Kenner C. Rice

National Institute on Alcohol Abuse and Alcoholism

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Arthur E. Jacobson

National Institute on Drug Abuse

199

Richard B. Rothman

National Institutes of Health

161

Agnieszka Sulima

National Institute on Alcohol Abuse and Alcoholism

Christina M. Dersch

National Institute on Drug Abuse

Kejun Cheng

Ruttonjee Hospital

Arthur E. Jacobson

National Institute on Drug Abuse

Linda R. Watkins

University of Colorado Boulder

Jeffrey R. Deschamps

United States Naval Research Laboratory

John S. Partilla

National Institute on Drug Abuse

Gregory T. Collins

The University of Texas Health Science Center at San Antonio

Cooperative Institutions

National Institutes of Health

550

National Institute on Drug Abuse

319

National Institute on Alcohol Abuse and Alcoholism

178

National Institute of Diabetes and Digestive and Kidney Diseases

146

University of Michigan–Ann Arbor

125

National Institute of Mental Health

101

University of Colorado Boulder

100

University of Arizona

Harvard University

Johns Hopkins University

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CCDC 955757: Experimental Crystal Structure Determination

The Cambridge Structural Database (2014)

Fuying Li Kejun Cheng Joshua F. G. Antoline Malliga R. Iyer Gary R. Matyas

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

10.5517/cc112jwj

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Citations (0)

Studies of the biogenic amine transporters. VII. Characterization of a novel cocaine binding site identified with [125I]RTI-55 in membranes prepared from human, monkey and guinea pig caudate

Synapse (1998)

Richard B. Rothman M L Silverthorn John R. Glowa Dorota Matecka Kenner C. Rice

[125I]RTI-55 is a cocaine analog with high affinity for dopamine (DA) and serotonin (5-HT) transporters. Quantitative ligand binding studies revealed a novel high affinity [125I]RTI-55 binding site assayed under 5-HT transporter (SERT) conditions which has low affinity for almost all classic biogenic amine transporter ligands, including high affinity 5-HT transporter inhibitors such as paroxetine, but which retains high affinity for cocaine analogs. This site, termed SERT(site2) for its detection under 5-HT transporter conditions (not for an association with the SERT) occurs in monkey caudate, human caudate, and guinea pig caudate membranes, but not in rat caudate membranes. SERT(site2) is distinguished from the DA transporter (DAT) and SERT by several criteria, including a distinct ligand-selectivity profile, the inability to detect SERT(site2) in cells stably expressing the cloned human DAT, and insensitivity to irreversible ligands which inhibit [125I]RTI-55 binding to the DAT and SERT. Perhaps the most striking finding about SERT(site2) is that a wide range of representative antidepressant agents have very low affinity for SERT(site2). The affinity of cocaine for this site is not very different from the concentration cocaine achieves in the brain at pharmacological doses. Viewed collectively with the observation that ligands with high affinity for SERT(site2) are mostly cocaine analogs, these data lead us to speculate that actions of cocaine which differ from those of classic biogenic amine uptake inhibitors may be mediated in part via SERT(site2).

Biogenic amine

10.1002/(sici)1098-2396(199804)28:4<322::aid-syn8>3.0.co;2-b

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Citations (25)

Phencyclidine binds to blood platelets with high affinity and specifically inhibits their activation by adrenaline

Biochemical Journal (1992)

Graham Jamieson A.K. Agrawal Nicholas J. Greco Thomas E. Tenner G D Jones

The ion channel probe phencyclidine [1-(1-phenylcyclohexyl)piperidine; PCP] selectively inhibited aggregation, secretion and ultrastructural changes in platelets induced by adrenaline, but did not affect activation induced by other common platelet agonists such as alpha-thrombin, ADP, collagen or ionophore A23187. [3H]PCP bound to platelets with high affinity (Kd 134 +/- 33 nM; 3600 +/- 1020 sites/platelet), as did the thienyl analogue [3H]TCP (1-[1-(2-thienyl)cyclohexyl]piperidine). PCP binding to platelets was increased 3-4-fold in N-methylglucamine buffer in the absence of Na+ ions. Binding was unaffected by haloperidol and was only weakly inhibited (EC50 10-20 microM), without significant stereoselectivity by the two sets of stereoselective ligands, dexoxadrol/levoxadrol and (+)MK801/(-)MK801. Binding of PCP was not competed for by adrenaline or yohimbine. Only the high-affinity binding of [3H]PCP to platelets was blocked by prior treatment of the platelets with the covalent affinity probe Metaphit, and these platelets no longer aggregated in response to adrenaline although they responded normally to alpha-thrombin, ADP and collagen. These results suggest that platelets contain high-affinity receptors for PCP that can modulate adrenaline-induced platelet activation.

