THCV is a somewhat selective cannabinoid receptor type 1 antagonist or, at higher doses, a CB₁ receptor agonist and cannabinoid receptor type 2 partial agonist.^[5] The isomer Δ⁸-THCV has also been shown to be a CB₁ antagonist.^[6] Both papers describing the antagonistic properties of THCV were demonstrated in murine models. THCV is an antagonist of CB₁ receptors and lessens the psychoactive effects of THC.^[7]

THCV also acts as an agonist of GPR55 and l-α-lysophosphatidylinositol (LPI), and beyond the endocannabinoid system, THCV also activate 5-HT1A receptors to produce an antipsychotic effect, that has shown therapeutic potential for ameliorating some of the negative, cognitive and positive symptoms of schizophrenia. THCV furthermore interacts with different transient receptor potential (TRP) channels including TRPV2, which may contribute to the analgesic, anti-inflammatory and anti-cancer effects of cannabinoids and Cannabis extracts. It has also shown anti-epileptiform and anticonvulsant properties, that suggest possible therapeutic application in the treatment of pathophysiologic hyperexcitability states such as untreatable epilepsy.^[8]

THCV is found to inhibit the activity of both fatty acid amide hydrolase (FAAH) and monoacyl glycerol lipase (MGL), even at micromolar concentrations, and thereby able to inhibit the hydrolysis of the endocannabinoids anandamide (AEA: C₂₂H₃₇NO₂; 20:4, ω-6) besides other N-acylethanolamines and 2-Arachidonoylglycerol (2-AG: C₂₃H₃₈O₄; 20:4, ω-6), respectively, therefore, it can also act as an indirect agonist at the cannabinoid receptors, by enhancing the activity of the endocannabinoid system (ECS).^[9][10]

Unlike THC, cannabidiol (CBD), and cannabichromene (CBC), THCV doesn’t begin as cannabigerolic acid (CBGA). Instead of combining with olivetolic acid to create CBGA, geranyl pyrophosphate joins with divarinolic acid, which has two fewer carbon atoms. The result is cannabigerovarin acid (CBGVA). Once CBGVA is created, the process continues exactly the same as it would for THC. CBGVA is broken down to tetrahydrocannabivarin carboxylic acid (THCVA) by the enzyme THCV synthase. At that point, THCVA can be decarboxylated with heat or UV light to create THCV.^[12]

THCV is a new potential treatment against obesity-associated glucose intolerance with pharmacology different from that of CB1 inverse agonists/antagonists.^[14] GW Pharmaceuticals is studying plant-derived tetrahydrocannabivarin (as GWP42004) for type 2 diabetes in addition to metformin.^{[15][better source needed]}

THC increases appetite, which is sometimes referred to as “the munchies“. THC acts as a CB1 agonist. As a CB1 antagonist, THCV has been shown to reduce appetite in murine models.^[16]

A 2:1 ratio of naturally derived THCV to THC extract has been demonstrated to show energizing and motivating effects in a double blind placebo clinical study which relied on a self-reported user survey for results.^[17][18]

It is not scheduled by Convention on Psychotropic Substances. ^{[citation needed]}