Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect

Srivastava, B.; Soni, Rina; Patel, Jayendra Z.; Joharapurkar, Amit; Sadhwani, Nisha; Kshirsagar, Samadhan; Mishra, Bhupendra; Takale, Vijay; Gupta, Sunil; Pandya, Purvi; Kapadnis, Prashant B.; Solanki, Manish; Patel, Harilal; Mitra, Prasenjit; Jain, Mukul; Patel, Pankaj

doi:10.1016/j.bmcl.2009.03.046

Cited by 26 publications

(12 citation statements)

References 28 publications

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“…Because CB 1 , unlike CB 2 , is expressed in a hair-cycle-dependent manner in the human HF epithelium, these data support the idea that human HFs exploit a CB 1 -mediated endocannabinoid signaling system that might act as an autocrine–paracrine negative regulator of human hair growth. Consistently with this idea, a recent study has demonstrated that CB 1 receptor antagonists do, indeed, induce hair growth in mice [54]. …”

Section: Role Of the Cutaneous Ecs In Skin Growth Control Survival Amentioning

confidence: 64%

The endocannabinoid system of the skin in health and disease: novel perspectives and therapeutic opportunities

Bı́ró

Tóth

Haskó³

et al. 2009

Trends in Pharmacological Sciences

219

171

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The newly discovered endocannabinoid system (ECS; comprising the endogenous lipid mediators endocannabinoids present in virtually all tissues, their G-protein-coupled cannabinoid receptors, biosynthetic pathways and metabolizing enzymes) has been implicated in multiple regulatory functions both in health and disease. Recent studies have intriguingly suggested the existence of a functional ECS in the skin and implicated it in various biological processes (e.g. proliferation, growth, differentiation, apoptosis and cytokine, mediator or hormone production of various cell types of the skin and appendages, such as the hair follicle and sebaceous gland). It seems that the main physiological function of the cutaneous ECS is to constitutively control the proper and well-balanced proliferation, differentiation and survival, as well as immune competence and/or tolerance, of skin cells. The disruption of this delicate balance might facilitate the development of multiple pathological conditions and diseases of the skin (e.g. acne, seborrhea, allergic dermatitis, itch and pain, psoriasis, hair growth disorders, systemic sclerosis and cancer).

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Section: Role Of the Cutaneous Ecs In Skin Growth Control Survival Amentioning

confidence: 64%

The endocannabinoid system of the skin in health and disease: novel perspectives and therapeutic opportunities

Bı́ró

Tóth

Haskó³

et al. 2009

Trends in Pharmacological Sciences

219

171

View full text Add to dashboard Cite

show abstract

“…Subsequently, tricarbonyl compound 3 and 2,4-dichlorophenylhydrazine were heated in ethanol [18] to afford the pyrazole 4 in rather modest yield (32%). The latter was regioselectively brominated, [19] employing NBS as bromine source, to afford the corresponding bromothiophene 5 in good yield (83%).…”

Section: Synthesis Of 123-triazolyl Compoundsmentioning

confidence: 99%

Pyrazoles with a “click” 4-[N-(4-fluorobutyl)-1,2,3-triazole] substituent in position 3 are nanomolar CB1 receptor ligands

Distinto

Zanato

Montanari

et al. 2014

Journal of Fluorine Chemistry

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“…mast cells, cutaneous nerve fibers, epidermal keratinocytes, and cells of the adnexal tissues [182,199,207,271,272,275,276]. While hair growth appears to be under CB 1 -mediated endocannabinoid signaling control (CB 1 antagonists promote hair growth in mice [277]), CB 2 receptors may be involved in control of lipid production and cell death in sebocytes [272]. …”

Section: Effects Of Cb2 Receptor Modulation In Disease Statesmentioning

confidence: 99%

Is lipid signaling through cannabinoid 2 receptors part of a protective system?

Pacher

Mechoulam

2011

Progress in Lipid Research

379

344

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The mammalian body has a highly developed immune system which guards against continuous invading protein attacks and aims at preventing, attenuating or repairing the inflicted damage. It is conceivable that through evolution analogous biological protective systems have been evolved against non-protein attacks. There is emerging evidence that lipid endocannabinoid signaling through cannabinoid 2 (CB 2 ) receptors may represent an example/part of such a protective system/ armamentarium. Inflammation/tissue injury triggers rapid elevations in local endocannabinoid levels, which in turn regulate signaling responses in immune and other cells modulating their critical functions. Changes in endocannabinoid levels and/or CB 2 receptor expressions have been reported in almost all diseases affecting humans, ranging from cardiovascular, gastrointestinal, liver, kidney, neurodegenerative, psychiatric, bone, skin, auto-immune, lung disorders to pain and cancer, and modulating CB 2 receptor activity holds tremendous therapeutic potential in these pathologies. While CB 2 receptor activation in general mediates immunosuppressive effects, which limit inflammation and associated tissue injury in large number of pathological conditions, in some disease states activation of the CB 2 receptor may enhance or even trigger tissue damage, which will also be discussed alongside the protective actions of the CB 2 receptor stimulation with endocannabinoids or synthetic agonists, and the possible biological mechanisms involved in these effects.

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Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect

Cited by 26 publications

References 28 publications

The endocannabinoid system of the skin in health and disease: novel perspectives and therapeutic opportunities

The endocannabinoid system of the skin in health and disease: novel perspectives and therapeutic opportunities

Pyrazoles with a “click” 4-[N-(4-fluorobutyl)-1,2,3-triazole] substituent in position 3 are nanomolar CB1 receptor ligands

Is lipid signaling through cannabinoid 2 receptors part of a protective system?

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