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The Pharmacology and Therapeutic Potential of Plant Cannabinoids

Abstract

The plant Cannabis sativa has been widely used by humans over many centuries as a source of fibre, for medicinal purposes, for religious ceremonies and as a recreational drug. Since the discovery of its main psychoactive ingredient, Δ9-tetrahydrocannabinol (THC), significant progress has been made towards the understanding (1) of the in vitro and in vivo pharmacology both of THC and of certain other cannabis-derived compounds, and (2) of the potential and actual uses of these “phytocannabinoids” as medicines. There is now extensive evidence that the pharmacological effects of some widely-studied phytocannabinoids, are due to their ability to interact with cannabinoid receptors and/or with other kinds of pharmacological targets, including non-cannabinoid receptors, and this makes the pharmacology of the phytocannabinoids rather complex and interesting. In this chapter, we provide an overview of the in vitro pharmacology of five selected phytocannabinoids and report findings that have identified potential new therapeutic uses for these compounds.

Keywords

  • Mouse Brain Membrane
  • House Musk Shrew
  • TRPM8 Cation Channel
  • Cannabidiolic Acid
  • TRPV3 Cation Channel

These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Fig. 9.1

Abbreviations

THC:

Tetrahydrocannabinol

CBD:

Cannabidiol

CBG:

Cannabigerol

THCV:

Tetrahydrocannabivarin

CBC:

Cannabichromene

CBDV:

Cannabidivarin

CBDA:

Cannabidiolic acid

CBGV:

Cannabigerovarin

CBGA:

Cannabigerolic acid

THCA:

Tetrahydrocannabinolic acid

THCVA:

Tetrahydrocannabivarinic acid

TRP:

Transient receptor potential

PPAR:

Peroxisome-proliferator activated receptor

GPCR:

G-protein coupled receptor

CB:

Cannabinoid

HT:

Hydroxytryptamine

8-OH-DPAT:

8-hydroxy-2-(di-n-propylamino)-tetralin

HU-201:

6aR,10aR)- 9-(Hydroxymethyl)- 6,6-dimethyl- 3-(2-methyloctan-2-yl)- 6a,7,10,10a-tetrahydrobenzo [c]chromen- 1-ol

WIN55212:

[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone mesylate

CP55940:

(-)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hydroxypropyl)cyclohexanol

GTPγS:

Guanosine 5′-O-[gamma-thio]triphosphate)

AMP:

Adenosine monophosphate

ERK:

Extracellular signal-regulated kinases

CHO:

Chinese hamster ovary

NAM:

Negative allosteric modulator

SR141716A:

N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride

WAY100135:

(S)-N-tert-Butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide dihydrochloride

WAY100635:

N-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexanecarboxamide maleate

AM251:

N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide

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Correspondence to Maria Grazia Cascio .

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Cascio, M.G., Pertwee, R.G., Marini, P. (2017). The Pharmacology and Therapeutic Potential of Plant Cannabinoids. In: Chandra, S., Lata, H., ElSohly, M. (eds) Cannabis sativa L. - Botany and Biotechnology. Springer, Cham. https://doi.org/10.1007/978-3-319-54564-6_9

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