PK563217M is a highly selective ligand for the dopamine D7 receptor, Ki 4.2nM at the cloned human receptor. GTP gamma S binding establishes it as a full agonist. It has a clean profile of activity against other dopamine receptors (>500nM); the nearest activity is at D4 (230nM), and no significant interaction with serotinergic, adrenergic, noradrenergic, muscarinic, cholinergic or histamine receptors. The bioavailability of PK563217M is 27% in rat (half-life 5 hours) and 38% in dog (half-life 8 hours). No significant toxicological effects were observed during 28 days dosing in rat and dog at doses below 75mg/kg. PK563217M was formulated in a gel capsule with starch filler for first human dosing
Subjects were recruited from undergraduates of ****** University Medical School and were medically and psychologically profiled before dosing. Subjects were scheduled to receive 5mg capsules of PK563217M for 5 consecutive days, followed by 9 days washout and 2 x 5mg capsules for 5 consecutive days. The individual responses to the initial dosing are reported below.
Samples were taken from the subjects at 30-minute intervals and indicate that PK563217M achieved peak plasma levels 1 hour post dosing with a mean half-life of 10 hours. Continue reading
It was Eclipse Day, and Archer Grey would become the first man in Nereid history to witness two total solar eclipses. Frankly, he couldn’t see what the fuss was about. The moon passed over the sun, everything went dark for a little while and then it returned to normal. Anyone damned fool enough to be staring up without the right spectacles on would go blind, but there was precious little entertainment otherwise.
That was one of the few perks of being ancient. He could moan and grumble and nobody could tell him to shut up. They could try, but as he commanded the family fortune and had known every one of his surviving family since they were mewling babies, they invariably failed. And he had much to grumble about. His children had died, three to old age and one to stupidity. Swimming in the height of summer and expecting the jellyfish of Nereus to leave you alone was the act of a fool. In Kayleigh’s case, the act of a dead fool. Most of his grandchildren ranged from tedious to despicable, though he did enjoy the ever-increasing resentment they felt towards his stubborn refusal to die. Over a hundred years old, and still he clung on.
Until today. Because today was the perfect opportunity to kill himself.
Archer’s mansion was built on a mountain so high it was always night, hence its name: Darkness Falls. Eighty years ago he had ordered a wing built equipped with photoelectric roofs that could become completely transparent at the touch of a button. In truth, he enjoyed the stars, but the real reason behind the construction was to amaze guests, whether visiting dignitaries or impressionable young ladies. Continue reading
Brasidas was waiting for her at Nephros.
“Congratulations on your first kill for The Sun Dancer,” he told her.
She tossed him the maldrive and resisted the urge to test her steel fist on his bloated body. Killing him would be easy, but the ship was in the middle of nowhere and she doubted a crew of pirates would let their captain’s death go unavenged.
Gertrude had no idea where her quarters were, but the thought summoned a diagram of The Sun Dancer in her ocular implant. She was surprised by the ship’s size, and took a moment to examine it. In addition to cargo holds, the mess and crew quarters, The Sun Dancer had not one but two bays for smaller craft. Her mind drifted to where her quarters might be, and an arrow appeared on the plans, guiding her through the narrow, pipe-lined corridors to the cabin she had been allocated.
The cabin was sparsely furnished. A mirror which doubled as an old-fashioned 2-D television was the only decoration. In the locker were two changes of clothes, and the chest of drawers contained a tablet. To her surprise, it also contained what appeared to be several white gold ingots as long as her finger and two flawless sapphires. Uncertain whether they were meant to be hers or belonged to the one-bed cabin’s previous occupant, she swiped the lot. Continue reading
She opened her eyes, and the whole world was different. Her ocular implant depicted a clinic painted in psychedelic hues of deep purples and bright oranges.
Reminds me of the time I tried coral mushrooms.
“Shal ma’kreeth?” Doctor Dubrovnik asked.
Before she could express her confusion a line of blue text appeared in her field of vision.
LANGUAGE IDENTIFIED: J’Karyth.
MESSAGE: How are you?
“I think I’m ok,” she answered.
“Any difficulty breathing?” When she shook her head he nodded. “Good. Each lung cost a bloody fortune. I’m going to activate your artificial limbs, which might feel a bit odd. You can sit up, but don’t try standing until you feel able.”
Her left arm and left leg suddenly tingled with sensation. They felt almost as if they had fallen asleep. She sat up and saw her arm for the first time. Not even the smallest effort had been made to normalise it. The limb wasn’t even painted to resemble flesh, let alone covered with synth-skin and implanted with genuine follicles. Brute bare metal studded with plastic nerves made no pretence of humanity.
Gertrude awoke, and screamed.
A stranger, a doctor, she guessed by his old-fashioned white coat, slapped her twice across the face.
“Keep your damned mouth shut,” he told her.
Heavy leather restraints around her wrists and ankles prevented her retaliating, but her neck was free and she could make out the fact that she was almost entirely naked. Thankfully her slightly singed underwear had been left on, though precious little was left to the imagination. Blazing fire had twisted and corrupted much of her flawless skin into a ruin of burns. Strangely, the tortured skin on the left side of her body did not hurt at all. In fact, she couldn’t feel a damned thing, unlike the right, which a draught had caused to come out in goosebumps. There was, however, a persistent stabbing pain inside her chest, and she felt short of breath.
“What’s my prognosis?” she asked the doctor, trying to keep calm.