Phencyclidine

Piperidine

10.1042/bj2850035

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Citations (8)

Effectiveness comparisons of G-protein biased and unbiased mu opioid receptor ligands in warm water tail-withdrawal and drug discrimination in male and female rats

Neuropharmacology (2019)

Kathryn L. Schwienteck Kaycee E. Faunce Kenner C. Rice Samuel Obeng Yan Zhang

Nalbuphine

μ-opioid receptor

Etorphine

10.1016/j.neuropharm.2019.01.020

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Citations (44)

A Journey through Diastereomeric Space: The Design, Synthesis, In Vitro and In Vivo Pharmacological Activity, and Molecular Modeling of Novel Potent Diastereomeric MOR Agonists and Antagonists

Molecules (2022)

Dana R. Chambers Agnieszka Sulima Dan Luo Thomas E. Prisinzano Alexander Goldberg

Four sets of diastereomeric C9-alkenyl 5-phenylmorphans, varying in the length of the C9-alkenyl chain, were designed to examine the effect of these spatially distinct ligands on opioid receptors. Functional activity was obtained by forskolin-induced cAMP accumulation assays and several compounds were examined in the [35S]GTPgS assay and in an assay for respiratory depression. In each of the four sets, similarities and differences were observed dependent on the length of their C9-alkenyl chain and, most importantly, their stereochemistry. Three MOR antagonists were found to be as or more potent than naltrexone and, unlike naltrexone, none had MOR, KOR, or DOR agonist activity. Several potent MOR full agonists were obtained, and, of particular interest partial agonists were found that exhibited less respiratory depression than that caused by morphine. The effect of stereochemistry and the length of the C9-alkenyl chain was also explored using molecular modeling. The MOR antagonists were found to interact with the inactive (4DKL) MOR crystal structures and agonists were found to interact with the active (6DDF) MOR crystal structures. The comparison of their binding modes at the mouse MOR was used to gain insight into the structural basis for their stereochemically induced pharmacological differences.

Diastereomer

Molecular model

Structure–activity relationship

10.3390/molecules27196455

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Citations (8)

A rapid, high-yield conversion of codeine to morphine

Journal of Medicinal Chemistry (1977)

Kenner C. Rice

Brief treatment of codeine (1) in chloroform with boron tribromide has consiste-tly given morphine (2) in 90-91% yield after a simple isolation procedure. The yield and simplicity of operation in this method are vastly superior to those previously reported for this transformation.

10.1021/jm00211a036

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Citations (109)

The Effects of Norbinaltorphimine Preexposure on THC‐induced Place and Taste Avoidance in Sprague‐Dawley Rats.

The FASEB Journal (2015)

Shaun M. Flax Alison Wakeford Kenner C. Rice Anthony L. Riley

Studying the mechanisms that modulate cannabinoid abuse potential is important, given that it is the most widely used drug of abuse in the United States. Although a drug's abuse potential is thought to be mediated by the balance between its rewarding and aversive effects, little is known about the aversive effects of Δ 9 ‐tetrahydrocannabinol (THC), the main psychoactive constituent of cannabis, and how these effects might vary with specific experiential and subject factors. The aversive effects of THC have been studied in CB57/BL mice using the place conditioning design, and these studies have argued that activity at the kappa opioid receptor (KOR) mediates the aversive effects of THC. Specifically, both genetic ablation and pharmacological antagonism of the KOR system blocks THC‐induced place avoidance. Given reported differences between mice and rats in other behavioral preparations, it is not known if this effect is evident in other species. To address this, the present experiment assessed the effects of the KOR antagonist, norbinaltorphimine (norBNI), on THC‐induced place and taste avoidance in Sprague‐Dawley rats. Specifically, rats were injected with 15 mg/kg of norBNI 24h prior to the pairing of a distinct side of a place conditioning chamber (Experiment 1) or a novel taste (Experiment 2) with one of three doses of THC (0.56, 1.0 and 3.2 mg/kg). Independent of the specific assay, norBNI had no significant effect on the aversive effects of THC. These data suggest that the specific mediation of THC's aversive effects by KOR activity may be species dependent.

