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The Info List - 8-Phenyltheophylline


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(i) (i) (i)

8-PHENYLTHEOPHYLLINE (8-PHENYL-1,3-DIMETHYLXANTHINE, 8-PT) is a drug derived from the xanthine family which acts as a potent and selective antagonist for the adenosine receptors A1 and A2A , but unlike other xanthine derivatives has virtually no activity as a phosphodiesterase inhibitor . It has stimulant effects in animals with similar potency to caffeine . Coincidentally 8-phenyltheophylline has also been found to be a potent and selective inhibitor of the liver enzyme CYP1A2
CYP1A2
which makes it likely to cause interactions with other drugs which are normally metabolised by CYP1A2.

SEE ALSO

* 8-Chlorotheophylline * 8-Cyclopentyltheophylline * DPCPX * DMPX * Xanthine

REFERENCES

* ^ Scotini E; Carpenedo F; Fassina G (February 1983). "New derivatives of methyl-xanthines: effect of thiocaffeine thiotheophylline and 8-phenyltheophylline on lipolysis and on phosphodiesterase activities". Pharmacological Research Communications. 15 (2): 131–43. doi :10.1016/s0031-6989(83)80055-1 . PMID 6844374 . * ^ Rabe KF; Magnussen H; Dent G (April 1995). " Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants". European Respiratory Journal. 8 (4): 637–42. PMID 7664866 . * ^ Howell LL; Morse WH; Spealman RD (September 1990). "Respiratory effects of xanthines and adenosine analogs in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics. 254 (3): 786–91. PMID 2395111 . * ^ Spealman RD (1988). "Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism". Psychopharmacology. 95 (1): 19–24. doi :10.1007/bf00212759 . PMID 3133696 . * ^ Murray S; Odupitan AO; Murray BP; Boobis AR; Edwards RJ (March 2001). "Inhibition of human CYP1A2
CYP1A2
activity in vitro by methylxanthines: potent competitive inhibition by 8-phenyltheophylline". Xenobiotica. 31 (3): 135–51. doi :10.1080/00498250110043292 . PMID 11465391 .

* v * t * e

Purine receptor modulators

Receptor (ligands )

P0 (ADENINE )

* AGONISTS: 8-Aminoadenine * Adenine
Adenine

P1 (adenosine )

* AGONISTS: 2-(1-Hexynyl)-N-methyladenosine * 2-Cl-IB-MECA * 2\'-MeCCPA * 4\'-O-β-D-Glucosyl-9-O-(6\'\'-deoxysaccharosyl)olivil * 5\'-N-ethylcarboxamidoadenosine * Adenosine
Adenosine
* ADP * AMP * Apadenoson * ATL-146e
ATL-146e
* ATP * BAY 60–6583 * Binodenoson * Capadenoson * CCPA * CGS-21680 * CP-532,903 * Evodenoson * GR 79236 * LUF-5835 * LUF-5845 * N6-Cyclopentyladenosine * Namodenoson * Neladenoson dalanate * Piclidenoson * Regadenoson * SDZ WAG 994 * Selodenoson * Sonedenoson * Tecadenoson * UK-432,097

* ANTAGONISTS: 8-Chlorotheophylline * 8-Phenyl-1,3-dipropylxanthine * 8-Phenyltheophylline * Acefylline * Aminophylline * ATL-444 * Bamifylline * Cafedrine * Caffeine
Caffeine
* Caffeine
Caffeine
citrate * Cartazolate * CGH-2466 * CGS-15943 * Choline theophyllinate * CPX * CVT-6883 * Dimethazan * DMPX * DPCPX * Dyphylline * Enprofylline * Etazolate * Fenethylline * IBMX * Isovaleric acid * Istradefylline * KF-26777 * MRE3008F20 * MRS-1220 * MRS-1334 * MRS-1706 * MRS-1754 * MRS-3777 * Paraxanthine * Pentoxifylline * Preladenant * Propentofylline * Proxyphylline * PSB-10 * PSB-11 * PSB-36 * PSB-603 * PSB-788 * PSB-1115 * Reversine * Rolofylline * SCH-442,416 * SCH-58261 * Theacrine * Theobromine
Theobromine
* Theodrenaline * Theophylline * Tozadenant * Tracazolate * VUF-5574 * ZM-241,385

P2 (nucleotide )

P2X (ATP )