“You’re screwed.” Continue reading
The experimental spacecraft’s dashboard fuzzed. Tyrell blinked. The blurriness remained. He flicked his spacesuit’s vitals onto his visor. All green and normal. Relieved, he breathed out. The vitals remained crisp. The fuzz was definitely vacuum-side.
He wiped the outside of his visor. A thin ice layer crazed then shattered into flakes floating away into space. He glanced beyond his cockpit into the Skylon’s hangar deck. The earthlight had grown strong enough to see the sheen of a new veneer covering every surface in sight. The wide even spread meant only one thing. They had had a gas leak, a bad one.
He gritted his teeth, suppressing a groan. Even if they corrected whatever the problem was, Bob and Shirley would block his test flight back to Earth on health and safety grounds. Damn their jealousy. But they were ensconced in their control cabin at the hangar’s other end, not out here taking the risks. Something snapped inside Tyrell. He would make that flight.
Making sure of his grip on the slippery handholds, he hauled himself out of the cockpit and around the spacecraft, searching for gas plumes and unusual ice build-ups. He paid particular attention to each of the two thousand thread nozzles tucked in their cup-like dimples on the spacecraft’s skin. Nothing, not even a telltale of lithium gas. Continue reading
“Are you by nature a religious man, Technician Brandt?”
I looked up from my diagnostics pad at the anthropomorphic bust of Leon Hurst, former CEO of Temple Pharmaceuticals. “Religious, sir? Not really; not beyond a general belief in a higher power.”
It smiled. “Quite the Masonic answer. Furthermore I cannot help but notice the ring which adorns your finger.”
“It was my father’s, Mister Hurst. I wear it in his memory.” I felt uncomfortable discussing my family history with a mere pseudo-human interface and moved the conversation back to more technical matters. “I’ve completed my routine diagnostics and everything seems to be in order, as always.” I unplugged my pad from the plinth, closed the access panel, and stood up.
The lifelike features of Hurst smiled at me, benignly. “I’m sure you’re right, Technician Brandt. You are the most diligent of those who maintain us.”
I inclined my head in acknowledgement of the compliment, even though it was a social interaction protocol, and prepared to leave.
The ‘Opinionated’ gallery took some getting used to and several other technicians had flatly refused to attend, especially after hours. It housed twelve non-sentient personality constructs based on dead corporate executives, designed to provide continued boardroom insight and guidance. Continue reading
Pain erupted as the ibulex burned through my veins. Accelerating when it reached my heart, the drug fired into my arteries like a sling shot; an inferno deep inside my chest. When the agony subsided I saw from the deep impressions left by the restraints that my body had fought on even when my mind was helpless.
Now I sagged, drained. The fire still burned, banked coals throughout my body which could be blown to life at the slightest touch. Even in the warm release-chamber sweat cooled on my skin, leaving a trail of goosebumps behind. Breathing gradually became easier, each breath reassuring me that the worst was over, at least for now.
Voices in the background, a drone which slowly resolved itself into the magistrate reading out the conditions of my release. My exhausted mind wondered if it had been worth it.
I was given civilian clothing, the sort a tramp from the ‘forties might have owned. It had been worn before and came with its own ecosystem of lice and fleas, its own atmosphere of stale body odour. I told myself it was better than being naked and my flight suit had been damaged beyond repair during my capture.
The walk from the detention block to the main gate was an exercise in endurance; cat calls from every shielded window as the entire prison population poured their hatred out at me. I was being released while they still served life sentences, but it wasn’t jealousy that drove them: I had been the most hated prisoner in the facility, in solitary confinement for the last seven years just to keep me alive. Even then there had been attempts on my life. I smiled.
* Winner of the 2014 Story of the Year Award *
Prosecutor General Eve Marshall – the meanest cross-examiner in the courts of New Scotland. Eyes that glint when she goes for the kill, a mouth that tightens at every lie, a manner that pulls jurors in and makes them believe.
And a babe; long hair practically to her waist, glasses she looks over the top of just so, and a way of sucking a pen that keeps men awake at night, and plenty of women, too.
Just my luck to get her on my case.
The jury were hanging on her every word. Sixteen fine upstanding citizens, chosen for this, “the trial of the year”. All of them watching Eve stick her little tongue out, all of them riveted as she put me through three days of questioning.
Three days where I hadn’t cracked, not once. Three days where question after question got hurled at me and I found the right answer. All I needed to do was survive this day and I’d be home and dry.
“So,” she said, in her lispy, false-cute voice. “You can’t tell us where you were the night of the murder, Oskar?”
“No, ma’am. Just that I wasn’t in the Five-in-a-Line store.” Continue reading
I didn’t realise that Sheeps were so large until they crowded around me and I got small and scared. We were inside a square wood home made by the Two-legged, and I went in by mistake because the chief Herder told me to, or at least I thought they told me to. It turned out that was wrong. I regret now that I didn’t understand what they meant – the Two-legged rulers, not the Herders. At the time I was new to everything, including what to do and what not to do, so what happened really was an accident, and not deliberate at all. I also didn’t know that the Two-legged command the Herders.
You know that strange effect when you see your reflection for the very first time, and you know it’s a reflection of you, and you’re really disappointed because you’ve imagined yourself like a superhero? I felt that when – inside the home – I looked at the eyes of the nearest Sheep and saw myself, and realised that the reflection was myself. There was a kind of nighty-night darkness to my body, a small head-ness, and tiny white eyes with metal inserts. I was a small, gleaming version of the Herders. Big ears though, which was odd, because Sheeps have quite small ears compared to mine. So there we were, inside the wood thing, and I was scared and I didn’t know what to do.