Δ9-tetrahydrocannabinol

κ-opioid receptor

Taste aversion

Conditioned place preference

Aversive Stimulus

10.1096/fasebj.29.1_supplement.1019.15

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Citations (0)

Methylone pre-exposure differentially impacts the aversive effects of MDPV and MDMA in male and female Sprague-Dawley rats: Implications for abuse vulnerability

Pharmacology Biochemistry and Behavior (2022)

Hayley N. Manke Katharine H. Nelson Shihui Huang Jacob Bailey Sara K. Bowman

MDMA

Ecstasy

Cathinone

Mephedrone

Methamphetamine

10.1016/j.pbb.2022.173470

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Citations (3)

Partial Synthesis of 3-Deoxydihydromorphine from (—)-4-Hydroxy-6-keto-N-methylmorphinan

Heterocycles (1979)

Arnold Brossi Fu‐Lian Hsu Arthur E. Jacobson Kenner C. Rice

Conversion of (-)-3-de~~dihydromorphine (3 into (-)-4-hydrony-6-keto-N-methylmorphinan (5) and reconversion of 2 into L via the ketone f : is described.The morphinan structure of 5 -was proven by reduction to the known (-)-4-hydroxy-Nmethylmorphinan (3.3-Deoxydihydromorphine (2) and 3-de~x~dih~dromorphinone (9, easily obtainable from dihydromorphine (9'.represent valuable intermediates for the preparation of a variety of anrinociceptive 3-deo~yopioids.~In addition the ketone 4, with the ether bridge linked at the u-position of the . ., carbonyl group, constitutes an important entry into the relatiyely unexplored class of 4-hydrolty-m~rphinans.~Such a conversion could be accomplished as fallows: 1. 8 1 = R 3 = OH, R 2 = H -

Carbonyl group

10.3987/s-1979-01-0259

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Citations (11)

Effects of phentermine and fenfluramine on extracellular dopamine and serotonin in rat nucleus accumbens: Therapeutic implications

Synapse (2000)

Michael H. Baumann Mario Ayestas Christina M. Dersch Alicia Brockington Kenner C. Rice

Combined administration of the amphetamine analogs phentermine and fenfluramine (PHEN/FEN) has been used in the treatment of obesity. While these medications are thought to modulate monoamine transmission, the precise neurochemical effects of the PHEN/FEN mixture have not been extensively studied. To assess the mechanism of PHEN/FEN action, in vivo microdialysis studies were performed in the nucleus accumbens of conscious freely moving rats. A series of amphetamine derivatives including phentermine, chlorphentermine, fenfluramine, and PHEN/FEN (1:1 ratio), were infused locally into the accumbens via reverse-dialysis (1, 10, 100 microM) or injected systemically (1 mg/kg, ip). Dialysate samples were assayed for dopamine (DA) and serotonin (5-HT) by high-performance liquid chromatography with electrochemical detection. When infused locally, phentermine preferentially increased extracellular DA, whereas fenfluramine selectively increased extracellular 5-HT. Local administration of chlorphentermine or the PHEN/FEN mixture caused parallel elevations of both transmitters. Analogous results were obtained when the drugs were injected systemically. Phentermine stimulated robust locomotor activity in mice, whereas chlorphentermine and fenfluramine did not. PHEN/FEN caused modest locomotor stimulation after a low dose, but had no effect at the highest dose. Accumulating evidence suggests that chronic drug and alcohol abuse is associated with deficits in both DA and 5-HT neuronal function. Thus, dual activation of DA and 5-HT neurotransmission with monoamine releasing agents may be an effective treatment strategy for substance use disorders, as well as for obesity. Synapse 36:102-113, 2000. Published 2000 Wiley-Liss, Inc.

Phentermine

10.1002/(sici)1098-2396(200005)36:2<102::aid-syn3>3.0.co;2-#

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Citations (101)