* AGONISTS: 2-Me-SATP * α,β-Me-ATP * Adenosine
Adenosine
* ADP * AMP * Ap4A * Ap5A * ATP * ATPγS * BzATP * Cibacron blue * CTP * D-β,γ-Me-ATP * GTP * HT-AMP * Ivermectin * L-β,γ-Me-ATP * MRS-2219 * PAPET-ATP * UTP * Zinc
Zinc

* ANTAGONISTS: 5-BDBD * A-317491 * A-438079 * A-740003 * A-804598 * A-839977 * AF-353 * AZ-10606120 * AZ-11645373 * BBG * Calcium
Calcium
* Calmidazolium * Chelerythrine
Chelerythrine
* Copper
Copper
* Emodin ( Rheum officinale ) * Evans Blue * GW-791343 * HMA * Ip5I * iso PPADS * JNJ-47965567 * KN-04 * KN-62 * Magnesium
Magnesium
* MRS-2159 * NF-023 * NF-110 * NF-157 * NF-279 * NF-449 * Opiranserin (VVZ-149) * Oxidized-ATP * Phenol Red
Phenol Red
* Phenolphthalein * PPADS * PPNDS * PSB-12062 * Puerarin ( Radix puerariae ) * Purotoxin 1 * RB-2 * Ro 0437626 * Ro 51 * RO-3 * Sodium ferulate ( Angelica sinensis , Ligusticum wallichii ) * Suramin
Suramin
* TC-P 262 * Tetramethylpyrazine (ligustrazine) ( Ligusticum wallichii ) * TNP-ATP * Zinc
Zinc

P2Y

* AGONISTS: 2-Me-SADP * 2-Me-SATP * 2-Thio-UTP * 5-Br-UDP * 5-OMe-UDP * α,β-Me-ATP * Adenosine
Adenosine
* ADP * ADPβS * Ap3A * AR-C 67085MX * ATP * ATPγS * CTP * dATP * Denufosol * Diquafosol * IDP * ITP * INS-365 * INS-37217 * MRS-2365 * MRS-2690 * MRS-2693 * MRS-2768 * MRS-2957 * MRS-4062 * NF-546 * PAPET-ATP * PSB-0474 * PSB-1114 * UDP * UDPβS * UDP-galactose * UDP-glucose * UDP-N-acetylglucosamine * Up3U * UTP * UTPγS

* ANTAGONISTS: 2-Me-SAMP * A3P5PS * AMPαS * Ap4A * AR-C 66096 * AR-C 67085MX * AR-C 69931MX * AR-C 118925XX * ATP * BzATP * C1330-7 * Cangrelor * Clopidogrel * Elinogrel * Ip5I * MRS-2179 * MRS-2211 * MRS-2279 * MRS-2395 * MRS-2500 * MRS-2578 * NF-157 * NF-340 * PIT * PPADS * Prasugrel * PSB-0739 * RB-2 * Regrelor * Suramin
Suramin
* Ticagrelor * Ticlopidine * UDP

Transporter (blockers )

CNTS

* 6-Hydroxy-7-methoxyflavone * Adenosine
Adenosine
* dMeThPmR * Estradiol
Estradiol
* KGO-2142 * KGO-2173 * MeThPmR * Phloridzin * Progesterone
Progesterone

ENTS

* Barbiturates * Benzodiazepines * Cilostazol * Dilazep * Dipyridamole * Estradiol
Estradiol
* Ethanol
Ethanol
* Hexobendine * NBMPR * Pentoxifylline * Progesterone
Progesterone
* Propentofylline

PMAT

* Decynium-22

Enzyme (inhibitors )

XO

* Allopurinol * Amflutizole * Benzbromarone * Caffeic acid
Caffeic acid
* Cinnamaldehyde
Cinnamaldehyde
* Cinnamomum osmophloeum * Febuxostat * Myo-inositol
Myo-inositol
* Kaempferol * Myricetin * Niraxostat * Oxipurinol * Phytic acid
Phytic acid
* Pistacia integerrima * Propolis * Quercetin
Quercetin
* Tisopurine * Topiroxostat

OTHERS

* Aminopterin * Azathioprine
Azathioprine
* Methotrexate
Methotrexate
* Mycophenolic acid * Pemetrexed * Pralatrexate * Many others

OTHERS

* PRECURSORS: Adenine
Adenine
* Adenosine
Adenosine
* AMP * ADP * ATP * Cytosine
Cytosine
*