effects of a Cannabinoid Agonist on Spinal Nociceptive Neurons in a Rodent Model of Neuropathic Pain J Neurophysiol, December 1, 2006; 96(6): 2984 - 2994. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. J. Khodayar, B. Shafaghi, N. Naderi, and M.-R. Zarrindast Antinociceptive effect of spinally administered cannabinergic and 2-adrenoceptor drugs on the formalin test in rat: possible interactions J Psychopharmacol, January 1, 2006; 20(1): 67 - 74. [Abstract] [PDF]
|
|
|
|
 |
|
 C. A. Newton, T. Lu, S. J. Nazian, I. Perkins, H. Friedman, and T. W. Klein The THC-induced suppression of Th1 polarization in response to Legionella pneumophila infection is not mediated by increases in corticosterone and PGE2 J. Leukoc. Biol., October 1, 2004; 76(4): 854 - 861. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. Duncan, D. A. Kendall, and V. Ralevic Characterization of Cannabinoid Modulation of Sensory Neurotransmission in the Rat Isolated Mesenteric Arterial Bed J. Pharmacol. Exp. Ther., October 1, 2004; 311(1): 411 - 419. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
L. B. Hough, J. W. Nalwalk, R. Stadel, H. Timmerman, R. Leurs, B. C. Paria, X. Wang, and S. K. Dey Inhibition of Improgan Antinociception by the Cannabinoid (CB)1 Antagonist N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A): Lack of Obligatory Role for Endocannabinoids Acting at CB1 Receptors J. Pharmacol. Exp. Ther., October 1, 2002; 303(1): 314 - 322. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. M. Rawls, J. Cabassa, E. B. Geller, and M. W. Adler CB1 Receptors in the Preoptic Anterior Hypothalamus Regulate WIN 55212-2 [(4,5-Dihydro-2-methyl-4(4-morpholinylmethyl)-1-(1-naphthalenyl-carbonyl)-6H-pyrrolo[3,2,1ij]quinolin-6-one]-Induced Hypothermia J. Pharmacol. Exp. Ther., June 1, 2002; 301(3): 963 - 968. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 A. C. Howlett, F. Barth, T. I. Bonner, G. Cabral, P. Casellas, W. A. Devane, C. C. Felder, M. Herkenham, K. Mackie, B. R. Martin, et al. International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors Pharmacol. Rev., June 1, 2002; 54(2): 161 - 202. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 B. L. Hungund and B. S. Basavarajappa ARE ANANDAMIDE AND CANNABINOID RECEPTORS INVOLVED IN ETHANOL TOLERANCE? A REVIEW OF THE EVIDENCE Alcohol Alcohol., March 1, 2000; 35(2): 126 - 133. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
